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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

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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 [1]
(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. [1] It markedly overcomes resistance in H3122 CR cells, harboring the fusion oncogene EML4-ALK, decreasing cell growth, suppressing ALK phosphorylation and inducing apoptosis.[2] Neurite outgrowth induced by expression of the mALK R1279Q mutant could be completely inhibited by this compound at 30 nM. [3]
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. [1] It also shows impressive antitumor activity against H3122 CR xenograft tumors. [2] Furthermore, treatment with this chemical improves the rough eye phenotype of both ALK mutants, especially that seen with ALKR1275Q. [3]
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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