LDK-378 dihydrochloride

参考资料仅供科学研究，不可用于个人用途。

货号：BCP10604CAS号：1380575-43-8纯度：98%

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CAS号	1380575-43-8	货号	BCP10604
中文名	LDK-378 dihydrochloride
英文名	LDK-378 dihydrochloride
中文别名
英文别名	LDK 378;LDK378;Ceritinib;
SMILES
化学名称
分子式	C28H38Cl3N5O3S	分子量	631.06
纯度	98%	配送	惯例下常温包邮
产品描述	in vitro: LDK378 shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC50 of 26.0 nM and 22.8 nM, compared with IC50 of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells . in vivo: LDK378 is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. LDK378 has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. LDK378 exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. LDK378 induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. LDK378 shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg .