PI3K/mTOR Inhibitor-12_product_DataBase

Bioactivity	PI3K/mTOR Inhibitor-12 is a potent, orally active and selective PI3K/mTOR inhibitor with IC50 values of 0.06 nM and 3.12 nM for PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-12 has antitumor activity. PI3K/mTOR Inhibitor-12 has lower liver toxicity[1].
Invitro	PI3K/mTOR Inhibitor-12 (compound 48; 72 h) 抑制癌细胞生长，对 PC-3、HT-29、HCT116、LOVO 和 HUVEC 细胞的 IC50 值分别为 0.07、0.09、0.54、0.54 和 0.68 μM[1].PI3K/mTOR Inhibitor-12 (0.25-1 μM; 12-48 h; HCT116 和 HT-29 细胞) 抑制细胞环境中 PI3K 和 mTOR 的激活[1]。 Western Blot Analysis[1] Cell Line:
In Vivo	PI3K/mTOR Inhibitor-12 (compound 48; 20 mg/kg; p.o.; 每日一次, 持续 14 天) 抑制雌性 BALB/c 裸鼠中 HCT116 异种移植物的肿瘤生长[1]。PI3K/mTOR Inhibitor-12 (1 和 5 mg/kg; i.v. 和 p.o.; 雄性 SD 大鼠) 具有快速血浆清除率 (1428 mL/h/kg) 和短 T1/2 (2.33 h)，AUC0-∞ 为 1356 h*ng/mL[1]。 Animal Model:
Name	PI3K/mTOR Inhibitor-12
Formula	C27H27F2N9O4S
Molar Mass	611.62
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Li C, et, al. Function-oriented synthesis of Imidazo[1,2-a]pyrazine and Imidazo[1,2-b]pyridazine derivatives as potent PI3K/mTOR dual inhibitors. Eur J Med Chem. 2022 Dec 20;247:115030.

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