HIF-2α-IN-8

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].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase

IC50: 9 nM (HIF2α SPA); 37 nM (HIF2α iScript); 246 nM (HIF2α HRE RGA)[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.