Laduviglusib (CHIR-99021)

別名:CT99021

ラドゥビグルシブ (Laduviglusib (CHIR-99021、CT99021)) は GSK-3α および GSK-3β 阻害剤であり、IC50 はそれぞれ 10 nM および 6.7 nM です。 ラドゥビグルシブは、サイクリン依存性キナーゼ (CDK) に対して交差反応性を示さず、CDK と比較して GSK-3β に対して 350 倍の選択性を示します。 Laduviglusib は Wnt/β-catenin 活性化因子として機能し、オートファジー (autophagy) を誘導します。

Laduviglusib (CHIR-99021)化学構造

CAS No. 252917-06-9

サイズ 価格(税別) 在庫状況
JPY 29500 国内在庫あり
JPY 41500 国内在庫あり
JPY 101500 国内在庫あり
JPY 190500 国内在庫あり
JPY 445500 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(819)

製品安全説明書

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Laduviglusib (CHIR-99021)と併用されることが多い化合物

SB431542


Laduviglusib and SB431542, along with other small molecules, enhance the neuronal conversion efficiency of mouse astrocytes.


Wang J, et al. Front Bioeng Biotechnol. 2022 Jul 7;10:799152.

Y-27632 2HCl


Laduviglusib and Y-27632 2HCl, along with other small molecules, enhance the neuronal conversion efficiency of mouse astrocytes.


Wang J, et al. Front Bioeng Biotechnol. 2022 Jul 7;10:799152.

DAPT


Laduviglusib and DAPT, along with other small molecules, enhance the neuronal conversion efficiency of mouse astrocytes.


Wang J, et al. Front Bioeng Biotechnol. 2022 Jul 7;10:799152.

LDN-193189


Laduviglusib and LDN-193189, in conjunction with specific growth factors, facilitate the directed differentiation of human induced pluripotent stem cells (hiPSCs) into functional cardiac myocytes.


Winanto, et al. Cell Death Dis. 2020 Mar 13;11(3):182.

