PI-273 - CAS:925069-34-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	PI-273 促销
英文名称:	PI-273
别名:	PI-273 2-({[(4-chlorophenyl)carbonyl]carbamothioyl}amino)-4-ethyl-5-methylthiophene-3-carboxamide
CAS No:	925069-34-7	分子式:	C₁₆H₁₆ClN₃O₂S₂	分子量:	381.9
CAS No:	925069-34-7
分子式:	C₁₆H₁₆ClN₃O₂S₂
分子量:	381.9

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P10810 PI-273 ≥98% (psaitong)

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包装规格：

1mg 5mg in glass bottle

溶解性：

溶于DMSO（6.02 mg/mL 超声）

产品描述：

基本信息

产品编号：P10810
产品名称：PI-273
CAS:	925069-34-7	储存条件	粉末	-20℃	四年

分子式：	C16H16ClN3O2S2		溶于液体	-80℃	六个月
分子量	381.90			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO
		Ethanol
		Water
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.6185 mL	13.0924 mL	26.1849 mL
5mM	0.5237 mL	2.6185 mL	5.2370 mL
10mM	0.2618 mL	1.3092 mL	2.6185 mL

生物活性

产品描述	是第一种可逆的和特异性磷脂酰肌醇 4-激酶 (PI4KIIα) 抑制剂，IC50 为 0.47 μM。PI-273 可以抑制乳腺癌细胞的增殖，阻断细胞周期并诱导细胞凋亡。
靶点/IC50	YES	Lyn		Fyn	Src
体外研究	PI-273 (2μM; 48 hours) blocks the cell cycle at the G2-M phase.PI-273 (2μM; 48 hours) induces cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3.PI-273 (0.5-2μM; for 3 days) can suppress the AKT signaling pathway in a dose- and time-dependent manner.PI-273 of 1μM and 2 μM inhibits the cell proliferation of both MCF-7 and T-47D cells in a time-dependent manner.PI-273 (2μM; 48 hours) blocks the cell cycle at the G2-M phase.PI-273 (2μM; 48 hours) induces cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3.PI-273 (0.5-2μM; for 3 days) can suppress the AKT signaling pathway in a dose- and time-dependent manner.PI-273 of 1μM and 2μM inhibits the cell proliferation of both MCF-7 and T-47D cells in a time-dependent manner.
	Cell Line:		MCF-7, T-47D, SK-BR-3, MDA-MB-231, SUM229PE, Hs 578T cells
	Concentration:		2μM
	Incubation Time:		48 hours
	Result:		Blocked the cell cycle at the G2-M phase.
	Apoptosis Analysis
	Cell Line:		MCF-7, T-47D, and SK-BR-3 cells
	Concentration:		2μM
	Incubation Time:		48 hours
	Result:		Induced cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SKBR-3.
	Western Blot Analysis
	Cell Line:		MCF-7 cells
	Concentration:		0.5, 1, 2μM
	Incubation Time:		For 3 days
	Result:		Suppressed the AKT signaling pathway in a dose- and time-dependent manner.
体内研究	PI-273 (intraperitoneal injection; 25mg/kg/day; 15 days) profoundly suppresses the tumor volume and weight in the MCF-7 xenografts.PI-273 (0.5mg/kg (intravenously) or 1.5mg/kg (intragastrically); 0.08-5 hours) has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%.
	Animal Model:		Eight-week-old male BALB/c nude mice with MCF-7 cell
	Dosage:		25 mg/kg
	Administration:		Intraperitoneal injection; daily; 15 days
	Result:		Suppressed the tumor volume and weight in the MCF-7 xenografts.

	Animal Model:		Male Sprague-Dawley (SD) rats
	Dosage:		0.5mg/kg (intravenously) or 1.5mg/kg (intragastrically) (Pharmacokinetic Study)
	Administration:		Intravenously or intragastrically; 0.08, 0.16, 0.33, 0.67, 1, 1.5, 2, 3 and 5 hours
	Result:		Has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%.