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AS-252424
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AS-252424图片
CAS NO:900515-16-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
AS-252424 是一种有效的选择性PI3Kγ抑制剂,IC50为 30±10 nM。
生物活性

AS-252424 is a potent and selectivePI3Kγinhibitor with anIC50of 30±10 nM.

IC50& Target[1]

PI3Kα

935 nM (IC50)

PI3Kγ

30 nM (IC50)

PI3Kδ

20 μM (IC50)

PI3Kβ

20 μM (IC50)

体外研究
(In Vitro)

AS-252424 also inhibits PI3Kα, PI3Kβ and PI3Kδ with IC50s of 935±150 nM, 20 μM and 20 μM, respectively. AS-252424 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC50value of 52 μM, as well as in the monocytic cell line THP-1 with an IC50value of 53 μM. In the human monocytic cell line THP-1, MCP-1 binding to the GPCR chemokine receptor CCR2, strongly induces phosphorylation of PKB/Akt, which is effectively inhibited by AS-252424 at IC50values as low as 0.4 μM. In contrast, induction of PKB/Akt phosphorylation by colony stimulating factor (CSF-1), binding to the growth factor receptor c-fms, is only blocked by AS-252424 at IC50values as high as 4.7 μM[1].

体内研究
(In Vivo)

Oral administration of AS-252424 in a mouse model of acute peritonitis leads to a significant reduction of leukocyte recruitment. To evaluate the efficacy of AS-252424 to block leukocyte migration in vivo, it is tested in a mouse model of thioglycollate-induced peritonitis. Oral administration of AS-252424 at 10 mg/kg results in moderate reduction of neutrophil recruitment (35%±14%), almost matching the result observed in PI3Kγ-deficient mice. Given the short oral half-life of AS-252424 (t1/2=1 h) and relative high clearance (2.25 L/kg per h), investigations at later time points (24-48 h) to assess macrophage and monoycyte recruitment are not undertaken. The modest pharmacokinetic properties do not appear to be caused by rapid oxidative metabolism (microsomal metabolism after 1 h: 16% (rat), 10% (human))[1].

分子量

305.28

性状

Solid

Formula

C14H8FNO4S

CAS 号

900515-16-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL(81.89 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.2757 mL16.3784 mL32.7568 mL
5 mM0.6551 mL3.2757 mL6.5514 mL
10 mM0.3276 mL1.6378 mL3.2757 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。