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Acalisib

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Chemical Structure| 870281-34-8 同义名 : GS-9820;CAL-120
CAS号 : 870281-34-8
货号 : A317394
分子式 : C21H16FN7O
纯度 : 99%+
分子量 : 401.397
MDL号 : MFCD28411423
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(298.96 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • p110δ

    p110δ, IC50:14 nM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.49mL

0.50mL

0.25mL

12.46mL

2.49mL

1.25mL

24.91mL

4.98mL

2.49mL
参考文献

[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.