PT2399 Inhibitor

PT2399 shows effective antitumor activity in vivo. PT2399 is an effective and selective HIF-2alpha antagonist, which directly binds to the HIF-2alpha PAS B domain (IC50: 6nM).

Chen W, et al. Targeting renal cell carcinoma with a HIF-2 antagonist. Nature. 2016 Nov 3;539(7627):112-117.
Chen W, et al. Targeting renal cell carcinoma with a HIF-2 antagonist. Nature. 2016 Nov 3;539(7627):112-117.
Cho H, et al. On-Target Efficacy of a HIF2alpha Antagonist in Preclinical Kidney Cancer Models. Nature. Nature. 2016 Nov 3;539(7627):107-111.
Cho H, et al. On-Target Efficacy of a HIF2alpha Antagonist in Preclinical Kidney Cancer Models. Nature. Nature. 2016 Nov 3;539(7627):107-111.
Wehn PM, et al. Design and Activity of Specific Hypoxia-Inducible Factor-2alpha (HIF-2alpha) Inhibitors for the treatment,of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385). J Med Chem. 2018 Nov 8;61(21):9691-9721.
Wehn PM, et al. Design and Activity of Specific Hypoxia-Inducible Factor-2alpha (HIF-2alpha) Inhibitors for the treatment,of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385). J Med Chem. 2018 Nov 8;61(21):9691-9721.

Small volumes of PT2399, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5753798 is an inhibitor targeting PT2399.