CAS:870281-34-8Acalisib

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Synonyms: GS-9820

Acalisib is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

870281-34-8

储存条件

分子式

C21H16FN7O

运输

蓝冰

分子量

401.40

别名

GS-9820

溶解度

DMSO	95.0 mg/mL (236.7 mM) warming
Water	insoluble

动物实验配方

生物活性

描述The phosphoinositide 3 kinases (PI3K) are a family of lipid kinases. In mammals, the PI3K family is divided into three different classes (I, II, and III), and class I PI3K is further subdivided into IA (activated by receptor tyrosine kinases) and IB (activated by G protein–coupled receptors). Class IA PI3K are heterodimers composed of the p85 regulatory subunit and the p110 catalytic subunit (isoforms: p110α, β, γ, δ). Acalisib is a potent and selective inhibitor of PI3Kδ with IC₅₀ value of 12.7 nM. Eligible patients who had measurable lymphadenopathy and required therapy for their cancers were treated with acalisib, with oral doses of 50, 100, 200, and 400 mg twice daily for 5.8 months and results showed that acalisib demonstrated clinical activity which may point to a class effect rather than a specific drug effect. GS-9820 at 5 or 10 mg/kg had no significant effect on obese hyperphagic ob/ob mice, while PI3Kα inhibitor, BYL-719 or CNIO-PI3Ki efficiently reduced body weight after 15 days of treatment.
动物研究
剂量
Ob/ob Mice: 5 mg/kg, 10 mg/kg^[2] (p.o.)

给药途径
p.o.