648450-29-7|AS-605240|CsnPharm

CAS No.: 648450-29-7

AS-605240 Catalog No. CSN13098

Synonyms: AS-605240

AS-605240 selectively inhibits PI3Kγ with IC50 of 8 nM, over 30-fold and 7.5-fold selective for PI3Kγ than PI3Kδ/β and PI3Kα in cell-free assays, respectively.

规格	价格	促销价格	库存	数量

400-920-2911

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tech@csnpharm.cn

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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

靶点 PI3Kα

IC50:60nM PI3Kβ

IC50:270nM PI3Kδ

IC50:300nM PI3Kγ

IC50:8nM
描述The phosphoinositide 3-kinases (PI3Ks) control a number of essential intracellular signaling pathways involved in the cell life cycle, and play a critical role in the cardiovascular system. The PI3K family is divided into three classes, with class I divided into subclass IA and IB. PI3K-α, -β, and -δ isoforms belong to class IA and are primarily activated by receptor tyrosine kinases, whereas PI3K-γ isoform, which belongs to class IB, are facilitated by G-protein-coupled receptors (GPCRs). PI3K-γ is a key regulator of inflammatory responses and cardiovascular homeostasis. PI3Kγ is also a mediator in G-protein coupled receptor signaling and therefore is involved in the directed migration of neutrophils and macrophages in response to chemokines^[3]. AS-605240 is a specific PI3Kγ inhibitor with IC50s 8 nM, 68 nM, 312 nM, and 386 nM for PI3Kγ, PI3Kα, PI3Kβ and PI3Kδ, respectively. AS-605240 can reduce the phosphorylation level of its downstream Akt^[3]. In a vitro study, treatment with 10 μM AS-605240 for 0, 2, 5 or 10 minutes blocked all Akt phosphorylation in T-ALL cell lines including 1156, 1713, C6, and C7 cell lines with high RasGRP1 expression^[4]. Administration of AS605240 at a dose of 10 mg/kg for 24h to LPS-treated mice reduced some patho-physiological characteristics of SIMD and reduced TNF-α, IL-6, cTnI and H-FABP production^[3].
细胞研究
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
RAW264.7 cells - Function assay - Inhibition of MCP1-induced chemotaxis in mouse RAW264.7 cells, IC50=5.31 μM 19904929
动物研究
剂量
Mice: 30 mg/kg^[3] (i.p.); 30 mg/kg^[4] (p.o.), 50 mg/kg^[5] (p.o.)

给药途径
i.p., p.o.
参考文献

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
RAW264.7 cells	-	Function assay	-	Inhibition of MCP1-induced chemotaxis in mouse RAW264.7 cells, IC50=5.31 μM	19904929

动物研究
剂量	Mice: 30 mg/kg^[3] (i.p.); 30 mg/kg^[4] (p.o.), 50 mg/kg^[5] (p.o.)
给药途径	i.p., p.o.

[1] Kim JI, Lee HR, et al. PI3Kγ is required for NMDA receptor-dependent long-term depression and behavioral flexibility. Nat Neurosci. 2011 Oct 23;14(11):1447-54.
[2] Camps M, Ruckle T, et al. Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med. 2005 Sep;11(9):936-43. Epub 2005 Aug 28.
[3] Fan TT, Feng XY, Yang YZ, Gao F, Liu Q. Downregulation of PI3K-γ in a mouse model of sepsis-induced myocardial dysfunction. Cytokine. 2017 Aug;96:208-216. doi: 10.1016/j.cyto.2017.04.018. Epub 2017 Apr 28. PMID: 28458167.
[4] Ksionda O, Mues M, Wandler AM, Donker L, Tenhagen M, Jun J, Ducker GS, Matlawska-Wasowska K, Shannon K, Shokat KM, Roose JP. Comprehensive analysis of T cell leukemia signals reveals heterogeneity in the PI3 kinase-Akt pathway and limitations of PI3 kinase inhibitors as monotherapy. PLoS One. 2018 May 25;13(5):e0193849. doi: 10.1371/journal.pone.0193849. PMID: 29799846; PMCID: PMC5969748.

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
- 3.8870 mL
- 19.4350 mL
- 38.8700 mL
- 5 mM
- 0.7774 mL
- 3.8870 mL
- 7.7740 mL
- 10 mM
- 0.3887 mL
- 1.9435 mL
- 3.8870 mL

技术信息

CAS号

648450-29-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H7N3O2S

运输

蓝冰

分子量

257.27

别名

AS-605240

溶解度

DMSO	800.0 mg/mL (3109.6 mM)
Water	100.0 mg/mL (388.7 mM)

动物实验配方

0.5% CMC-Na

80 mg/mL

clear

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靶点	Description	IC50
PI3Kα		IC50:60nM
PI3Kβ		IC50:270nM
PI3Kδ		IC50:300nM
PI3Kγ		IC50:8nM

AS-605240 Catalog No. CSN13098

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