HIF-2α-IN-8 is a potent and orally active HIF2α inhibitor with IC50 values of 9, 37, 246 nM for HIF2α SPA, HIF2α iScript, HIF2α HRE RGA, respectively. HIF-2α-IN-8 shows antitumor activity[1].
HIF-2α-IN-8 (Example 31) (30 mg/kg; p.o.; daily for 21 days) 在小鼠体内显示出抗肿瘤活性[1]。
| Animal Model: | 6-9 weeks, female nude Crl:NU(NCr)-Foxn1nu-Homozygous mice (786-O mouse model)[1] |
| Dosage: | 30 mg/kg |
| Administration: | P.o.; started 34 days post tumor inoculation; daily for 21 days |
| Result: | Inhibited the tumor growth. |
[1]. Robin Alec Fairhurst, et al. Compounds and compositions for inhibiting the activity of hif2-alpha and their methods of use. WO2021220170A1.