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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 | ￥947 | 有现货 |
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| 5MG | ￥1397 | 有现货 |
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| 10MG | ￥2451 | 有现货 |
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| 25MG | ￥4027 | 有现货 |
|
| 50MG | ￥5747 | 有现货 |
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| 100MG | ￥7641 | 有现货 |
|
| 500MG | ￥15120 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥1482 | 有现货 |
|
生物学信息
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产品名称PT2385
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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
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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。
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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).
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体外实验PT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1α.
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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.
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同义词PT-2385
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通路Angiogenesis
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靶点HIF/HIF Prolyl-hydroxylase
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受体HIF/HIF Prolyl-hydroxylase
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研究领域Cancer
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适应症Kidney Cancer
化学信息
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CAS Number1672665-49-4
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分子量383.3417
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分子式C17H12F3NO4S
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纯度>98% (HPLC)
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溶解度10 mM in DMSO
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SMILESCS(C(C=C1)=C2C(CC(F)(F)[C@H]2O)=C1OC3=CC(C#N)=CC(F)=C3)(=O)=O
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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
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储存条件(-20℃)
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运输条件With Ice Pack
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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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