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TAE684 (NVP-TAE684)

TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM of 3 nM, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis.

TAE684 (NVP-TAE684)化学構造

CAS No. 761439-42-3

サイズ 価格(税別) 在庫状況
JPY 24000 国内在庫あり
JPY 115500 国内在庫あり

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TAE684 (NVP-TAE684)関連製品

シグナル伝達経路

ALK Signaling Pathways

ALKシグナル伝達経路

ALK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
SCC-3 Growth Inhibition Assay IC50=0.0000603 μM
SF539 Growth Inhibition Assay IC50=0.000564 μM
DEL Growth Inhibition Assay IC50=0.000927 μM
NB1 Growth Inhibition Assay IC50=0.00162 μM
SR Growth Inhibition Assay IC50=0.00277 μM
KARPAS-299 Growth Inhibition Assay IC50=0.02384 μM
MHH-CALL-2 Growth Inhibition Assay IC50=0.02952 μM
SU-DHL-1 Growth Inhibition Assay IC50=0.04865 μM
A4-Fuk Growth Inhibition Assay IC50=0.05565 μM
EW-1 Growth Inhibition Assay IC50=0.10256 μM
NOS-1 Growth Inhibition Assay IC50=0.10294 μM
EW-16 Growth Inhibition Assay IC50=0.10568 μM
TE-11 Growth Inhibition Assay IC50=0.16096 μM
SW982 Growth Inhibition Assay IC50=0.16478 μM
LAN-6 Growth Inhibition Assay IC50=0.17443 μM
MZ1-PC Growth Inhibition Assay IC50=0.17835 μM
KS-1 Growth Inhibition Assay IC50=0.19343 μM
PSN1 Growth Inhibition Assay IC50=0.19631 μM
LC-2-ad Growth Inhibition Assay IC50=0.19692 μM
COLO-320-HSR Growth Inhibition Assay IC50=0.19776 μM
OPM-2 Growth Inhibition Assay IC50=0.22669 μM
SK-NEP-1 Growth Inhibition Assay IC50=0.23524 μM
ALL-PO Growth Inhibition Assay IC50=0.24524 μM
CMK Growth Inhibition Assay IC50=0.2553 μM
NCI-H1648 Growth Inhibition Assay IC50=0.27855 μM
SIG-M5 Growth Inhibition Assay IC50=0.29159 μM
TGBC24TKB Growth Inhibition Assay IC50=0.30218 μM
DOHH-2 Growth Inhibition Assay IC50=0.31204 μM
NB69 Growth Inhibition Assay IC50=0.31787 μM
MFH-ino Growth Inhibition Assay IC50=0.32523 μM
KP-N-RT-BM-1 Growth Inhibition Assay IC50=0.33123 μM
MONO-MAC-6 Growth Inhibition Assay IC50=0.33291 μM
ATN-1 Growth Inhibition Assay IC50=0.33303 μM
NTERA-S-cl-D1 Growth Inhibition Assay IC50=0.33396 μM
L-540 Growth Inhibition Assay IC50=0.36988 μM
GB-1 Growth Inhibition Assay IC50=0.38867 μM
MV-4-11 Growth Inhibition Assay IC50=0.39446 μM
KG-1 Growth Inhibition Assay IC50=0.39561 μM
OVCAR-4 Growth Inhibition Assay IC50=0.40569 μM
NEC8 Growth Inhibition Assay IC50=0.41292 μM
SK-MM-2 Growth Inhibition Assay IC50=0.41609 μM
TE-8 Growth Inhibition Assay IC50=0.4288 μM
697 Growth Inhibition Assay IC50=0.43215 μM
NB14 Growth Inhibition Assay IC50=0.43826 μM
GDM-1 Growth Inhibition Assay IC50=0.47116 μM
HUTU-80 Growth Inhibition Assay IC50=0.47375 μM
HL-60 Growth Inhibition Assay IC50=0.48142 μM
OCI-AML2 Growth Inhibition Assay IC50=0.48328 μM
ML-2 Growth Inhibition Assay IC50=0.49031 μM
ES4 Growth Inhibition Assay IC50=0.49109 μM
