PT-2399

Research use only, not for human use.

PT-2399 (PT 2399, PT2399)?is a selective, potent HIF-2α antagonist that binds directly to the HIF2α PAS B domain.

PT-2399 (PT 2399, PT2399)?is a selective, potent HIF-2α antagonist that binds directly to the HIF2α PAS B domain; minimally affects a panel of 68 receptors, ion channels, and enzymes; specifically disassembles HIF-2 but not HIF-1 complexes, reduces the expression of HIF-2 target genes (VEGF, SERPINE1, IGFBP3, CCND1, TGFA, and SLC2A1), but not HIF-1 targets (CA9, PGK1, and LDHA); exhibits tumor growth inhibition in selected VHL-deficient clear-cell renal cell carcinoma (ccRCC) models.

——

Animal Model:Mice with RCC tumorgraft Dosage:100 mg/kg Administration:Oral gavage; every 12 hours Result:More active than SU 11248, and inhibited tumor growth in several SU 11248-resistant tumors.

PT 2399 | PT2399

Angiogenesis

HIF/HIF Prolyl-hydroxylase

HIF/HIF Prolyl-hydroxylase

——

——

1672662-14-4

419.32

C17H10F5NO4S

>98% (HPLC)

DMSO : ≥ 200 mg/mL 476.96 mM

N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C(F)F)=O)C3=C2CC(F)(F)[C@H]3O)=C1

3-[(1S)-7-(difluoromethylsulfonyl)-2,2-difluoro-1-hydroxy-indan-4-yl]oxy-5-fluoro-benzonitrile

(-20℃)

With Ice Pack

≥ 2 years