化合物 PI3Kα-IN-9 T61654

Product Introduction
Bioactivity


英文名: PI3Kα-IN-9

描述: PI3Kα-IN-9 (compound 27) is a highly specific, orally active, and long-lasting inhibitor of PI3Kα, demonstrating potent inhibitory effects with IC50 values of 4.4, 128, 146, and 153 nM against PI3Kα, PI3Kγ, PI3Kδ, and PI3Kβ, respectively. Additionally, PI3Kα-IN-9 exhibits antiproliferative properties and effectively induces apoptosis. Given its characteristics, PI3Kα-IN-9 holds great potential for cancer research [1].

体外活性: PI3Kα-IN-9 (compound 27) (0-8 μM; 72 hours; cancer cell lines) has antiproliferative activity and induces apoptosis [1]. PI3Kα-IN-9 (compound 27) (0-8 μM; MGC-803 cells) down-regulates the expression of PI3Kα protein, the proteins of PI3K downstream, p-AKT and p-P70S6 K [1]. Cell Viability Assay [1] Cell Line: MGC-803 (gastric cancer), SKOV-3 (ovarian cancer), PC-3(prostate cancer), MCF-7 (breast cancer), MDA-MB-231 (triple-negative breast cancer), HepG2 (liver cancer), RPMI8226 (multiple myeloma), K562 (chronic myeloid leukemia), U251 (glioma) and MOLT-4 (acute lymphoblastic leukemia) cell lines Concentration: 0-2 μM Incubation Time: 72 hours Result: Inhibited the growth of a variety of cancer cells with IC 50 values ranging from 0.43 to 1.33 μM. Apoptosis Analysis [1] Cell Line: MGC-803 cells Concentration: 0, 2, 4 and 8 μM Incubation Time: 36 hours Result: Increased the percentage of apoptotic cells from 12.07 to 61.69% in a dose-dependent manner.

体内活性: PI3Kα-IN-9 (compound 27) (1-10 mg/kg; p.o. and i.v.; for 24 hours; male Sprague-Dawley rat) has favorable stability (T 1/2 >10 h) and high bioavailability (130%) [1]. PI3Kα-IN-9 (compound 27) (30 mg/kg; p.o.; daily, for 3 weeks; male BALB/c nude mice) has antitumor activity and low cytotoxicity [1]. Animal Model: Male Sprague-Dawley rat [1] Dosage: 1 and 10 mg/kg Administration: Oral administration and intravenous injection; for 24 hours (Pharmacokinetic Analysis) Result: 1.19 parameters IV PO dose (mg/kg) 1 10 T 1/2 (h) 6.29 ﹥10 T max (h) 0.003 9.33 C max (ng/mL) 454.7 2256.7 AUC 0-t (ng·h/mL) 2237 36697 AUC 0-∞ (ng·h/mL) 2922.4 38114.3 CL (mL/h/kg) 343 F % 130.4 Animal Model: Male BALB/c nude mice [1] Dosage: 30 mg/kg Administration: Oral administration; daily, for 3 weeks Result: Inhibited tumor growth with a tumor growth inhibition (TGI) rate of 41.5%.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途