NCI-H747 Growth Inhibition Assay IC50=0.4989 μM
RL95-2 Growth Inhibition Assay IC50=0.50112 μM
TE-15 Growth Inhibition Assay IC50=0.51124 μM
TE-12 Growth Inhibition Assay IC50=0.53349 μM
LB1047-RCC Growth Inhibition Assay IC50=0.54549 μM
LB831-BLC Growth Inhibition Assay IC50=0.55023 μM
NCI-H1355 Growth Inhibition Assay IC50=0.55184 μM
CTV-1 Growth Inhibition Assay IC50=0.55624 μM
RXF393 Growth Inhibition Assay IC50=0.55794 μM
SW872 Growth Inhibition Assay IC50=0.56724 μM
MPP-89 Growth Inhibition Assay IC50=0.57884 μM
RPMI-8226 Growth Inhibition Assay IC50=0.63526 μM
LS-1034 Growth Inhibition Assay IC50=0.6358 μM
SJSA-1 Growth Inhibition Assay IC50=0.63725 μM
HOP-62 Growth Inhibition Assay IC50=0.65033 μM
KGN Growth Inhibition Assay IC50=0.66168 μM
D-336MG Growth Inhibition Assay IC50=0.66169 μM
LS-411N Growth Inhibition Assay IC50=0.67462 μM
TE-1 Growth Inhibition Assay IC50=0.69074 μM
LB996-RCC Growth Inhibition Assay IC50=0.69389 μM
TE-10 Growth Inhibition Assay IC50=0.71496 μM
NCI-SNU-16 Growth Inhibition Assay IC50=0.72664 μM
ES8 Growth Inhibition Assay IC50=0.74975 μM
COLO-800 Growth Inhibition Assay IC50=0.76695 μM
ES6 Growth Inhibition Assay IC50=0.77559 μM
L-363 Growth Inhibition Assay IC50=0.82375 μM
NMC-G1 Growth Inhibition Assay IC50=0.83233 μM
LU-134-A Growth Inhibition Assay IC50=0.83912 μM
SF268 Growth Inhibition Assay IC50=0.84042 μM
KARPAS-45 Growth Inhibition Assay IC50=0.84263 μM
TGW Growth Inhibition Assay IC50=0.85863 μM
CHP-126 Growth Inhibition Assay IC50=0.85957 μM
MOLT-16 Growth Inhibition Assay IC50=0.87589 μM
LB771-HNC Growth Inhibition Assay IC50=0.89757 μM
NALM-6 Growth Inhibition Assay IC50=0.90739 μM
GCIY Growth Inhibition Assay IC50=0.95526 μM
IST-MES1 Growth Inhibition Assay IC50=0.98824 μM
LB2241-RCC Growth Inhibition Assay IC50=0.9884 μM
BL-70 Growth Inhibition Assay IC50=0.99535 μM
NB17 Growth Inhibition Assay IC50=1.00639 μM
LXF-289 Growth Inhibition Assay IC50=1.03076 μM
TK10 Growth Inhibition Assay IC50=1.05063 μM
K5 Growth Inhibition Assay IC50=1.06274 μM
NCI-H716 Growth Inhibition Assay IC50=1.07259 μM
HCE-T Growth Inhibition Assay IC50=1.08819 μM
GI-1 Growth Inhibition Assay IC50=1.09798 μM
KARPAS-422 Growth Inhibition Assay IC50=1.10022 μM
TE-9 Growth Inhibition Assay IC50=1.11328 μM
SF126 Growth Inhibition Assay IC50=1.11568 μM
BB30-HNC Growth Inhibition Assay IC50=1.13112 μM
NCI-H1304 Growth Inhibition Assay IC50=1.13338 μM
HEL Growth Inhibition Assay IC50=1.14895 μM
HAL-01 Growth Inhibition Assay IC50=1.15283 μM
SK-LMS-1 Growth Inhibition Assay IC50=1.15974 μM
SW954 Growth Inhibition Assay IC50=1.19567 μM
D-283MED Growth Inhibition Assay IC50=1.22379 μM
NCI-H1882 Growth Inhibition Assay IC50=1.2389 μM
GI-ME-N Growth Inhibition Assay IC50=1.25208 μM
SK-PN-DW Growth Inhibition Assay IC50=1.26348 μM
C2BBe1 Growth Inhibition Assay IC50=1.29117 μM
