| Identification | Back Directory | [Name]
Ensartinib dihydrochloride | [CAS]
2137030-98-7 | [Synonyms]
X-396 hydrochloride
Ensartinib hydrochloride
Ensartinib dihydrochloride | [Molecular Formula]
C26H28Cl3FN6O3 | [MDL Number]
MFCD31657344 | [MOL File]
2137030-98-7.mol | [Molecular Weight]
597.9 |
| Chemical Properties | Back Directory | [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) |
| Hazard Information | Back Directory | [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 |
|
| Company Name: |
Wuhan Topule
|
| Tel: |
+86-02787215551 +86-19945035818 |
| Website: |
http://www.topule.com/ |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|