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WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
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17702719238 17702719238 |
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sales@sun-shinechem.com |
| Products Intro: |
Product Name:Ensartinib hydrochloride
CAS:2137030-98-7
Purity:98% HPLC Package:50.0mg;100.0mg; 200.0mg;500mg;1g;5g; 10g
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Ensartinib dihydrochloride manufacturers
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| | Ensartinib dihydrochloride Basic information |
| Product Name: | Ensartinib dihydrochloride | | Synonyms: | Ensartinib dihydrochloride;Ensartinib hydrochloride;X-396 hydrochloride;Ensartinib hydrochloride ( X396);X-396 dihydrochloride;Ensartinib,X396,Cluster of differentiation 246,X 396,Inhibitor,CD246,Anaplastic lymphoma kinase (ALK),Anaplastic lymphoma kinase,c-Met/HGFR,ALK tyrosine kinase receptor,Ensartinib hydrochloride,inhibit,X-396;Ensartinib 2HCl;Ensartinib (X-396) dihydrochloride | | CAS: | 2137030-98-7 | | MF: | C26H28Cl3FN6O3 | | MW: | 597.9 | | EINECS: | | | Product Categories: | APIS | | Mol File: | 2137030-98-7.mol |  |
| | Ensartinib dihydrochloride Chemical Properties |
| storage temp. | 0 - 4℃ for short term (days to weeks), or -20℃ for long term (months). | | form | solid | | color | white | | Water Solubility | Water : 5 mg/mL (7.88 mM) |
| | Ensartinib dihydrochloride Usage And Synthesis |
| Description | Ensartinib
HCl is the salt form of Ensartinib, an orally available small molecule
inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase
(ALK) with potential antineoplastic activity. Upon oral administration,
X-396 binds to and inhibits ALK kinase, ALK fusion proteins and ALK
point mutation variants. Inhibition of ALK leads to the disruption of
ALK-mediated signaling and eventually inhibits tumor cell growth in
ALK-expressing tumor cells. ALK belongs to the insulin receptor
superfamily and plays an important role in nervous system development. | | Uses | Ensartinib dihydrochloride (X-396 dihydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. | | in vivo | Ensartinib (X-396) dihydrochloride shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with Ensartinib dihydrochloride at 25 mg/kg bid. Ensartinib dihydrochloride significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, Ensartinib dihydrochloride appears well-tolerated in vivo. Mouse weight is unaffected by Ensartinib dihydrochloride treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of Ensartinib dihydrochloride, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of Ensartinib dihydrochloride at 20, 40, 80 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 80 mg/kg for Ensartinib dihydrochloride. At NST levels, Ensartinib dihydrochloride achieves an AUC of 66 μM×hr and a Cmax of 7.19 μM[1]. | | References | [1] Lovly CM, et al. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinaseinhibitors. Cancer Res. 2011 Jul 15;71(14):4920-31. DOI:10.1158/0008-5472.CAN-10-3879 |
| | Ensartinib dihydrochloride Preparation Products And Raw materials |
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