A704 Growth Inhibition Assay IC50=1.32689 μM
KALS-1 Growth Inhibition Assay IC50=1.3408 μM
ETK-1 Growth Inhibition Assay IC50=1.34489 μM
LB647-SCLC Growth Inhibition Assay IC50=1.34986 μM
OCUB-M Growth Inhibition Assay IC50=1.36143 μM
NCI-H720 Growth Inhibition Assay IC50=1.36378 μM
NB13 Growth Inhibition Assay IC50=1.37293 μM
GR-ST Growth Inhibition Assay IC50=1.38757 μM
DU-4475 Growth Inhibition Assay IC50=1.45853 μM
HCC2157 Growth Inhibition Assay IC50=1.46659 μM
RKO Growth Inhibition Assay IC50=1.49922 μM
LS-123 Growth Inhibition Assay IC50=1.51594 μM
NCI-H69 Growth Inhibition Assay IC50=1.55811 μM
SW962 Growth Inhibition Assay IC50=1.5613 μM
PF-382 Growth Inhibition Assay IC50=1.5696 μM
A101D Growth Inhibition Assay IC50=1.57113 μM
NB10 Growth Inhibition Assay IC50=1.57392 μM
NB5 Growth Inhibition Assay IC50=1.58476 μM
HCE-4 Growth Inhibition Assay IC50=1.6085 μM
HT-144 Growth Inhibition Assay IC50=1.6319 μM
NCI-H524 Growth Inhibition Assay IC50=1.64307 μM
NKM-1 Growth Inhibition Assay IC50=1.6866 μM
KURAMOCHI Growth Inhibition Assay IC50=1.69573 μM
NCI-H187 Growth Inhibition Assay IC50=1.70036 μM
U-266 Growth Inhibition Assay IC50=1.73842 μM
BL-41 Growth Inhibition Assay IC50=1.76272 μM
SK-N-DZ Growth Inhibition Assay IC50=1.78309 μM
Daudi Growth Inhibition Assay IC50=1.78967 μM
CPC-N Growth Inhibition Assay IC50=1.85096 μM
EM-2 Growth Inhibition Assay IC50=1.851 μM
HCC1187 Growth Inhibition Assay IC50=1.86241 μM
LP-1 Growth Inhibition Assay IC50=1.87143 μM
CAS-1 Growth Inhibition Assay IC50=1.98299 μM
NB7 Growth Inhibition Assay IC50=2.00555 μM
VA-ES-BJ Growth Inhibition Assay IC50=2.01513 μM
SNU-C2B Growth Inhibition Assay IC50=2.03351 μM
LOXIMVI Growth Inhibition Assay IC50=2.06786 μM
NCI-H1581 Growth Inhibition Assay IC50=2.11559 μM
IST-SL2 Growth Inhibition Assay IC50=2.12445 μM
NOMO-1 Growth Inhibition Assay IC50=2.17683 μM
TE-6 Growth Inhibition Assay IC50=2.1905 μM
NCI-H526 Growth Inhibition Assay IC50=2.19141 μM
MSTO-211H Growth Inhibition Assay IC50=2.20041 μM
LS-513 Growth Inhibition Assay IC50=2.22269 μM
NCI-SNU-1 Growth Inhibition Assay IC50=2.33256 μM
BB65-RCC Growth Inhibition Assay IC50=2.37493 μM
GT3TKB Growth Inhibition Assay IC50=2.39972 μM
OS-RC-2 Growth Inhibition Assay IC50=2.42341 μM
NCI-H2126 Growth Inhibition Assay IC50=2.43674 μM
SK-UT-1 Growth Inhibition Assay IC50=2.47467 μM
DMS-114 Growth Inhibition Assay IC50=2.61524 μM
ONS-76 Growth Inhibition Assay IC50=2.63641 μM
8-MG-BA Growth Inhibition Assay IC50=2.65414 μM
BOKU Growth Inhibition Assay IC50=2.72764 μM
LAMA-84 Growth Inhibition Assay IC50=2.79912 μM
ES1 Growth Inhibition Assay IC50=2.81804 μM
NCI-H1395 Growth Inhibition Assay IC50=2.82012 μM
A388 Growth Inhibition Assay IC50=2.9617 μM
NCCIT Growth Inhibition Assay IC50=3.08862 μM
HD-MY-Z Growth Inhibition Assay IC50=3.13203 μM
