JH-VIII-157-02

SKU: orb1308177

Description

JH-VIII-157-02

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1639422-97-1
• MW: 465.55
• Purity: 99.58% (May vary between batches)
• Formula: C₂₈H₂₇N₅O₂
• SMILES: CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1-c1cnn(CC(=O)N(C)C)c1
• Target: ALK,Microtubule Associated
• Solubility: DMSO:25 mg/mL (53.7 mM)

Bioactivity

• Target IC50:
  EML4-ALK (F1174L):2 nM|EML4-ALK (C1156Y):2 nM|EML4-ALK (G1202R):2 nM|EML4-ALK (WT):2 nM
• In Vivo:
  In mice, JH-VIII-157-02 (10 mg/kg) exhibits good oral bioavailability and penetrates the central nervous system.
• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cluster of differentiation 246, CD246, Anaplastic lymphoma kinase, Anaplastic lymphoma kinase (ALK), ALK tyrosine kinase receptor, ALK, inhibit, JH VIII 157 02, JHVIII15702, JH-VIII-157-02, Microtubule Associated, MicrotubuleAssociated, EML4-ALKwt, cell assay, EML4-ALK C1156Y, cell assay, EML4-ALK F1174L, cell assay, EML4-ALK G1202R, cell assay, Inhibitor

Compound Identifiers

PubChem CID

127037084