Laduviglusib (CHIR-99021)関連製品

シグナル伝達経路

GSK-3阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
ES-CCE Function Assay 5 μM 3 d Strongly induces the activity of Wnt/beta-catenin pathway 24779365
ES-D3 Function Assay 5 μM 3 d Strongly induces the activity of Wnt/beta-catenin pathway 24779365
ES-CCE Cytotoxic Assay 10 μM 3 d Induces moderate cytotoxicity 24779365
ES-D3 Cytotoxic Assay 10 μM 3 d Induces moderate cytotoxicity with IC50 of 4.9 μM 24779365
Neural progenitor cells Function Assay 3 μM 10 d Induces generation of neural progenitor cells 24638034
A549 Apoptosis Assay 5 µM 24 h Increases cell apoptosis 24367688
H157 Apoptosis Assay 5 µM 24 h Does not significantly affect apoptosis 24367688
H460 Apoptosis Assay 5 µM 24 h Attenuates cell apoptosis 24367688
H157 Growth Inhibition Assay 5 µM 24 h Promotes cell proliferation 24367688
H460 Growth Inhibition Assay 5 µM 24 h Promotes cell proliferation 24367688
embryonic stem cells (ESC) Function Assay 3 µM 11 d Promotes self-renewal of naïve-type mouse embryonic stem cells (ESC) 23843312
DN3 Function Assay 10 μM 96 h Increases cell development and proliferation 23526989
platelets Function Assay 10 μM 15 min Increases thrombin-mediated platelet aggregation and ATP secretion 23239877
hiPSC-NPs Growth Inhibition Assay 3 μM 72 h Increases cell proliferation  22642687
INS-1E Function Assay 2.5 μM 24 h Induces a reduction of NP1 overexpression 22427704
PANC1 Apoptosis Assay  5 μM 72 h Triggers an apoptotic response 22201186
HMC1.2 Growth Inhibition Assay 30 μM 72 h Reduces cell survival 22039301
Sca-1+ HPC Growth Inhibition Assay 2 μM 6 d Synergistically promotes Sca-1+ HPC proliferation and colony formation together with EGF 21624348
Oct4/Sox2/Klf4-infected MEFs Function Assay 10 μM 28 d Promotes MEFs reprogramming Transduced by Oct4, Sox2, and Klf4 19839055
H4IIE Function Assay 10 μM 24 h Regulates β-catenin activity and TIRE containing promoter activity 15350195
insulin receptor–expressing CHO-IR Function Assay 500 nM 30 min Activates Glycogen Synthase (GS) 12606497
3T3-L1 Function Assay 3 μM 4 h Inhibits preadipocyte differentiation 12055200
Endothelial cell(EC) Function Assay 3 μM Promotes endothelial cell (EC) differentiation 22052006
CHO-IR Function Assay 30 min EC50=0.77 μM 29016121
HepG2 Function Assay 3 h EC50=1.5 μM 22261023
JVM-3 Growth Inhibition Assay IC50=198.419 μM SANGER
TE-5 Growth Inhibition Assay IC50=198.033 μM SANGER
IA-LM Growth Inhibition Assay IC50=197.822 μM SANGER
22RV1 Growth Inhibition Assay IC50=197.424 μM SANGER
TE-1 Growth Inhibition Assay IC50=196.26 μM SANGER
SW780 Growth Inhibition Assay IC50=196.734 μM SANGER
KOSC-2 Growth Inhibition Assay IC50=195.818 μM SANGER
SW1088 Growth Inhibition Assay IC50=195.677 μM SANGER
HGC-27 Growth Inhibition Assay IC50=195.538 μM SANGER
COLO-668 Growth Inhibition Assay IC50=193.157 μM SANGER
A2780 Growth Inhibition Assay IC50=192.891 μM SANGER
HCE-4 Growth Inhibition Assay IC50=190.992 μM SANGER
NCI-H838 Growth Inhibition Assay IC50=190.34 μM SANGER
ETK-1 Growth Inhibition Assay IC50=190.181 μM SANGER
KG-1 Growth Inhibition Assay IC50=189.798 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=188.719 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=188.428 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=187.453 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=187.392 μM SANGER
MDA-MB-453 Growth Inhibition Assay IC50=186.941 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=185.209 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=185.145 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=184.972 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=184.651 μM SANGER
DOK Growth Inhibition Assay IC50=184.643 μM SANGER
A427 Growth Inhibition Assay IC50=184.631 μM SANGER
SN12C Growth Inhibition Assay IC50=182.829 μM SANGER
LOUCY Growth Inhibition Assay IC50=182.688 μM SANGER
HT55 Growth Inhibition Assay IC50=199.192 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=200.116 μM SANGER
SJRH30 Growth Inhibition Assay IC50=200.515 μM SANGER
COLO-679 Growth Inhibition Assay IC50=200.859 μM SANGER
MFM-223 Growth Inhibition Assay IC50=201.587 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=200.902 μM SANGER
MFE-280 Growth Inhibition Assay IC50=201.961 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=202.073 μM SANGER
LS-1034 Growth Inhibition Assay IC50=202.553 μM SANGER
NCI-H345 Growth Inhibition Assay IC50=203.027 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=203.879 μM SANGER
EGI-1 Growth Inhibition Assay IC50=204.833 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=205.467 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=206.73 μM SANGER
HPAF-II Growth Inhibition Assay IC50=209.671 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=209.678 μM SANGER
DJM-1 Growth Inhibition Assay IC50=209.897 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=210.381 μM SANGER
EW-18 Growth Inhibition Assay IC50=210.763 μM SANGER
BT-20 Growth Inhibition Assay IC50=210.986 μM SANGER
A431 Growth Inhibition Assay IC50=211.299 μM SANGER
TCCSUP Growth Inhibition Assay IC50=211.533 μM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=212.894 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=214.185 μM SANGER
ES7 Growth Inhibition Assay IC50=214.878 μM SANGER
C3A Growth Inhibition Assay IC50=215.575 μM SANGER
UACC-257 Growth Inhibition Assay IC50=217.43 μM SANGER
DMS-153 Growth Inhibition Assay IC50=217.836 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=217.893 μM SANGER
HOS Growth Inhibition Assay IC50=218.9 μM SANGER
THP-1 Growth Inhibition Assay IC50=219.606 μM SANGER
SCC-4 Growth Inhibition Assay IC50=220.353 μM SANGER
SCC-3 Growth Inhibition Assay IC50=220.577 μM SANGER
BC-1 Growth Inhibition Assay IC50=220.799 μM SANGER
NCI-H1618 Growth Inhibition Assay IC50=221.018 μM SANGER
CaR-1 Growth Inhibition Assay IC50=221.251 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=221.377 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=222.239 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=222.389 μM SANGER
AGS Growth Inhibition Assay IC50=222.523 μM SANGER
SAS Growth Inhibition Assay IC50=223.796 μM SANGER
HCC1937 Growth Inhibition Assay IC50=224.389 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=226.53 μM SANGER
NCI-H322M Growth Inhibition Assay IC50=228.019 μM SANGER
CHL-1 Growth Inhibition Assay IC50=228.13 μM SANGER
NCI-H630 Growth Inhibition Assay IC50=232.897 μM SANGER
5637 Growth Inhibition Assay IC50=233.003 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=233.276 μM SANGER
YAPC Growth Inhibition Assay IC50=234.253 μM SANGER
SW1783 Growth Inhibition Assay IC50=234.41 μM SANGER
GB-1 Growth Inhibition Assay IC50=235.177 μM SANGER
