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PT-2385 is a selective inhibitor of HIF-2α with a dissociation constant (Kd) of less than 50 nM (Kd<50 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $61 | In Stock | |
2 mg | $89 | In Stock | |
5 mg | $155 | In Stock | |
10 mg | $271 | In Stock | |
25 mg | $433 | In Stock | |
50 mg | $642 | In Stock | |
100 mg | $913 | In Stock | |
1 mL x 10 mM (in DMSO) | $128 | In Stock |
Description | PT-2385 is a selective inhibitor of HIF-2α with a dissociation constant (Kd) of less than 50 nM (Kd<50 nM). |
Targets&IC50 | HIF2α:<50 nM (Kd) |
In vitro | PT-2385 is a selective antagonist of HIF-2 and inactive for HIF-1α [1]. |
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) [1]. PT-2385 (30 or 100 mg/kg; oral gavage; twice daily) result in a rapid, dose-dependent tumor regression [2]. |
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 [2] |
Molecular Weight | 383.34 |
Formula | C17H12F3NO4S |
Cas No. | 1672665-49-4 |
Smiles | CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC(F)(F)[C@@H](O)c12 |
Relative Density. | 1.57 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (143.48 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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