WY-135|WY135

Cas No.:	2163060-83-9
Chemical Name:	5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-4-(4-((4-methylpiperazin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)pyrimidine-2,4-diamine
Synonyms:	WY135
SMILES:	C(NC1=CC=C(N2C=C(CN3CCN(C)CC3)N=N2)C=C1OC)1=NC=C(Cl)C(NC2=CC=CC=C2S(C(C)C)(=O)=O)=N1
Formula:	C₂₈H₃₄ClN₉O₃S
M.Wt:	612.15
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

WY-135 (WY135) is a novel potent inhibitor of ALK and ROS1 with IC50 of 1.2 and 0.48 nM, respectively; exhibits better enzyme inhibitory activity than ceritinib, demonstrates anti-proliferative effects on Karpas299 and H2228 cells with IC50 of 28 and 164 nM respectively in MTT assay; induces cell cycle arrest at G1 phase in a dose-dependent manner and subsequently progressed into apoptosis, significantly suppressed ALK and its downstream protein expression.

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).