NCI-H510A Growth Inhibition Assay IC50=3.18943 μM
NCI-N87 Growth Inhibition Assay IC50=3.2002 μM
SCLC-21H Growth Inhibition Assay IC50=3.26859 μM
SH-4 Growth Inhibition Assay IC50=3.28797 μM
QIMR-WIL Growth Inhibition Assay IC50=3.32849 μM
KM12 Growth Inhibition Assay IC50=3.33544 μM
ST486 Growth Inhibition Assay IC50=3.53883 μM
HC-1 Growth Inhibition Assay IC50=3.62028 μM
BV-173 Growth Inhibition Assay IC50=3.64088 μM
EW-24 Growth Inhibition Assay IC50=3.66434 μM
LU-65 Growth Inhibition Assay IC50=3.6871 μM
ECC4 Growth Inhibition Assay IC50=3.7756 μM
ARH-77 Growth Inhibition Assay IC50=4.11067 μM
BC-3 Growth Inhibition Assay IC50=4.13068 μM
SNB75 Growth Inhibition Assay IC50=4.2619 μM
MEG-01 Growth Inhibition Assay IC50=4.27419 μM
NCI-H1417 Growth Inhibition Assay IC50=4.28443 μM
MDA-MB-134-VI Growth Inhibition Assay IC50=4.30601 μM
Becker Growth Inhibition Assay IC50=4.47336 μM
DMS-153 Growth Inhibition Assay IC50=4.66475 μM
TGBC1TKB Growth Inhibition Assay IC50=4.68515 μM
EW-3 Growth Inhibition Assay IC50=4.76248 μM
KE-37 Growth Inhibition Assay IC50=4.86196 μM
NCI-H23 Growth Inhibition Assay IC50=4.87227 μM
MC116 Growth Inhibition Assay IC50=4.94126 μM
NH-12 Growth Inhibition Assay IC50=4.96439 μM
CTB-1 Growth Inhibition Assay IC50=4.97721 μM
KM-H2 Growth Inhibition Assay IC50=5.05323 μM
MOLT-4 Growth Inhibition Assay IC50=5.1183 μM
NCI-H2141 Growth Inhibition Assay IC50=5.14268 μM
EB-3 Growth Inhibition Assay IC50=5.17504 μM
NCI-H1522 Growth Inhibition Assay IC50=5.26322 μM
MRK-nu-1 Growth Inhibition Assay IC50=5.43633 μM
no-11 Growth Inhibition Assay IC50=5.47087 μM
CESS Growth Inhibition Assay IC50=5.58034 μM
KMOE-2 Growth Inhibition Assay IC50=5.58659 μM
REH Growth Inhibition Assay IC50=6.25618 μM
KU812 Growth Inhibition Assay IC50=6.42791 μM
SK-N-FI Growth Inhibition Assay IC50=6.60674 μM
MMAC-SF Growth Inhibition Assay IC50=7.06492 μM
RCC10RGB Growth Inhibition Assay IC50=7.22977 μM
NCI-H322M Growth Inhibition Assay IC50=7.33335 μM
NB6 Growth Inhibition Assay IC50=7.54899 μM
MN-60 Growth Inhibition Assay IC50=7.69215 μM
NCI-H1092 Growth Inhibition Assay IC50=8.01734 μM
EKVX Growth Inhibition Assay IC50=8.47066 μM
D-263MG Growth Inhibition Assay IC50=8.55396 μM
NCI-H209 Growth Inhibition Assay IC50=8.64006 μM
IST-SL1 Growth Inhibition Assay IC50=8.89892 μM
ACN Growth Inhibition Assay IC50=9.19157 μM
MHH-PREB-1 Growth Inhibition Assay IC50=9.21219 μM
EW-11 Growth Inhibition Assay IC50=9.65396 μM
KASUMI-1 Growth Inhibition Assay IC50=9.7877 μM
KINGS-1 Growth Inhibition Assay IC50=10.2347 μM
EVSA-T Growth Inhibition Assay IC50=10.3192 μM
DSH1 Growth Inhibition Assay IC50=10.3972 μM
COLO-824 Growth Inhibition Assay IC50=10.8669 μM
K052 Growth Inhibition Assay IC50=10.9322 μM
SK-MEL-2 Growth Inhibition Assay IC50=10.9939 μM
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生物活性

