HIF-2α-IN-8 is a potent and orally active HIF2α inhibitor with IC 50 values of 9, 37, 246 nM for HIF2α SPA, HIF2α iScript, HIF2α HRE RGA, respectively. HIF-2α-IN-8 shows antitumor activity
In Vivo
HIF-2α-IN-8 (Example 31) (30 mg/kg; p.o.; daily for 21 days) shows antitumor activity in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-9 weeks, female nude Crl:NU(NCr)-Foxn1nu-Homozygous mice (786-O mouse model) Dosage: 30 mg/kg Administration: P.o.; started 34 days post tumor inoculation; daily for 21 days Result: Inhibited the tumor growth.
