AS-605240|648450-29-7|-陌孚医药/Medlife

您当前的位置：

AS-605240

目录号: PC15447 纯度: ≥98%

CAS No. :648450-29-7

商品编号	规格	价格	会员价
PC15447-10mg	10mg	¥490.00	请登录
PC15447-50mg	50mg	¥1911.00	请登录
PC15447-100mg	100mg	¥2744.00	请登录
PC15447-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥539.00	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称

AS-605240

中文别名

5-(6-喹噁啉yl亚甲基)-2,4-噻唑烷二酮;5-(6-喹喔啉亚甲基)-2,4-噻唑啉二酮;AS-605240 磷酸肌醇3激酶抑制剂;AS-605240 抑制剂;酮比索洛尔;替诺福韦

英文名称

AS-605240

英文别名

2,4-Thiazolidinedione,5-(6-quinoxalinylmethylene)-;AS-605240;5-(6-Quinoxalinylmethylene)-2,4-thiazolidinedione;AS 605240;AS 605240,5-(6-Quinoxalinylmethylene)-2,4-thiazolidine-2,4-dione;PI 3-Kγ Inhibitor;AS605240;5-QUINOXALIN-6-YLMETHYLENE-THIAZOLIDINE-2,4-DIONE;PI 3-Kgamma Inhibitor;(5Z)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolidine-2,4-dione;(5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE-2,4-DIONE;QYT;(Z)-5-(Quinoxalin-6-ylmethylene)thiazolidine-2,4-dione;PI 3-Kg inhibitor;2a5u;5-(quinoxalin-6-ylmethylene)thiazolidine-2,4-dione;GTPL6023;AOB3848;HMS3650I15;HMS3229I19;HMS32

Cas No.

648450-29-7

分子式

C₁₂H₇N₃O₂S

分子量

257.27

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC₅₀ of 8 nM, and a K_i of 7.8 nM.

性状

Solid

IC50 & Target[1][2]

PI3Kα

60 nM (IC₅₀)

PI3Kβ

270 nM (IC₅₀)

PI3Kδ

300 nM (IC₅₀)

PI3Kγ

8 nM (IC₅₀)

PI3Kγ

7.8 nM (Ki)

Autophagy

体外研究(In Vitro)

AS-605240 is an isoform-selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18- and 7.5-fold selectivity over PI3Kα, respectively. AS-605240 shows an inhibitory effect on C5a-mediated PKB phosphorylation in RAW264 mouse macrophages with an IC₅₀ of 0.09 μM. AS-605240 blocks PKB phosphorylation induced by MCP-1 and has little or no effect after stimulation with CSF-1. AS-605240 inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α and β in a concentration-dependent manner. AS605240 suppresses in a dose-dependent manner the proliferation of BDC2.5 CD4 T cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

AS-605240 (30 mg/kg BW, per os, every 12 h) markedly decreases FoxM1 expression in mouse lungs and fails to restore vascular integrity. AS-605240 reduces RANTES-induced peritoneal neutrophil recruitment, with ED₅₀ of 9.1 mg/kg. In the CCL5 model, AS-605240 shows an ED₅₀ value of 10 mg/kg, in correlation with the percentage of reduction of neutrophil recruitment observed in Pik3cg mice. AS-605240 (50 mg/kg, p.o.) substantially reduces clinical and histological signs of joint inflammation to a similar extent to that of Pik3cg mice. AS605240 (30 mg/kg, i.p.) suppresses intracellular PAkt in splenocytes of NOD mice and delays diabetes onset. AS605240 also prevents autoimmune diabetes in prediabetic NOD mice, and suppresses autoreactive T cells while increasing Tregs in NOD mice. AS605240 (30 mg/kg, i.p.) reverses hyperglycemia in newly hyperglycemic NOD mice, reverses hyperglycemia in early diabetic NOD mice through Tregs and suppresses T-cell infiltration in pancreatic islets while increasing Tregs. AS605240 (25, 50 mg/kg) markedly reduces total cell count and numbers of macrophages, neutrophils and lymphocytes in rats. AS605240 significantly reduces the levels of TNF-α and IL-1β in BALF to 132.7±11.2 pg/mL and 49.2±11.3 pg/mL in 25 mg/kg AS605240 + BLM group and 131.3±10.7 and 49.6±8.8 pg/mL in 50 mg/kg AS605240 + BLM group, respectively. AS605240 inhibits prefibrotic cytokines production in bleomycin-induced pulmonary fibrosis. AS605240 inhibits phosphorylation of Akt of inflammatory cells in bleomycin-induced pulmonary fibrosis model.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Huang X, et al. Endothelial p110γPI3K Mediates Endothelial Regeneration and Vascular Repair After Inflammatory Vascular Injury. Circulation. 2016 Mar 15;133(11):1093-103. [Information]

[2]. Camps M, et al. Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med. 2005 Sep;11(9):936-43. [Information]

[3]. Azzi J, et al. The novel therapeutic effect of phosphoinositide 3-kinase-γ inhibitor AS605240 in autoimmune diabetes. Diabetes. 2012 Jun;61(6):1509-18. Epub 2012 Mar 8. [Information]

[4]. Wei X, et al. A phosphoinositide 3-kinase-gamma inhibitor, AS605240 prevents bleomycin-induced pulmonary fibrosis in rats. Biochem Biophys Res Commun. 2010 Jun 25;397(2):311-7. Epub 2010 May 26. [Information]

溶解度数据

体外研究:

DMSO : 3.33 mg/mL (12.94 mM; ultrasonic and warming and heat to 80°C)

H₂O : 2.78 mg/mL (10.81 mM; ultrasonic and warming and adjust pH to 10 with NaOH and heat to 60°C)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.8870 mL	19.4348 mL	38.8697 mL
5 mM	0.7774 mL	3.8870 mL	7.7739 mL
10 mM	0.3887 mL	1.9435 mL	3.8870 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 0.5% CMC-Na 0.5% Tween-80
Solubility: 6.25 mg/mL (24.29 mM); Suspened solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (9.72 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (9.72 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (9.72 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.72 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

相关产品

The molarity calculator equation

The dilution calculator equation