NCI-H520 Growth Inhibition Assay IC50=235.741 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=236.02 μM SANGER
NCCIT Growth Inhibition Assay IC50=236.873 μM SANGER
SW954 Growth Inhibition Assay IC50=237.868 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=241.209 μM SANGER
EB2 Growth Inhibition Assay IC50=241.907 μM SANGER
IPC-298 Growth Inhibition Assay IC50=242.072 μM SANGER
GP5d Growth Inhibition Assay IC50=242.616 μM SANGER
HN Growth Inhibition Assay IC50=242.991 μM SANGER
BFTC-909 Growth Inhibition Assay IC50=243.118 μM SANGER
ES5 Growth Inhibition Assay IC50=245.038 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=246.043 μM SANGER
T47D Growth Inhibition Assay IC50=247.013 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=247.517 μM SANGER
LC-1F Growth Inhibition Assay IC50=248.156 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=249.495 μM SANGER
COR-L23 Growth Inhibition Assay IC50=250.412 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=250.864 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=251.417 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=252.875 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=253.156 μM SANGER
CAL-27 Growth Inhibition Assay IC50=253.485 μM SANGER
NCI-H187 Growth Inhibition Assay IC50=256.76 μM SANGER
HSC-2 Growth Inhibition Assay IC50=258.584 μM SANGER
CAL-39 Growth Inhibition Assay IC50=260.272 μM SANGER
HuH-7 Growth Inhibition Assay IC50=260.996 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=261.192 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=261.918 μM SANGER
A673 Growth Inhibition Assay IC50=267.025 μM SANGER
LU-165 Growth Inhibition Assay IC50=267.941 μM SANGER
CAL-12T Growth Inhibition Assay IC50=268.366 μM SANGER
RD Growth Inhibition Assay IC50=269.119 μM SANGER
MDA-MB-468 Growth Inhibition Assay IC50=269.333 μM SANGER
LN-405 Growth Inhibition Assay IC50=269.708 μM SANGER
MHH-CALL-2 Growth Inhibition Assay IC50=269.92 μM SANGER
ES3 Growth Inhibition Assay IC50=270.358 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=275.457 μM SANGER
TE-10 Growth Inhibition Assay IC50=276.439 μM SANGER
BEN Growth Inhibition Assay IC50=276.461 μM SANGER
NB69 Growth Inhibition Assay IC50=277.405 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=278.279 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=279.187 μM SANGER
UACC-893 Growth Inhibition Assay IC50=280.54 μM SANGER
TGW Growth Inhibition Assay IC50=283.058 μM SANGER
SH-4 Growth Inhibition Assay IC50=283.123 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=283.953 μM SANGER
T84 Growth Inhibition Assay IC50=284.665 μM SANGER
EW-7 Growth Inhibition Assay IC50=285.232 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=286.035 μM SANGER
GMS-10 Growth Inhibition Assay IC50=287.183 μM SANGER
HC-1 Growth Inhibition Assay IC50=290.602 μM SANGER
ABC-1 Growth Inhibition Assay IC50=291.069 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=292.146 μM SANGER
HT-1197 Growth Inhibition Assay IC50=292.879 μM SANGER
SHP-77 Growth Inhibition Assay IC50=295.597 μM SANGER
NCI-H524 Growth Inhibition Assay IC50=295.769 μM SANGER
SW626 Growth Inhibition Assay IC50=296.115 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=296.425 μM SANGER
U251 Growth Inhibition Assay IC50=298.438 μM SANGER
RL95-2 Growth Inhibition Assay IC50=300.247 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=300.691 μM SANGER
HLE Growth Inhibition Assay IC50=301.818 μM SANGER
COLO-680N Growth Inhibition Assay IC50=302.893 μM SANGER
PLC-PRF-5 Growth Inhibition Assay IC50=304.907 μM SANGER
SCC-15 Growth Inhibition Assay IC50=306.017 μM SANGER
ECC12 Growth Inhibition Assay IC50=310.254 μM SANGER
A388 Growth Inhibition Assay IC50=312.022 μM SANGER
ES1 Growth Inhibition Assay IC50=312.189 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=313.521 μM SANGER
SNU-475 Growth Inhibition Assay IC50=314.091 μM SANGER
647-V Growth Inhibition Assay IC50=314.673 μM SANGER
IMR-5 Growth Inhibition Assay IC50=315.38 μM SANGER
EW-24 Growth Inhibition Assay IC50=320.07 μM SANGER
CAL-51 Growth Inhibition Assay IC50=321.403 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=321.409 μM SANGER
EW-13 Growth Inhibition Assay IC50=322.424 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=322.452 μM SANGER
BHY Growth Inhibition Assay IC50=323.175 μM SANGER
OCUB-M Growth Inhibition Assay IC50=323.434 μM SANGER
HCC1954 Growth Inhibition Assay IC50=323.582 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=324.111 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=326.489 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=326.738 μM SANGER
LS-123 Growth Inhibition Assay IC50=328.164 μM SANGER
SF268 Growth Inhibition Assay IC50=330.265 μM SANGER
BT-474 Growth Inhibition Assay IC50=332.418 μM SANGER
NCI-H1522 Growth Inhibition Assay IC50=334.339 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=336.591 μM SANGER
LAN-6 Growth Inhibition Assay IC50=336.977 μM SANGER
ARH-77 Growth Inhibition Assay IC50=337.32 μM SANGER
HuO9 Growth Inhibition Assay IC50=337.47 μM SANGER
MLMA Growth Inhibition Assay IC50=338.155 μM SANGER
Raji Growth Inhibition Assay IC50=338.38 μM SANGER
GT3TKB Growth Inhibition Assay IC50=338.412 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=341.418 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=341.609 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=342.636 μM SANGER
KP-4 Growth Inhibition Assay IC50=343.733 μM SANGER
PF-382 Growth Inhibition Assay IC50=344.422 μM SANGER
NB13 Growth Inhibition Assay IC50=345.58 μM SANGER
D-502MG Growth Inhibition Assay IC50=345.812 μM SANGER
CAL-54 Growth Inhibition Assay IC50=345.879 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=346.65 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=347.426 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=349.846 μM SANGER
SW1990 Growth Inhibition Assay IC50=351.28 μM SANGER
NCI-H2196 Growth Inhibition Assay IC50=352.624 μM SANGER
P30-OHK Growth Inhibition Assay IC50=353.063 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=355.356 μM SANGER
CW-2 Growth Inhibition Assay IC50=356.529 μM SANGER
COLO-678 Growth Inhibition Assay IC50=357.863 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=358.521 μM SANGER
DMS-53 Growth Inhibition Assay IC50=358.711 μM SANGER
NCI-H1838 Growth Inhibition Assay IC50=359.987 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=360.939 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=363.924 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=372.926 μM SANGER
U-266 Growth Inhibition Assay IC50=373.132 μM SANGER
P31-FUJ Growth Inhibition Assay IC50=376.964 μM SANGER
HCC2157 Growth Inhibition Assay IC50=378.161 μM SANGER
