JH-VIII-157-02|

Cas No.:	1639422-97-1
Chemical Name:	2-(4-(3-cyano-9-ethyl-6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazol-8-yl)-1H-pyrazol-1-yl)-N,N-dimethylacetamide
SMILES:	C(N(C)C)(=O)CN1C=C(C2C=C3C(=CC=2CC)C(=O)C2C4=C(NC=2C3(C)C)C=C(C#N)C=C4)C=N1
Formula:	C₂₈H₂₇N₅O₂
M.Wt:	465.557
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

JH-VIII-157-02 is a potent, orally active, CNS-permeable, second-generation inhibitor of ALK G1202R mutant with IC50 of 2 nM, also shows high potency against a variety of other frequently observed mutants (G1269A, S1206Y, F1174L and C1156Y); inhibits EML4-ALKWT with IC50 of 2 nM, demonstrates inhibition of CSNK2A1 <10 uM, IRAK1 (IC50 =14 nM), IRAK4 with (IC50=465 nM), CLK4 (IC50=14 nM), RET (IC50=3 nM), RET V804L (IC50=13 nM); potently inhibits proliferation of NSCLC H3122 cell line with IC50 of 5 nM.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47761	ALK-IN-12	ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities.
DC47760	ALK-IN-13	ALK-IN-13 is an ALK inhibitor, extracted from patent US20130225528A1, example 19.
DC44522	EML4-ALK kinase inhibitor 1	EML4-ALK kinase inhibitor 1 is a potent orally active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.
DC42445	CJ-2360	CJ-2360 is a potent and orally active ALK with IC50s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potenty activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated.
DC28690	ALK/ROS1-IN-1	ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
DC28469	TGFβRI-IN-2	TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.
DC10916	WY-135	WY-135 (WY135) is a novel potent inhibitor of ALK and ROS1 with IC50 of 1.2 and 0.48 nM, respectively.
DC10998	JH-VIII-157-02	JH-VIII-157-02 is a potent, orally active, CNS-permeable, second-generation inhibitor of ALK G1202R mutant with IC50 of 2 nM, also shows high potency against a variety of other frequently observed mutants (G1269A, S1206Y, F1174L and C1156Y).