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PT-2385

PT-2385 是一种选择性HIF-2α抑制剂，Ki< 50 nM。

CAS号

1672665-49-4

分子式

C17H12F3NO4S

主要靶点

HIF/HIF Prolyl-Hydroxylase|HIF

仅限科研使用

Cat No : CM04472

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Synonyms

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  • CAS No.: 1672665-49-4

    PT-2385
    CAS#: 1672665-49-4

产品信息

PT-2385 is a selective HIF-2α inhibitor (Kd<50 nM).

CAS号 1672665-49-4
分子式 C17H12F3NO4S
主要靶点 HIF/HIF Prolyl-Hydroxylase|HIF
主要通路 表观遗传|血管生成|代谢
分子量 383.34
纯度 98.69%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

HIF-2α:<50 nM (Kd)

体内活性

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].

体外活性

PT-2385 is a selective antagonist of HIF-2 and inactive for HIF-1α [1].

溶解度

DMSO:50 mg/mL (130.43 mM)

动物实验

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]

参考文献

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.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.

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