A HIF-2α inhibitor
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Isomer(s)
39652Belzutifan
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PT2385

Item No. 21325

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[(1S)-2,2-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluoro-benzonitrile
CAS Number
1672665-49-4
Molecular Formula
C17H12F3NO4S
Formula Weight
383.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
FC1=CC(OC2=CC=C(S(C)(=O)=O)C3=C2CC(F)(F)[C@H]3O)=CC(C#N)=C1
InChi Code
InChI=1S/C17H12F3NO4S/c1-26(23,24)14-3-2-13(12-7-17(19,20)16(22)15(12)14)25-11-5-9(8-21)4-10(18)6-11/h2-6,16,22H,7H2,1H3/t16-/m0/s1
InChi Key
ONBSHRSJOPSEGS-INIZCTEOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    50 mg

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    100 mg

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    Cayman Chemical
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    Product Description

    PT2385 is an inhibitor of hypoxia-inducible factor-2α (HIF-2α; IC50 = 12 nM).1 It inhibits HIF-2α-induced transcription of intratumoral Vegfa mRNA and reduces tumor volume in a 786-O renal cell carcinoma mouse xenograft model when administered at a dose of 10 mg/kg. PT2385 (20 mg/kg) also inhibits the production of soluble FMS-related tyrosine kinase 1 (sFlt1) and prevents the development of hypertension and proteinuria, markers of preeclampsia, in pregnant rat dams.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wehn, P.M., Rizzi, J.P., Dixon, D.D., et al. Design and activity of specific hypoxia-inducible factor-2α (HIF-2α) inhibitors for the treatment of clear cell renal cell carcinoma: Discovery of clinical candidate (s)-3-((2,2-difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1h-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385). J. Med. Chem. 61(21), 9691-9721 (2018).

    2. Colson, A., Depoix, C.L., Lambert, I., et al. Specific HIF-2α (hypoxia-inducible factor-2) inhibitor PT2385 mitigates placental dysfunction in vitro and in a rat model of preeclampsia (RUPP). Hypertension 80(5), 1011-1023 (2023).