PT2399

PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β.

Product information

CAS Number: 1672662-14-4

Molecular Weight: 419.32

Formula: C17H10F5NO4S

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

Smiles: N#CC1=CC(F)=CC(=C1)OC1=CC=C(C2[C@H](O)C(F)(F)CC=21)S(=O)(=O)C(F)F

InChiKey: MXUSGDMIHGLCNC-HNNXBMFYSA-N

InChi: InChI=1S/C17H10F5NO4S/c18-9-3-8(7-23)4-10(5-9)27-12-1-2-13(28(25,26)16(19)20)14-11(12)6-17(21,22)15(14)24/h1-5,15-16,24H,6H2/t15-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO 84 mg/mL (200.32 mM) Ethanol 84 mg/mL (200.32 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

PT2399 dissociates HIF-2 (an obligatory heterodimer [HIF-2α/HIF-1β])14 in human Clear cell Renal Cell Carcinoma (ccRCC) suppressing tumorigenesis in 56% (10/18) lines. PT2399 has greater activity than sunitinib, is active in sunitinib-progressing tumors, and is better tolerated. Illustrating drug specificity, gene expression is largely unaffected by PT2399 in resistant tumors. Sensitive tumors exhibits a distinguishing gene expression signature, and generally higher HIF-2α levels. Prolonged PT2399 treatment leads to resistance.

References:

1. Olga Martínez-Sáez, et al. Crit Rev Oncol Hematol. 2017 Mar;111:117-123.
2. Wenfang Chen, et al. Nature. 2016 Nov 3;539(7627):112-117.

Products are for research use only. Not for human use.