Ensartinib dihydrochloride

Catalog No.S2934 Batch:S293401

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Technical Data

Formula

C26H29Cl4FN6O3
Molecular Weight 634.36 CAS No. 2137030-98-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (157.63 mM)
Water 27 mg/mL (42.56 mM)
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.83mg/ml Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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].

Protocol (from reference)

Selleck's Ensartinib dihydrochloride has been cited by 6 publications

NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations [ Cancer Discov, 2024, OF1-OF20.] PubMed: 39269178
Induction of in vivo-like ciliation in confluent monolayers of re-differentiated equine oviduct epithelial cells [ Biol Reprod, 2024, ioae090] PubMed: 38847468
Pharmacological targeting of the receptor ALK inhibits tumorigenicity and overcomes chemoresistance in pancreatic ductal adenocarcinoma [ Biomed Pharmacother, 2022, 158:114162] PubMed: 36571997
P-glycoprotein Mediates Resistance to the Anaplastic Lymphoma Kinase Inhiitor Ensartinib in Cancer Cells [ Cancers (Basel), 2022, 14(9)2341] PubMed: 35565470
Mechanisms of targeted therapy resistance in a pediatric glioma driven by ETV6-NTRK3 fusion [ Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109] PubMed: 34429303
Flow-cytometrická analýza inhibičního vlivu nových cílených léčiv na aktivitu ABC lékových efluxních transportérů [ CU Digital Repository, 2020, N/A] PubMed: N/A

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.