COR-L88 Growth Inhibition Assay IC50=383.677 μM SANGER
NCI-H596 Growth Inhibition Assay IC50=385.34 μM SANGER
GOTO Growth Inhibition Assay IC50=390.641 μM SANGER
NCI-H719 Growth Inhibition Assay IC50=391.893 μM SANGER
MN-60 Growth Inhibition Assay IC50=393.948 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=394.406 μM SANGER
TE-6 Growth Inhibition Assay IC50=397.254 μM SANGER
SW962 Growth Inhibition Assay IC50=398.69 μM SANGER
FADU Growth Inhibition Assay IC50=403.083 μM SANGER
ECC4 Growth Inhibition Assay IC50=408.458 μM SANGER
MES-SA Growth Inhibition Assay IC50=409.98 μM SANGER
NCI-H716 Growth Inhibition Assay IC50=410.075 μM SANGER
GR-ST Growth Inhibition Assay IC50=410.497 μM SANGER
KY821 Growth Inhibition Assay IC50=414.086 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=424.388 μM SANGER
MDA-MB-134-VI Growth Inhibition Assay IC50=431.033 μM SANGER
RH-1 Growth Inhibition Assay IC50=435.09 μM SANGER
AM-38 Growth Inhibition Assay IC50=438.54 μM SANGER
BL-70 Growth Inhibition Assay IC50=439.429 μM SANGER
COLO-684 Growth Inhibition Assay IC50=448.888 μM SANGER
DMS-79 Growth Inhibition Assay IC50=449.68 μM SANGER
EW-1 Growth Inhibition Assay IC50=452.888 μM SANGER
MS-1 Growth Inhibition Assay IC50=454.385 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=454.507 μM SANGER
TALL-1 Growth Inhibition Assay IC50=455.297 μM SANGER
SCLC-21H Growth Inhibition Assay IC50=455.699 μM SANGER
KMS-12-PE Growth Inhibition Assay IC50=456.822 μM SANGER
TE-441-T Growth Inhibition Assay IC50=457.186 μM SANGER
A3-KAW Growth Inhibition Assay IC50=460.841 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=463.943 μM SANGER
COR-L279 Growth Inhibition Assay IC50=464.847 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=472.28 μM SANGER
JAR Growth Inhibition Assay IC50=474.788 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=477.08 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=480.869 μM SANGER
D-283MED Growth Inhibition Assay IC50=488.924 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=489.004 μM SANGER
RPMI-6666 Growth Inhibition Assay IC50=491.398 μM SANGER
CPC-N Growth Inhibition Assay IC50=502.063 μM SANGER
EC-GI-10 Growth Inhibition Assay IC50=502.169 μM SANGER
CA46 Growth Inhibition Assay IC50=504.407 μM SANGER
EHEB Growth Inhibition Assay IC50=507.208 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=510.021 μM SANGER
DU-4475 Growth Inhibition Assay IC50=511.101 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=511.416 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=512.439 μM SANGER
NCI-H2171 Growth Inhibition Assay IC50=512.705 μM SANGER
Mo-T Growth Inhibition Assay IC50=515.116 μM SANGER
HL-60 Growth Inhibition Assay IC50=522.924 μM SANGER
NCI-H1436 Growth Inhibition Assay IC50=523.064 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=524.696 μM SANGER
NCI-H2081 Growth Inhibition Assay IC50=525.513 μM SANGER
NB5 Growth Inhibition Assay IC50=526.43 μM SANGER
NCI-H2227 Growth Inhibition Assay IC50=530.254 μM SANGER
HSC-4 Growth Inhibition Assay IC50=539.293 μM SANGER
RL Growth Inhibition Assay IC50=542.442 μM SANGER
EVSA-T Growth Inhibition Assay IC50=543.684 μM SANGER
NCI-H889 Growth Inhibition Assay IC50=547.23 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=551.35 μM SANGER
EW-11 Growth Inhibition Assay IC50=552.399 μM SANGER
UACC-812 Growth Inhibition Assay IC50=559.391 μM SANGER
CAL-148 Growth Inhibition Assay IC50=565.089 μM SANGER
K052 Growth Inhibition Assay IC50=579.213 μM SANGER
L-428 Growth Inhibition Assay IC50=600.671 μM SANGER
LP-1 Growth Inhibition Assay IC50=603.587 μM SANGER
ML-2 Growth Inhibition Assay IC50=606.579 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=618.221 μM SANGER
HT Growth Inhibition Assay IC50=622.785 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=628.353 μM SANGER
L-363 Growth Inhibition Assay IC50=648.064 μM SANGER
IM-9 Growth Inhibition Assay IC50=651.541 μM SANGER
TUR Growth Inhibition Assay IC50=671.322 μM SANGER
NCI-SNU-16 Growth Inhibition Assay IC50=680.462 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=690.172 μM SANGER
U-87-MG Growth Inhibition Assay IC50=694.585 μM SANGER
KM-H2 Growth Inhibition Assay IC50=699.059 μM SANGER
DEL Growth Inhibition Assay IC50=700.838 μM SANGER
KARPAS-422 Growth Inhibition Assay IC50=789.315 μM SANGER
BC-3 Growth Inhibition Assay IC50=805.203 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=818.059 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=900.231 μM SANGER
ONS-76 Growth Inhibition Assay IC50=182.387 μM SANGER
SBC-5 Growth Inhibition Assay IC50=181.934 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=181.672 μM SANGER
PSN1 Growth Inhibition Assay IC50=181.66 μM SANGER
NCI-H522 Growth Inhibition Assay IC50=181.059 μM SANGER
SF126 Growth Inhibition Assay IC50=179.432 μM SANGER
NB10 Growth Inhibition Assay IC50=177.846 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=177.806 μM SANGER
COLO-741 Growth Inhibition Assay IC50=177.561 μM SANGER
EW-3 Growth Inhibition Assay IC50=176.555 μM SANGER
YT Growth Inhibition Assay IC50=176.399 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=175.861 μM SANGER
SW756 Growth Inhibition Assay IC50=174.863 μM SANGER
ME-180 Growth Inhibition Assay IC50=174.016 μM SANGER
HH Growth Inhibition Assay IC50=173.848 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=172.273 μM SANGER
SW620 Growth Inhibition Assay IC50=171.535 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=171.032 μM SANGER
Daoy Growth Inhibition Assay IC50=169.891 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=169.636 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=168.415 μM SANGER
Calu-3 Growth Inhibition Assay IC50=168.311 μM SANGER
JVM-2 Growth Inhibition Assay IC50=167.451 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=168.309 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=167.354 μM SANGER
EFO-21 Growth Inhibition Assay IC50=165.45 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=164.321 μM SANGER
AU565 Growth Inhibition Assay IC50=163.64 μM SANGER
CHP-212 Growth Inhibition Assay IC50=163.626 μM SANGER
CAL-62 Growth Inhibition Assay IC50=162.613 μM SANGER
EFO-27 Growth Inhibition Assay IC50=160.584 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=159.583 μM SANGER
ES4 Growth Inhibition Assay IC50=159.396 μM SANGER
HCC70 Growth Inhibition Assay IC50=159.242 μM SANGER
HCC38 Growth Inhibition Assay IC50=157.369 μM SANGER
DG-75 Growth Inhibition Assay IC50=156.694 μM SANGER
HCC1419 Growth Inhibition Assay IC50=156.077 μM SANGER
CAL-120 Growth Inhibition Assay IC50=155.821 μM SANGER
DK-MG Growth Inhibition Assay IC50=155.183 μM SANGER
RERF-LC-MS Growth Inhibition Assay IC50=154.772 μM SANGER
Calu-1 Growth Inhibition Assay IC50=154.003 μM SANGER
