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MedChemExpressModel PT-2385 -1672665-49-4

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PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM[1][2].
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PT-2385

MCE China:PT-2385

Brand:MedChemExpress (MCE)

Cat. No.HY-12867

CAS:1672665-49-4

Purity:99.95%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months

Shipping:Room temperature in continental US; may vary elsewhere.

Description:PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM.

In Vitro:PT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1α[1].

In Vivo:PT-2385 (30 or 100 mg/kg; oral gavage; twice daily) result in a rapid, dose-dependent tumor regression[3]. PT-2385 (PT2385) 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].

IC50 & Target:Kd: [1] In Vitro PT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1α[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PT-2385 Related Antibodies

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References:

[1]. Eli Wallace, Ph.D. PT2385: HIF-2α Antagonist for the Treatment of VHL Mutant ccRCC. 12th International VHL Medical Symposium April 8, 2016.

[2]. Xie C, et al. Activation of intestinal hypoxia-inducible factor 2α during obesity contributes to hepatic steatosis. Nat Med. 2017 Nov;23(11):1298-1308.  [Content Brief]

[3]. Wallace EM, et al. A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma. Cancer Res. 2016 Sep 15;76(18):5491-500.  [Content Brief]

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