PT-2385

SKU: orb1299450

Description

PT-2385 is a potent and selective small molecule inhibitor of HIF-2α, exhibiting a dissociation constant (Kd) below 50 nM. It is a valuable research tool for studying hypoxia signaling pathways in both cellular and animal models, particularly in oncology and renal physiology research.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Metabolism Research

Key Properties

• CAS Number: 1672665-49-4
• MW: 383.34
• Purity: 99.55% (May vary between batches)
• Formula: C₁₇H₁₂F₃NO₄S
• SMILES: CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC(F)(F)[C@@H](O)c12
• Target: HIF,HIF/HIF Prolyl-Hydroxylase
• Solubility: DMSO:270 mg/mL (704.34 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.22 mM)

Bioactivity

• Target IC50:
  HIF2α:<50 nM (Kd)
• In Vivo:
  PT-2385 inhibits expression of HIF-2α regulated genes in a dose dependent manner in vivo. Tumor is regressed with PT-2385 (3 and 10 mg/kg, p.o., b.i.d. dose) in 786-O xenograft. PT-2385 (1,3 and 10 mg/kg) also inhibits tumor-derived VEGFA protein levels. PT-2385 (10 mg/kg) treatment reduces proliferation (Ki67) and angiogenesis (CD-31) . PT-2385 (30 or 100 mg/kg; oral gavage; twice daily) result in a rapid, dose-dependent tumor regression .
• In Vitro:
  PT-2385 is a selective antagonist of HIF-2 and inactive for HIF-1α .
• Animal Research:
  Animal Model: SCID/beige mice with the 786-O and A498 RCC cell lines. Dosage: 30 or 100 mg/kg. Administration: Oral gavage; twice daily

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Hypoxia-inducible factors, HIFProlylHydroxylase, HIFs, HIF ProlylHydroxylase, HIF Prolyl-Hydroxylase, HIF, HIF/HIFProlylHydroxylase, HIF/HIF ProlylHydroxylase, HIF/HIF Prolyl-Hydroxylase, HIF-PH, HIF-2α, PT 2385, PT2385, PT-2385

Compound Identifiers

PubChem CID

91754484