TT Growth Inhibition Assay IC50=153.49 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=153.164 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=152.764 μM SANGER
GAK Growth Inhibition Assay IC50=151.374 μM SANGER
GDM-1 Growth Inhibition Assay IC50=151.135 μM SANGER
NCI-H748 Growth Inhibition Assay IC50=150.209 μM SANGER
L-540 Growth Inhibition Assay IC50=149.75 μM SANGER
Caov-3 Growth Inhibition Assay IC50=149.714 μM SANGER
TE-9 Growth Inhibition Assay IC50=149.443 μM SANGER
639-V Growth Inhibition Assay IC50=148.705 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=148.562 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=148.54 μM SANGER
GAMG Growth Inhibition Assay IC50=148.247 μM SANGER
GCIY Growth Inhibition Assay IC50=147.797 μM SANGER
DMS-114 Growth Inhibition Assay IC50=147.441 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=147.404 μM SANGER
SW13 Growth Inhibition Assay IC50=147.253 μM SANGER
LK-2 Growth Inhibition Assay IC50=147.143 μM SANGER
OMC-1 Growth Inhibition Assay IC50=145.967 μM SANGER
G-401 Growth Inhibition Assay IC50=145.835 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=145.075 μM SANGER
SCC-25 Growth Inhibition Assay IC50=144.005 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=143.687 μM SANGER
CCF-STTG1 Growth Inhibition Assay IC50=143.334 μM SANGER
YKG-1 Growth Inhibition Assay IC50=142.889 μM SANGER
OE33 Growth Inhibition Assay IC50=141.798 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=141.507 μM SANGER
Detroit562 Growth Inhibition Assay IC50=141.466 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=140.749 μM SANGER
BHT-101 Growth Inhibition Assay IC50=140.208 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=138.831 μM SANGER
OAW-42 Growth Inhibition Assay IC50=137.856 μM SANGER
G-402 Growth Inhibition Assay IC50=135.295 μM SANGER
NOS-1 Growth Inhibition Assay IC50=134.765 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=134.59 μM SANGER
JEG-3 Growth Inhibition Assay IC50=134.359 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=134.2 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=134.116 μM SANGER
Capan-2 Growth Inhibition Assay IC50=133.975 μM SANGER
CTB-1 Growth Inhibition Assay IC50=132.897 μM SANGER
HT-1080 Growth Inhibition Assay IC50=132.204 μM SANGER
MFH-ino Growth Inhibition Assay IC50=131.114 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=130.375 μM SANGER
LU-99A Growth Inhibition Assay IC50=129.931 μM SANGER
HEC-1 Growth Inhibition Assay IC50=129.198 μM SANGER
EB-3 Growth Inhibition Assay IC50=127.013 μM SANGER
UMC-11 Growth Inhibition Assay IC50=126.038 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=124.283 μM SANGER
SW1463 Growth Inhibition Assay IC50=124.077 μM SANGER
OPM-2 Growth Inhibition Assay IC50=123.176 μM SANGER
HT-29 Growth Inhibition Assay IC50=122.778 μM SANGER
HAL-01 Growth Inhibition Assay IC50=122.499 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=122.141 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=121.55 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=121.044 μM SANGER
OVCAR-3 Growth Inhibition Assay IC50=119.915 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=119.417 μM SANGER
SUP-T1 Growth Inhibition Assay IC50=118.956 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=118.116 μM SANGER
RKO Growth Inhibition Assay IC50=117.898 μM SANGER
ATN-1 Growth Inhibition Assay IC50=117.828 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=117.668 μM SANGER
HCC1599 Growth Inhibition Assay IC50=117.156 μM SANGER
Calu-6 Growth Inhibition Assay IC50=116.798 μM SANGER
DMS-273 Growth Inhibition Assay IC50=115.617 μM SANGER
786-0 Growth Inhibition Assay IC50=113.453 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=113.125 μM SANGER
NEC8 Growth Inhibition Assay IC50=112.624 μM SANGER
MDA-MB-157 Growth Inhibition Assay IC50=112.49 μM SANGER
U031 Growth Inhibition Assay IC50=112.065 μM SANGER
WSU-NHL Growth Inhibition Assay IC50=112.01 μM SANGER
HCT-15 Growth Inhibition Assay IC50=110.661 μM SANGER
A253 Growth Inhibition Assay IC50=110.479 μM SANGER
DU-145 Growth Inhibition Assay IC50=109.945 μM SANGER
D-263MG Growth Inhibition Assay IC50=108.961 μM SANGER
FTC-133 Growth Inhibition Assay IC50=108.488 μM SANGER
HOP-92 Growth Inhibition Assay IC50=108.475 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=108.357 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=106.85 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=106.678 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=105.023 μM SANGER
UM-UC-3 Growth Inhibition Assay IC50=103.842 μM SANGER
MKN45 Growth Inhibition Assay IC50=103.584 μM SANGER
KE-37 Growth Inhibition Assay IC50=102.95 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=101.762 μM SANGER
TE-11 Growth Inhibition Assay IC50=101.724 μM SANGER
Saos-2 Growth Inhibition Assay IC50=101.437 μM SANGER
LU-65 Growth Inhibition Assay IC50=101.081 μM SANGER
Mewo Growth Inhibition Assay IC50=99.5603 μM SANGER
IGR-1 Growth Inhibition Assay IC50=99.3119 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=99.3004 μM SANGER
PC-3 Growth Inhibition Assay IC50=99.0564 μM SANGER
U-698-M Growth Inhibition Assay IC50=98.9489 μM SANGER
MKN7 Growth Inhibition Assay IC50=97.7439 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=97.461 μM SANGER
Caov-4 Growth Inhibition Assay IC50=95.685 μM SANGER
A2058 Growth Inhibition Assay IC50=95.4617 μM SANGER
RMG-I Growth Inhibition Assay IC50=95.1072 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=94.954 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=94.5984 μM SANGER
J82 Growth Inhibition Assay IC50=93.7811 μM SANGER
23132-87 Growth Inhibition Assay IC50=93.168 μM SANGER
CAL-33 Growth Inhibition Assay IC50=93.0601 μM SANGER
BOKU Growth Inhibition Assay IC50=92.6957 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=91.2676 μM SANGER
C-33-A Growth Inhibition Assay IC50=90.54 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=89.8724 μM SANGER
TE-12 Growth Inhibition Assay IC50=89.3741 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=85.7426 μM SANGER
SBC-1 Growth Inhibition Assay IC50=84.0208 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=84.0172 μM SANGER
SW1573 Growth Inhibition Assay IC50=82.5893 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=81.8531 μM SANGER
NCI-H1417 Growth Inhibition Assay IC50=81.4368 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=81.344 μM SANGER
NB12 Growth Inhibition Assay IC50=80.9369 μM SANGER
KYSE-410 Growth Inhibition Assay IC50=80.2857 μM SANGER
HCE-T Growth Inhibition Assay IC50=80.1588 μM SANGER
SF295 Growth Inhibition Assay IC50=79.9553 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=78.5878 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=78.435 μM SANGER
