A molecular glue
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Product Categories

Product Type

Biochemicals

Research Area

Cancer
Cell Cycle
G1
Cell Death
Apoptosis
Necrosis

OPB-171775

Item No. 45601

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[2,3-difluoro-4-(2-hydroxy-2-methylpropoxy)phenyl]-4,5-dihydro-5-methyl-3(2H)-pyridazinone
CAS Number
2131210-15-4
Molecular Formula
C15H18F2N2O3
Formula Weight
312.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/mLEthanol: Slightly soluble: 0.1-1 mg/mL
SMILES
FC1=C(C2=NNC(C[C@H]2C)=O)C=CC(OCC(C)(O)C)=C1F
InChi Code
InChI=1S/C15H18F2N2O3/c1-8-6-11(20)18-19-14(8)9-4-5-10(13(17)12(9)16)22-7-15(2,3)21/h4-5,8,21H,6-7H2,1-3H3,(H,18,20)/t8-/m1/s1
InChi Key
GGUTYKLJESECBW-MRVPVSSYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $189

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    10 mg

    $284

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    Cayman Chemical
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    Product Description

    OPB-171775 is a molecular glue.1 It induces the formation of a complex between phosphodiesterase 3A (PDE3A) and ribonuclease SLFN12. OBI-171775 (10 nM) induces G0/G1 phase cell cycle arrest, apoptosis, and necrosis in PFSK-1 primitive neuroectodermal tumor cells, with cell cycle arrest partially blocked by the general control nonderepressible 2 kinase (GCN2) inhibitor GCN2iB (Item No. 35897). It reduces tumor volume and induces tumor regression in patient-derived xenograft (PDX) mouse models of a variety of cancer types, including gastrointestinal stromal tumor (GIST), ovarian, and lung cancers. OPB-171775 (0.03 mg/kg) reduces tumor growth in a GS11353 PDX mouse model of GIST, with tumor eradication when administered in combination with imatinib (Item No. 13139).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Takaki, E.O., Kiyono, K., Obuchi, Y., et al. A PDE3A-SLFN12 molecular glue exhibits significant antitumor activity in TKI-resistant gastrointestinal stromal yumors. Clin. Cancer Res. 30(16), 3603-3621 (2024).