Home Angiogenesis ALK inhibitor Ensartinib dihydrochloride For research use only.

Ensartinib dihydrochloride

Synonyms: X-396 dihydrochloride

Ensartinib dihydrochloride is a potent new-generation ALK inhibitor with high activity against a broad range of known crizotinib-resistant ALK mutations and CNS metastases. It potently inhibits both wild-type ALK and ALK variants (F1174, C1156Y, L1196M, S1206R, T1151, and G1202R mutants) with in vitro IC50s of <4 nM.

Ensartinib dihydrochloride Chemical Structure

Ensartinib dihydrochloride Chemical Structure

CAS No. 2137030-98-7

Purity & Quality Control

Batch: S293401 DMSO]100 mg/mL]false]Water]27 mg/mL]false]Ethanol]Insoluble]false Purity: 99.87%
99.87

Ensartinib dihydrochloride Related Products

Signaling Pathway

ALK Signaling Pathways

ALK Signaling Pathway

Biological Activity

Description Ensartinib dihydrochloride is a potent new-generation ALK inhibitor with high activity against a broad range of known crizotinib-resistant ALK mutations and CNS metastases. It potently inhibits both wild-type ALK and ALK variants (F1174, C1156Y, L1196M, S1206R, T1151, and G1202R mutants) with in vitro IC50s of <4 nM.
Targets
TPM3-TRKA [1]
(Cell-free assay)		 TRKC [1]
(Cell-free assay)		 GOPC-ROS1 [1]
(Cell-free assay)		 ALK [1]
(Cell-free assay)		 ALK variants [1]
(Cell-free assay)
<1 nM <1 nM <1 nM <4 nM <4 nM
In vitro
In vitro

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

Chemical Information & Solubility

Molecular Weight 634.36 Formula

C26H29Cl4FN6O3
CAS No. 2137030-98-7 SDF --
Smiles CC1CN(CC(N1)C)C(=O)C2=CC=C(C=C2)NC(=O)C3=NN=C(C(=C3)OC(C)C4=C(C=CC(=C4Cl)F)Cl)N.Cl.Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (157.63 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 27 mg/mL

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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