AS-604850|648449-76-7|-陌孚医药/Medlife

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AS-604850

目录号: PC15477 纯度: ≥98%

CAS No. :648449-76-7

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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。

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中文名称

AS-604850

中文别名

5-(2,2-二氟-苯唑[1,3]二氧-5-基亚甲基)-噻唑烷-2,4-二酮;5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮

英文名称

AS-604850

英文别名

AS-604850;PI 3-Kinase Inhibitor (AS604850) B-0302;5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione;PI3Kγ inhibitor;PI 3-Kgamma Inhibitor II;(5E)-5-[(2,2-DIFLUORO-1,3-BENZODIOXOL-5-YL)METHYLENE]-1,3-THIAZOLIDINE-2,4-DIONE;PI3Kgamma inhibitor;(5Z)-5-[(2,2-difluoro-1,3-benzodioxol-5-yl)methylidene]-1,3-thiazolidine-2,4-dione;BYM;2a4z;AS604850;PI 3-Kg inhibitor II;MLS006010996;GTPL6024;HMS3261F11;HMS3229I21;HMS3650F11;BCPP000389;Tox21_500505;s2681

Cas No.

648449-76-7

分子式

C₁₁H₅F₂NO₄S

分子量

285.22

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-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC₅₀ value of 0.25 μM and a K_i value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively.

性状

Solid

IC50 & Target[1][2]

PI3Kγ

0.25 μM (IC₅₀)

PI3Kγ

0.18 μM (Ki)

PI3Kα

4.5 μM (IC₅₀)

体外研究(In Vitro)

AS-604850 inhibits C5a-mediated PKB phosphorylation with an IC₅₀ of 10 μM in RAW264 mouse macrophages.
AS-604850 blocks PKB phosphorylation induced by MCP-1 and has little or no effect after stimulation with CSF-1 in in primary monocytes from Pik3cg or Pik3cg mice.
AS-604850 (0-30 μM; 15 minutes; primary monocytes from Pik3cg mice) treatment inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs is also reduced, in a concentration dependent manner in primary monocytes from Pik3cg mice.

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

Western Blot Analysis

Cell Line:	Primary monocytes from Pik3cg mice
Concentration:	0 μM, 1 μM, 3 μM, 10 μM, 30 μM
Incubation Time:	15 minutes
Result:	Inhibited MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs was also reduced, in a concentrationdependent manner in primary monocytes from Pik3cg mice.

体内研究(In Vivo)

AS-604850 (10-100 mg/kg; oral administration; for 4.5 or 4.25 hours; Balb/C or C3H mice) treatment reduces RANTES-induced peritoneal neutrophil recruitment with an ED₅₀ value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, oral administration of 10 mg/kg AS-604850 results in a 31% reduction of neutrophil recruitment.

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

Animal Model:	Balb/C or C3H mice with human recombinant RANTES or thioglycollate
Dosage:	10 mg/kg, 30 mg/kg or 100 mg/kg
Administration:	Oral administration; for 4.5 or 4.25 hours
Result:	Reduced RANTES-induced peritoneal neutrophil recruitment with an ED₅₀ value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, resulted in a 31% reduction of neutrophil recruitment.

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]. 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]

溶解度数据

体外研究:

DMSO : 250 mg/mL (876.52 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.5061 mL	17.5303 mL	35.0607 mL
5 mM	0.7012 mL	3.5061 mL	7.0121 mL
10 mM	0.3506 mL	1.7530 mL	3.5061 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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.29 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.29 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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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。

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