NB6 Growth Inhibition Assay IC50=78.1299 μM SANGER
HSC-3 Growth Inhibition Assay IC50=77.0282 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=76.1096 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=75.8019 μM SANGER
LS-411N Growth Inhibition Assay IC50=74.2528 μM SANGER
RT4 Growth Inhibition Assay IC50=73.5742 μM SANGER
KALS-1 Growth Inhibition Assay IC50=73.5475 μM SANGER
EW-16 Growth Inhibition Assay IC50=71.7415 μM SANGER
HCC1806 Growth Inhibition Assay IC50=71.4587 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=70.3 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=69.3961 μM SANGER
C-4-II Growth Inhibition Assay IC50=69.3607 μM SANGER
NCI-H1703 Growth Inhibition Assay IC50=68.1171 μM SANGER
HuCCT1 Growth Inhibition Assay IC50=67.0374 μM SANGER
MFE-296 Growth Inhibition Assay IC50=64.4473 μM SANGER
AN3-CA Growth Inhibition Assay IC50=64.3035 μM SANGER
SCH Growth Inhibition Assay IC50=64.2351 μM SANGER
T-24 Growth Inhibition Assay IC50=62.7126 μM SANGER
K-562 Growth Inhibition Assay IC50=62.2452 μM SANGER
NCI-H1734 Growth Inhibition Assay IC50=61.9663 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=61.9242 μM SANGER
EKVX Growth Inhibition Assay IC50=61.4958 μM SANGER
SiHa Growth Inhibition Assay IC50=59.6487 μM SANGER
LU-134-A Growth Inhibition Assay IC50=59.6016 μM SANGER
ACN Growth Inhibition Assay IC50=59.1587 μM SANGER
HT-1376 Growth Inhibition Assay IC50=59.0921 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=59.0553 μM SANGER
BV-173 Growth Inhibition Assay IC50=57.5142 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=57.2412 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=56.6057 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=56.1693 μM SANGER
RCM-1 Growth Inhibition Assay IC50=56.0078 μM SANGER
DV-90 Growth Inhibition Assay IC50=55.8917 μM SANGER
ES6 Growth Inhibition Assay IC50=55.8899 μM SANGER
LXF-289 Growth Inhibition Assay IC50=55.5066 μM SANGER
A375 Growth Inhibition Assay IC50=54.8059 μM SANGER
MC-IXC Growth Inhibition Assay IC50=54.4364 μM SANGER
697 Growth Inhibition Assay IC50=54.1555 μM SANGER
KGN Growth Inhibition Assay IC50=53.959 μM SANGER
MG-63 Growth Inhibition Assay IC50=53.9381 μM SANGER
COLO-824 Growth Inhibition Assay IC50=53.6976 μM SANGER
CHP-126 Growth Inhibition Assay IC50=53.5169 μM SANGER
CESS Growth Inhibition Assay IC50=52.145 μM SANGER
DB Growth Inhibition Assay IC50=51.9855 μM SANGER
SW837 Growth Inhibition Assay IC50=51.9785 μM SANGER
SK-N-AS Growth Inhibition Assay IC50=51.8281 μM SANGER
MCF7 Growth Inhibition Assay IC50=51.7554 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=51.5849 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=51.231 μM SANGER
KS-1 Growth Inhibition Assay IC50=50.2225 μM SANGER
LC4-1 Growth Inhibition Assay IC50=49.8912 μM SANGER
SNU-C1 Growth Inhibition Assay IC50=49.3207 μM SANGER
COR-L105 Growth Inhibition Assay IC50=48.973 μM SANGER
SNB75 Growth Inhibition Assay IC50=48.4118 μM SANGER
HCC2998 Growth Inhibition Assay IC50=48.2982 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=47.7264 μM SANGER
D-542MG Growth Inhibition Assay IC50=47.4589 μM SANGER
UACC-62 Growth Inhibition Assay IC50=46.8608 μM SANGER
no-11 Growth Inhibition Assay IC50=46.2031 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=46.0755 μM SANGER
COLO-800 Growth Inhibition Assay IC50=45.5898 μM SANGER
H4 Growth Inhibition Assay IC50=45.3296 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=45.0437 μM SANGER
ESS-1 Growth Inhibition Assay IC50=44.2062 μM SANGER
SR Growth Inhibition Assay IC50=43.8673 μM SANGER
TE-8 Growth Inhibition Assay IC50=43.7895 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=43.697 μM SANGER
HCT-116 Growth Inhibition Assay IC50=43.2099 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=42.6938 μM SANGER
NY Growth Inhibition Assay IC50=42.1801 μM SANGER
MPP-89 Growth Inhibition Assay IC50=41.9211 μM SANGER
SK-CO-1 Growth Inhibition Assay IC50=41.7755 μM SANGER
BE-13 Growth Inhibition Assay IC50=41.4473 μM SANGER
HCC2218 Growth Inhibition Assay IC50=40.5849 μM SANGER
KM12 Growth Inhibition Assay IC50=38.5998 μM SANGER
CMK Growth Inhibition Assay IC50=38.4162 μM SANGER
HT-144 Growth Inhibition Assay IC50=38.2575 μM SANGER
no-10 Growth Inhibition Assay IC50=38.1294 μM SANGER
MKN1 Growth Inhibition Assay IC50=36.8444 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=36.3331 μM SANGER
8505C Growth Inhibition Assay IC50=35.9294 μM SANGER
EFE-184 Growth Inhibition Assay IC50=35.917 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=35.3416 μM SANGER
TK10 Growth Inhibition Assay IC50=35.1322 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=34.9241 μM SANGER
KU-19-19 Growth Inhibition Assay IC50=33.7534 μM SANGER
RVH-421 Growth Inhibition Assay IC50=33.168 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=32.8467 μM SANGER
HCC1143 Growth Inhibition Assay IC50=32.7979 μM SANGER
SW948 Growth Inhibition Assay IC50=32.7548 μM SANGER
KNS-42 Growth Inhibition Assay IC50=31.8662 μM SANGER
CAS-1 Growth Inhibition Assay IC50=31.7665 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=31.0047 μM SANGER
SK-MM-2 Growth Inhibition Assay IC50=30.9792 μM SANGER
NALM-6 Growth Inhibition Assay IC50=30.4965 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=30.2656 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=30.2059 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=29.7092 μM SANGER
A204 Growth Inhibition Assay IC50=29.6828 μM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=29.6719 μM SANGER
SW872 Growth Inhibition Assay IC50=28.5326 μM SANGER
C32 Growth Inhibition Assay IC50=28.0826 μM SANGER
OAW-28 Growth Inhibition Assay IC50=28.0052 μM SANGER
SU-DHL-1 Growth Inhibition Assay IC50=27.9474 μM SANGER
MC-CAR Growth Inhibition Assay IC50=27.7907 μM SANGER
ES8 Growth Inhibition Assay IC50=27.7814 μM SANGER
COLO-792 Growth Inhibition Assay IC50=27.7728 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=27.5282 μM SANGER
KLE Growth Inhibition Assay IC50=27.2565 μM SANGER
SNG-M Growth Inhibition Assay IC50=27.2271 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=26.8986 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=26.7377 μM SANGER
KASUMI-1 Growth Inhibition Assay IC50=24.9328 μM SANGER
LU-139 Growth Inhibition Assay IC50=24.835 μM SANGER
NCI-H1963 Growth Inhibition Assay IC50=24.2839 μM SANGER
HMV-II Growth Inhibition Assay IC50=24.2163 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=24.0898 μM SANGER
K5 Growth Inhibition Assay IC50=23.5486 μM SANGER
REH Growth Inhibition Assay IC50=23.1699 μM SANGER
M14 Growth Inhibition Assay IC50=23.1132 μM SANGER
