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PT2385
CAS No. 1672665-49-4
PT2385( PT-2385 )
Catalog No. M12551 CAS No. 1672665-49-4
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.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 122 | In Stock |
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| 2MG | 85 | In Stock |
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| 5MG | 147 | In Stock |
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| 10MG | 235 | In Stock |
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| 25MG | 400 | In Stock |
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| 50MG | 550 | In Stock |
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| 100MG | 765 | In Stock |
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| 200MG | 1014 | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NamePT2385
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NoteResearch use only, not for human use.
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Brief DescriptionPT2385 (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.
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DescriptionPT2385 (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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In VitroPT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1α.
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In VivoPT-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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SynonymsPT-2385
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PathwayAngiogenesis
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TargetHIF/HIF Prolyl-hydroxylase
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RecptorHIF/HIF Prolyl-hydroxylase
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Research AreaCancer
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IndicationKidney Cancer
Chemical Information
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CAS Number1672665-49-4
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Formula Weight383.3417
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Molecular FormulaC17H12F3NO4S
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Purity>98% (HPLC)
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Solubility10 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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Chemical NameBenzonitrile, 3-[[(1S)-2,2-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluoro-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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.
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