基本属性 生物活性靶点体外研究体内研究 用途与合成方法 PI-273 价格(试剂级) 供应商

PI-273

PI-273

中文名称:PI-273
英文名称:2-[(4-chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide
CAS号:925069-34-7
分子式:C16H16ClN3O2S2
分子量:381.9
EINECS号:
Mol文件:925069-34-7.mol
PI-273 结构式

PI-273 性质

密度 1.425±0.06 g/cm3(Predicted)
储存条件 Store at -20°C
溶解度 二甲基亚砜:6.25 mg/mL(16.37 mM)
酸度系数(pKa) 8.09±0.70(Predicted)

PI-273 用途与合成方法

PI-273 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。

PI4KIIα

0.47 μM (IC 50 )

PI-273 (2 μM; 48 hours) blocks the cell cycle at the G2-M phase.
PI-273 (2 μM; 48 hours) induces cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3.
PI-273 (0.5-2 μM; for 3 days) can suppress the AKT signaling pathway in a dose- and time-dependent manner.
PI-273 of 1 μM and 2 μM inhibits the cell proliferation of both MCF-7 and T-47D cells in a time-dependent manner.

Cell Cycle Analysis

Cell Line: MCF-7, T-47D, SK-BR-3, MDA-MB-231, SUM229PE, Hs 578T cells
Concentration: 2 μM
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: 2 μM
Incubation Time: 48 hours
Result: Induced cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3.

Western Blot Analysis

Cell Line: MCF-7 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: For 3 days
Result: Suppressed the AKT signaling pathway in a dose- and time-dependent manner.

PI-273 (intraperitoneal injection; 25 mg/kg/day; 15 days) profoundly suppresses the tumor volume and weight in the MCF-7 xenografts.
PI-273 (0.5 mg/kg (intravenously) or 1.5 mg/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: 0.5 mg/kg (intravenously) or 1.5 mg/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%.

PI-273 价格(试剂级)

更新日期 产品编号 产品名称 CAS号 包装 价格
2024-04-30 HY-103489 PI-273 925069-34-7 1mg 800
2024-04-30 HY-103489 PI-273 925069-34-7 5mg 1400

PI-273供应商 更多

上海一飞生物科技有限公司
联系电话:021-65675885 18964387627
产品介绍:
英文名称:PI-273
CAS:925069-34-7
纯度:98%
包装信息:5mg;10mg;25mg
备注:试剂级
天津凯利奇生物科技有限公司
联系电话: 15076683720
产品介绍:
英文名称:PI-273
CAS:925069-34-7
纯度:≥98%
包装信息:1g,5g,10g,25g根据客户需要分装
备注:Not For Human Use, Lab Use Only.
上海瀚香生物科技有限公司
联系电话:17754423994 17754423994
产品介绍:
英文名称:PI-273
CAS:925069-34-7
纯度:98% HPLC LCMS
包装信息:100mg;500mg;1g
备注:现货,仅供科研用途
北京普西唐生物科技有限公司
联系电话:010-60605840 18892239720
产品介绍:
英文名称:PI-273
CAS:925069-34-7
纯度:98%
包装信息:1mg;5mg
ChemeGen 中国
联系电话: 18818260767
产品介绍:
英文名称:PI-273
CAS:925069-34-7
纯度:98%
包装信息:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
备注:品牌:ChemeGen