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CAS No.: 870281-34-8

Acalisib Catalog No. CSN18510

Synonyms: GS-9820;CAL-120

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

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

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^[2]. 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^[2]. 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^[3].
动物研究
剂量
Ob/ob Mice: 5 mg/kg, 10 mg/kg^[2] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Ob/ob Mice: 5 mg/kg, 10 mg/kg^[2] (p.o.)
给药途径	p.o.

[1] Shugg RP, Thomson A, et al. Effects of isoform-selective phosphatidylinositol 3-kinase inhibitors on osteoclasts: actions on cytoskeletal organization, survival, and resorption. J Biol Chem. 2013 Dec 6;288(49):35346-57.
[2] Kater AP, Tonino SH, Spiering M, Chamuleau MED, Liu R, Adewoye AH, Gao J, Dreiling L, Xin Y, Doorduijn JK, Kersten MJ; HOVON Lunenburg Lymphoma Phase I/II Consortium. Final results of a phase 1b study of the safety and efficacy of the PI3Kδ inhibitor acalisib (GS-9820) in relapsed/refractory lymphoid malignancies. Blood Cancer J. 2018 Feb 12;8(2):16. doi: 10.1038/s41408-018-0055-x. PMID: 29434192; PMCID: PMC5809482.
[3] Lopez-Guadamillas E, Muñoz-Martin M, Martinez S, Pastor J, Fernandez-Marcos PJ, Serrano M. PI3Kα inhibition reduces obesity in mice. Aging (Albany NY). 2016 Nov 4;8(11):2747-2753. doi: 10.18632/aging.101075. PMID: 27816049; PMCID: PMC5191867.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4913 mL
- 12.4565 mL
- 24.9130 mL
- 5 mM
- 0.4983 mL
- 2.4913 mL
- 4.9826 mL
- 10 mM
- 0.2491 mL
- 1.2457 mL
- 2.4913 mL

技术信息

CAS号

870281-34-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H16FN7O

运输

蓝冰

分子量

401.40

别名

GS-9820;CAL-120

溶解度

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

动物实验配方

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