Ensartinib hydrochloride

SKU: orb1306001

Description

Ensartinib hydrochloride (X-396 dihydrochloride) is a next-generation, potent ALK inhibitor effective against wild-type ALK and multiple crizotinib-resistant mutants, including G1202R and L1196M, with IC50 values below 4 nM. It demonstrates significant activity against central nervous system metastases and is utilized in preclinical oncology research for both in vitro and in vivo studies of ALK-driven cancers.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2137030-98-7
• MW: 634.36
• Purity: 99.29% (May vary between batches)
• Formula: C₂₆H₂₉Cl₄FN₆O₃
• SMILES: Cl.Cl.C[C@@H](Oc1cc(nnc1N)C(=O)Nc1ccc(cc1)C(=O)N1C[C@H](C)N[C@H](C)C1)c1c(Cl)ccc(F)c1Cl
• Target: Trk receptor,c-Met/HGFR,ALK
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:2 mg/mL (3.15 mM);DMSO:33 mg/mL (52.02 mM)

Bioactivity

• Target IC50:
  GOPC-ROS1:<1 nM|ALK (variants):<4 nM|ALK:<4 nM|TrkC:<1 nM|TPM3-TRKA:<1 nM
• In Vitro:
  Ensartinib potently inhibits both wild-type ALK and all evaluated ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM. Besides ALK, ensartinib also potently inhibits GOPC-ROS1, TPM3-TRKA, and TRKC with an IC50 of <1 nM, and inhibits EphA1, EphA2, EphB1 and c-MET with an IC50 of 1-10 nM.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cluster of differentiation 246, CD246, cMet, c-Met, cMet/HGFR, c-Met/HGFR, ALK tyrosine kinase receptor, ALK variants, ALK, Anaplastic lymphoma kinase (ALK), Anaplastic lymphoma kinase, GOPC-ROS1, Ensartinib, Ensartinib dihydrochloride, Ensartinib Dihydrochloride, Ensartinib Hydrochloride, Ensartinib hydrochloride, HGFR, inhibit, Inhibitor, X 396, X 396 Dihydrochloride, X-396 Dihydrochloride, X396, X-396, X396 Dihydrochloride, X-396 dihydrochloride, TPM3-TRKA, Trk receptor, TRKC, Trkreceptor

Compound Identifiers

PubChem CID

138320013