PT2399

• Description:

  PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo[1][2][3].

• UNSPSC:

  12352005

• Target:

  HIF/HIF Prolyl-Hydroxylase

• Type:

  Reference compound

• Related Pathways:

  Metabolic Enzyme/Protease

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/pt2399.html

• Purity:

  99.96

• Solubility:

  DMSO : ≥ 200 mg/mL

• Smiles:

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

• Molecular Formula:

  C17H10F5NO4S

• Molecular Weight:

  419.32

• References & Citations:

  [1]Chen W, et al. Targeting renal cell carcinoma with a HIF-2 antagonist. Nature. 2016 Nov 3;539 (7627) :112-117.|[2]Cho H, et al. On-Target Efficacy of a HIF2α Antagonist in Preclinical Kidney Cancer Models. Nature. Nature. 2016 Nov 3;539 (7627) :107-111.|[3]Wehn PM, et al. Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) 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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, stored under nitrogen)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  [1672662-14-4]