製品説明 TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM of 3 nM, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis.
Targets
ALK
(Cell lines)
2-10 nM
In Vitro
In vitro

TAE684 (NVP-TAE684) does not exhibit significant cross-reactivity against other kinases. This compound potently inhibits the proliferation of Ba/F3 NPM-ALK cells with IC50 of 3 nM, without affecting the survival of Ba/F3 cells even at 1 μM. It also inhibits proliferation of NPM-ALK-expressing human ALCL cell lines including Karpas-299 and SU-DHL-1 with IC50 of 2–5 nM. Molecular modeling reveals that L258 may be one of the major kinase-selectivity determinants for this chemical. Its treatment results in a rapid and sustained inhibition of phosphorylation of NPM-ALK. The compound induces apoptosis and G1 phase arrest in NPM-ALK-expressing Ba/F3 cells and ALCL patient cell lines. It markedly overcomes resistance in H3122 CR cells, harboring the fusion oncogene EML4-ALK, decreasing cell growth, suppressing ALK phosphorylation and inducing apoptosis. Neurite outgrowth induced by expression of the mALK R1279Q mutant could be completely inhibited by this compound at 30 nM.

Kinase Assay In vitro Enzyme Assays.
All in vitro enzyme assays are done at Upstate Biotechnology with the exception of InsR and IGF-1R. To determine the IC50 of TAE684 (NVP-TAE684) against InsR and IGF-1R a homogeneous time-resolved fluorescence assay is performed. ATP (10 mM) and 20 mg/ml biotinylated PolyEY (Glu, Tyr 4:1) are combined with 50 nL of serial dilutions of this compound (10-500 nM) and 4 ng of InsR enzyme in the presence of the kinase reaction buffer (20 mM Tris–Cl, pH 7.5/10 mM MgCl2/3 mM MnCl2/1 mM DTT/10 mM NaVO4/0.1 mg/ml of BSA). Assays are incubated for 1 hour at ambient temperature. Reactions are terminated by adding 10 mL of the detection solution containing 50 mM EDTA, 500 mM KF, 0.5 mg/ml of BSA, 5 mg/mL Eu3+ cryptate-labeled anti-phosphotyrosine antibody Mab PT66-K, and 5 mg/mL Streptavidin-XLent. The reaction is incubated for half an hour, and fluorescence signals are read on Analyst GT.
細胞実験 細胞株 Luciferase-expressing Karpas-299, SU-DHL-1, and Ba/F3 cells and transformed Ba/F3 stably expressing NPM-ALK, Bcr-Abl, or TEL-kinase fusion constructs.
濃度 1 nM-10 μM
反応時間 2–3 days
実験の流れ

Cells are seeded in 384-well plates (2.5×104 cells per well) and incubated with serial dilutions of TAE684 (NVP-TAE684) or DMSO for 2–3 days. Luciferase expression is used as a measure of cell proliferation/survival and is evaluated with the Bright-Glo Luciferase Assay System. IC50 values are generated by using XLFit software.
実験結果図 Methods Biomarkers 結果図 PMID
Growth inhibition assay Cell viability S1108-viability1.gif 18594010
Western blot p-ROS1 / ROS1 p-ALK / ALK / p-STAT3 / STAT3 / p-ERK / ERK / p-AKT / AKT / Survivin / BIM / PARP S1108-WB1.gif 25351743
In Vivo
In Vivo

After 4 weeks of treatment with TAE684 (NVP-TAE684) at 3 and 10 mg/kg, there is a significant delay in lymphoma development and 100- to 1,000-fold reduction in luminescence signal, without any signs of compound- or disease-related toxicity in Karpas-299 lymphoma model. This compound treatment also induces disease regression in established Karpas-299 lymphomas and down-regulates CD30 expression. It also shows impressive antitumor activity against H3122 CR xenograft tumors. Furthermore, treatment with this chemical improves the rough eye phenotype of both ALK mutants, especially that seen with ALKR1275Q.

動物実験 動物モデル Karpas-299 xenografts are established in 4- to 6-week old female Fox Chase SCIDBeige mice.
投与量 1, 3, and 10 mg/kg
投与経路 Once daily by oral gavage for 3 weeks
  • https://pubmed.ncbi.nlm.nih.gov/17185414/
  • https://pubmed.ncbi.nlm.nih.gov/21502504/
  • https://pubmed.ncbi.nlm.nih.gov/21838707/

化学情報

分子量 614.2 化学式

C30H40ClN7O3S
CAS No. 761439-42-3 SDF Download TAE684 (NVP-TAE684) SDFをダウンロードする
Smiles CC(C)S(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCC(CC4)N5CCN(CC5)C)OC
保管

In vitro
Batch:

DMSO : 10 mg/mL ( (16.28 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 匹

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。

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