GI-1 Growth Inhibition Assay IC50=22.7841 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=22.7069 μM SANGER
LS-513 Growth Inhibition Assay IC50=22.6192 μM SANGER
RXF393 Growth Inhibition Assay IC50=22.6068 μM SANGER
SW684 Growth Inhibition Assay IC50=22.2858 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=22.1954 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=21.8957 μM SANGER
EoL-1- Growth Inhibition Assay IC50=21.8385 μM SANGER
BPH-1 Growth Inhibition Assay IC50=21.7035 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=21.6863 μM SANGER
KYSE-450 Growth Inhibition Assay IC50=21.5354 μM SANGER
HCC1187 Growth Inhibition Assay IC50=20.3589 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=20.2169 μM SANGER
Becker Growth Inhibition Assay IC50=20.1777 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=19.5342 μM SANGER
A101D Growth Inhibition Assay IC50=19.243 μM SANGER
SNU-449 Growth Inhibition Assay IC50=18.715 μM SANGER
EM-2 Growth Inhibition Assay IC50=18.6248 μM SANGER
8305C Growth Inhibition Assay IC50=18.5305 μM SANGER
SIMA Growth Inhibition Assay IC50=17.9118 μM SANGER
Daudi Growth Inhibition Assay IC50=17.6149 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=16.6702 μM SANGER
NH-12 Growth Inhibition Assay IC50=16.0097 μM SANGER
LoVo Growth Inhibition Assay IC50=15.2659 μM SANGER
ST486 Growth Inhibition Assay IC50=14.2251 μM SANGER
NB1 Growth Inhibition Assay IC50=14.1935 μM SANGER
SF539 Growth Inhibition Assay IC50=14.0116 μM SANGER
SW48 Growth Inhibition Assay IC50=13.7265 μM SANGER
MEL-HO Growth Inhibition Assay IC50=13.8829 μM SANGER
KU812 Growth Inhibition Assay IC50=13.5175 μM SANGER
T98G Growth Inhibition Assay IC50=13.4717 μM SANGER
DSH1 Growth Inhibition Assay IC50=13.3879 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=13.2909 μM SANGER
C8166 Growth Inhibition Assay IC50=13.2318 μM SANGER
PC-14 Growth Inhibition Assay IC50=12.324 μM SANGER
PA-1 Growth Inhibition Assay IC50=11.93 μM SANGER
HEL Growth Inhibition Assay IC50=11.6579 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=11.1365 μM SANGER
SNU-387 Growth Inhibition Assay IC50=10.7235 μM SANGER
HT-3 Growth Inhibition Assay IC50=10.6179 μM SANGER
M059J Growth Inhibition Assay IC50=10.6102 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=10.4677 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=10.4413 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=9.99798 μM SANGER
U-118-MG Growth Inhibition Assay IC50=9.94444 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=9.7777 μM SANGER
EFM-19 Growth Inhibition Assay IC50=9.75566 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=9.65742 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=9.52397 μM SANGER
U-2-OS Growth Inhibition Assay IC50=9.45006 μM SANGER
CTV-1 Growth Inhibition Assay IC50=9.43894 μM SANGER
COLO-205 Growth Inhibition Assay IC50=9.43821 μM SANGER
NCI-H64 Growth Inhibition Assay IC50=9.42255 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=9.39986 μM SANGER
ACHN Growth Inhibition Assay IC50=9.30546 μM SANGER
MEG-01 Growth Inhibition Assay IC50=8.99043 μM SANGER
MKN28 Growth Inhibition Assay IC50=8.88516 μM SANGER
CAL-72 Growth Inhibition Assay IC50=8.76113 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=8.54304 μM SANGER
SW1417 Growth Inhibition Assay IC50=7.64584 μM SANGER
G-361 Growth Inhibition Assay IC50=7.46561 μM SANGER
MC116 Growth Inhibition Assay IC50=7.28691 μM SANGER
RT-112 Growth Inhibition Assay IC50=7.16456 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=6.60936 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=6.53195 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=6.417 μM SANGER
WM-115 Growth Inhibition Assay IC50=5.81509 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=6.38344 μM SANGER
BL-41 Growth Inhibition Assay IC50=5.81266 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=5.72627 μM SANGER
D-392MG Growth Inhibition Assay IC50=5.49145 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=5.45628 μM SANGER
SW1710 Growth Inhibition Assay IC50=5.42456 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=4.9934 μM SANGER
ALL-PO Growth Inhibition Assay IC50=4.83858 μM SANGER
BxPC-3 Growth Inhibition Assay IC50=4.70391 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=4.29479 μM SANGER
NKM-1 Growth Inhibition Assay IC50=4.13971 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=4.04545 μM SANGER
OE19 Growth Inhibition Assay IC50=3.96451 μM SANGER
TE-15 Growth Inhibition Assay IC50=3.95343 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=3.88556 μM SANGER
A172 Growth Inhibition Assay IC50=3.75498 μM SANGER
HCC1569 Growth Inhibition Assay IC50=3.48305 μM SANGER
HOP-62 Growth Inhibition Assay IC50=3.36054 μM SANGER
A704 Growth Inhibition Assay IC50=3.0812 μM SANGER
SCC-9 Growth Inhibition Assay IC50=2.95485 μM SANGER
COLO-829 Growth Inhibition Assay IC50=2.7654 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=2.70193 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=2.64128 μM SANGER
SNU-423 Growth Inhibition Assay IC50=2.49787 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=2.27684 μM SANGER
RS4-11 Growth Inhibition Assay IC50=1.95415 μM SANGER
HCC1395 Growth Inhibition Assay IC50=1.78273 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=1.75977 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=1.72788 μM SANGER
BCPAP Growth Inhibition Assay IC50=1.66898 μM SANGER
A498 Growth Inhibition Assay IC50=1.30469 μM SANGER
TYK-nu Growth Inhibition Assay IC50=1.07912 μM SANGER
D-247MG Growth Inhibition Assay IC50=0.94852 μM SANGER
S-117 Growth Inhibition Assay IC50=0.92131 μM SANGER
D-336MG Growth Inhibition Assay IC50=0.8462 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=0.58832 μM SANGER
769-P Growth Inhibition Assay IC50=0.58499 μM SANGER
GCT Growth Inhibition Assay IC50=0.30672 μM SANGER
SW982 Growth Inhibition Assay IC50=0.21416 μM SANGER
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明 ラドゥビグルシブ (Laduviglusib (CHIR-99021、CT99021)) は GSK-3α および GSK-3β 阻害剤であり、IC50 はそれぞれ 10 nM および 6.7 nM です。 ラドゥビグルシブは、サイクリン依存性キナーゼ (CDK) に対して交差反応性を示さず、CDK と比較して GSK-3β に対して 350 倍の選択性を示します。 Laduviglusib は Wnt/β-catenin 活性化因子として機能し、オートファジー (autophagy) を誘導します。
Targets
GSK-3β [1]
(Cell-free assay)
GSK-3α [1]
(Cell-free assay)
6.7 nM 10 nM
In Vitro
In vitro CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. Furthermore, CHIR-99021 shows only weak binding to a panel of 22 pharmacologically relevant receptors and little inhibitory activity against a panel of 23 nonkinase enzymes. CHIR-99021 induces the activation of glycogen synthase (GS) in insulin receptor-expressing CHO-IR cells with EC50 of 0.763 μM[1].
細胞実験 細胞株 Insulin receptor–expressing CHO-IR cells; Primary rat hepatocytes
濃度 0.01-10 μM
反応時間 30 min
実験の流れ

