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JH-VIII-157-02

Catalog No. T15612   CAS 1639422-97-1

JH-VIII-157-02 is an inhibitor of ALK and inhibits echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) with IC50s of 2 nM for EML4-ALK G1202R, EML4-ALKwt, EML4-ALK C1156Y, EML4-ALK F1174L, and EML4-ALK F1174L.

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JH-VIII-157-02 Chemical Structure
JH-VIII-157-02, CAS 1639422-97-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 197.00
5 mg In stock $ 422.00
10 mg In stock $ 628.00
25 mg In stock $ 981.00
50 mg In stock $ 1,350.00
100 mg In stock $ 1,820.00
1 mL * 10 mM (in DMSO) In stock $ 432.00
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Purity: 98.02%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description JH-VIII-157-02 is an inhibitor of ALK and inhibits echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) with IC50s of 2 nM for EML4-ALK G1202R, EML4-ALKwt, EML4-ALK C1156Y, EML4-ALK F1174L, and EML4-ALK F1174L.
Targets&IC50 EML4-ALK (F1174L):2 nM, EML4-ALK (C1156Y):2 nM, EML4-ALK (G1202R):2 nM, EML4-ALK (WT):2 nM
In vitro JH-VIII-157-02 potently inhibits EML4-ALKS1206Y, EML4-ALKG1269A, EML4-ALKL1196M, EML4-ALK1151Tins, and EML4-ALKL1152R with IC50s of 2, 3, 58, 107 and 196 nM, respectively. JH-VIII-157-02 has selectivity at other kinases, including IRAK1, CLK4, RET, RET V804L, RET V804M and IRAK 4 with IC50s of 14 nM, 14 nM, 3 nM, 13 nM, 12 nM, and 465 nM, respectively[1].
In vivo In mice, JH-VIII-157-02 (10 mg/kg) exhibits good oral bioavailability and penetrates the central nervous system[1].
Molecular Weight 465.55
Formula C28H27N5O2
CAS No. 1639422-97-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (53.70 mM)

TargetMolReferences and Literature

1. Hatcher JM, et al. Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. J Med Chem. 2015 Dec 10;58(23):9296-9308.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Inhibitor Library Kinase Inhibitor Library Microtubule-Targeted Compound Library Bioactive Compounds Library Max Bioactive Compound Library Cytoskeletal Signaling Pathway Compound Library

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Keywords

JH-VIII-157-02 1639422-97-1 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors ALK Microtubule Associated CD246 Cluster of differentiation 246 inhibit Anaplastic lymphoma kinase Anaplastic lymphoma kinase (ALK) ALK tyrosine kinase receptor Inhibitor JHVIII15702 JH VIII 157 02 inhibitor

 

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