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PT2385

CAS No. 1672665-49-4

PT2385 ( PT-2385 )

产品货号. M12551 CAS No. 1672665-49-4

PT2385 (PT-2385) 是一种有效的、选择性的、口服活性的 HIF2α 拮抗剂,与 HIF2α PAS-B 结构域 (Kd=50 nM) 结合并破坏 HIF2α/ARNT 二聚体的形成。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
2MG ¥721 有现货
5MG ¥1256 有现货
10MG ¥2195 有现货
25MG ¥3507 有现货
50MG ¥5200 有现货
100MG ¥7395 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    PT2385
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    PT2385 (PT-2385) 是一种有效的、选择性的、口服活性的 HIF2α 拮抗剂,与 HIF2α PAS-B 结构域 (Kd=50 nM) 结合并破坏 HIF2α/ARNT 二聚体的形成。
  • 产品描述
    PT2385 (PT-2385) is a potent, selective, and orally active antagonist of HIF2α, binds to HIF2α PAS-B domain (Kd=50 nM) and disrupts HIF2α/ARNT dimer formation; allosterically blocks HIF2α dimerization with the HIF1α/2α transcriptional dimerization partner ARNT/HIF1β, disrupts HIF2α, but not HIF1α, heterodimerization with ARNT in Hep3B cells; inhibits the expression of HIF2α-dependent genes, including VEGF-A, PAI-1, and cyclin D1 in ccRCC cell lines and tumor xenografts, also reduces HIF2α mRNA and protein levels in xenograft tumors.Kidney Cancer Phase 2 Clinical(In Vitro):PT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1α.(In Vivo):PT-2385 (30 or 100 mg/kg; oral gavage; twice daily) result in a rapid, dose-dependent tumor regression.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).
  • 体外实验
    PT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1α.
  • 体内实验
    PT-2385 (30 or 100 mg/kg; oral gavage; twice daily) result in a rapid, dose-dependent tumor regression. 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). 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 Result:Resulted in a rapid, dose-dependent tumor regression.
  • 同义词
    PT-2385
  • 通路
    Angiogenesis
  • 靶点
    HIF/HIF Prolyl-hydroxylase
  • 受体
    HIF/HIF Prolyl-hydroxylase
  • 研究领域
    Cancer
  • 适应症
    Kidney Cancer

化学信息

  • CAS Number
    1672665-49-4
  • 分子量
    383.3417
  • 分子式
    C17H12F3NO4S
  • 纯度
    >98% (HPLC)
  • 溶解度
    10 mM in DMSO
  • SMILES
    CS(C(C=C1)=C2C(CC(F)(F)[C@H]2O)=C1OC3=CC(C#N)=CC(F)=C3)(=O)=O
  • 化学全称
    Benzonitrile, 3-[[(1S)-2,2-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluoro-

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Wallace EM, et al. Cancer Res. 2016 Sep 15;76(18):5491-500. 2. Chen W, et al. Nature. 2016 Nov 3;539(7627):112-117. 3. Courtney KD, et al. J Clin Oncol. 2018 Mar 20;36(9):867-874. 4. Xie C, et al. Nat Med. 2017 Nov;23(11):1298-1308.
产品手册
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