CHO-IR cells expressing human insulin receptor are grown to 80% confluence in Hamm’s F12 medium with 10% fetal bovine serum and without hypoxanthine. Trypsinized cells are seeded in 6-well plates at 1 × 106 cells/well in 2 ml of medium without fetal bovine serum. After 24 h, medium is replaced with 1 ml of serum-free medium containing GSK-3 inhibitor or control (final DMSO concentration <0.1%) for 30 min at 37°C. Cells are lysed and centrifuged 15 min at 4°C/14000g. The activity ratio of GS is calculated as the GS activity in the absence of glucose-6-phosphate divided by the activity in the presence of 5 mmol/l glucose-6-phosphate, using the filter paper assay of Thomas et al.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot Cleaved PARP / CD31 / VE-Cadherin / α-SMA / vimentin β-catenin CTNNB1 30709379
Growth inhibition assay Cell viability 22039301
Immunofluorescence Oct3/4 SOX10/EdU 24779365
In Vivo
In Vivo Oral administration of CHIR-99021 at 30 mg/kg enhances glucose metabolism in a rodent model of type 2 diabetes, with a maximal plasma glucose reduction of nearly 150 mg/dl 3-4 hours after administration, while plasma insulin remains at or below control levels. Oral administration of CHIR-99021 at 16 or 48 mg/kg 1 hour before oral glucose challenges in ZDF rats significantly improves glucose tolerance with 14% and 33% reduction in plasma glucose at 16 mg/kg and 48 mg/kg, respectively, and the higher dose of CHIR-99021 also reduces hyperglycemia before the oral glucose challenge[1].
動物実験 動物モデル Female db/db mice; Male ZDF rats
投与量 8-48 mg/kg
投与経路 oral administration

化学情報

分子量 465.34 化学式

C22H18Cl2N8

CAS No. 252917-06-9 SDF Download Laduviglusib (CHIR-99021) SDFをダウンロードする
Smiles CC1=CN=C(N1)C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)Cl)NCCNC4=NC=C(C=C4)C#N
保管

In vitro
Batch:

DMSO : 39 mg/mL ( (83.8 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

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