PD-1/PD-L1-IN-9
产品名称:PD-1/PD-L1-IN-9
产品描述:
产品描述 | PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, IC50 = 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model. |
体外活性 | PD-1/PD-L1-IN-9 (46.9-1500 nM; pretreated for 2 h) dose-dependently significantly activates the antitumor immunity of PBMCs to MDB-MB 231 cells, EC50 = ∼100 nM[1]. |
体内活性 | PD-1/PD-L1-IN-9 (40-80 mg/kg; p.o. once a day for 2 weeks) inhibits tumor growth in a dose-dependent manner and does not cause any body weight loss or mortality of mice. PD-1/PD-L1-IN-9 (3 mg/kg; a single i.v.) exhibits half-life (t1/2=4.2 h), plasma clearance (Cl=11.5 L/h/kg) and Cmax (1233 ng/mL) in rats. PD-1/PD-L1-IN-9 (25 mg/kg; a single p.o.) exhibits moderate oral bioavailability (F=22 %), half-life (t1/2=6.4 h) and Cmax (192 ng/mL) in rats[1]. |
分子量 | 348.44 |
分子式 | C22H24N2O2 |
CAS No. | 2628506-54-5 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 90 mg/mL (258.3 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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