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925069-34-7

中文名稱 PI-273
英文名稱 2-[(4-chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide
CAS 925069-34-7
分子式 C16H16ClN3O2S2
分子量 381.9
MOL 文件 925069-34-7.mol
925069-34-7 結(jié)構(gòu)式 925069-34-7 結(jié)構(gòu)式

基本信息

中文別名
化合物PI-273
2-(3-(4-氯苯甲?;?硫脲基)-4-乙基-5-甲基噻吩-3-甲酰胺
英文別名
PI-273
2-[(4-chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide
2-({[(4-chlorobenzoyl)amino]carbonothioyl}amino)-4-ethyl-5-methyl-3-thiophenecarboxamide
3-Thiophenecarboxamide, 2-[[[(4-chlorobenzoyl)amino]thioxomethyl]amino]-4-ethyl-5-methyl-

物理化學(xué)性質(zhì)

密度1.425±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 6.25 mg/mL (16.37 mM)
酸度系數(shù)(pKa)8.09±0.70(Predicted)
形態(tài)Solid
顏色Light yellow to yellow

安全數(shù)據(jù)

PI-273價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-103489PI-273
PI-273
925069-34-71mg800元
2024/11/08HY-103489PI-273
PI-273
925069-34-75mg1400元
2024/11/08HY-103489PI-273
PI-273
925069-34-710mM * 1mLin DMSO1540元

常見問題列表

生物活性
PI-273 是第一種可逆的和特異性磷脂酰肌醇 4-激酶 (PI4KIIα) 抑制劑,IC50 為 0.47 μM。PI-273 可以抑制乳腺癌細胞的增殖,阻斷細胞周期并誘導(dǎo)細胞凋亡。
靶點

PI4KIIα

0.47 μM (IC 50 )

體外研究

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.
體內(nèi)研究

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%.
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