PI-273

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PI-273 (PI273) 是一种有效、特异性、底物竞争性的 PI4KIIα 小分子抑制剂，IC50 为 0.47 uM。

PI-273 (PI273) is a potent, specific, substrate-competitive small molecule inhibitor of PI4KIIα with IC50 of 0.47 uM; reduces PI4P content, cell viability and AKT signaling in wild-type MCF-7 cells but not in PI4KIIα knockout MCF-7 cells; retards cell proliferation by blocking cells in G2/M, inducing cell apoptosis and suppressing colony-forming ability, significantly inhibits MCF-7 cell-induced breast tumor growth without toxicity in a xenograft model (intravenous or intragastrical).

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%.

PI273

PI3K/Akt/mTOR signaling

PI4K

PI4K

Cancer

——

925069-34-7

381.893

C16H16ClN3O2S2

>98% (HPLC)

In Vitro:?DMSO : 6.02 mg/mL (15.76 mM)

CCC1=C(SC(=C1C(=O)N)NC(=S)NC(=O)C2=CC=C(C=C2)Cl)C

2-(3-(4-chlorobenzoyl)thioureido)-4-ethyl-5-methylthiophene-3-carboxamide

(-20℃)

With Ice Pack

≥ 2 years