A BMI1 inhibitor
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PTC-028

Item No. 34471

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(5,6-difluoro-2-methyl-1H-benzimidazol-1-yl)-N-[4-(trifluoromethyl)phenyl]-2-pyrazinamine
CAS Number
1782970-28-8
Molecular Formula
C19H12F5N5
Formula Weight
405.3
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 1 mg/ml
λmax
280, 350 nm
SMILES
FC1=C(F)C=C2N(C3=NC(NC4=CC=C(C(F)(F)F)C=C4)=CN=C3)C(C)=NC2=C1
InChi Code
InChI=1S/C19H12F5N5/c1-10-26-15-6-13(20)14(21)7-16(15)29(10)18-9-25-8-17(28-18)27-12-4-2-11(3-5-12)19(22,23)24/h2-9H,1H3,(H,27,28)
InChi Key
JEZGPBWIZWPDHP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $158

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    10 mg

    $291

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    25 mg

    $543

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    Cayman Chemical
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    Product Description

    PTC-028 is an inhibitor of B cell-specific Moloney murine leukemia virus integration site 1 (BMI1), which is a member of the polycomb repressive complex 1 (PRC1) that has a role in gene silencing.1 It inhibits proliferation of OVCAR-4 and OV-90 ovarian cancer cells (IC50s = ~0.1 µM for both). It also induces BMI1 degradation in, and apoptosis of, the same cells in a concentration-dependent manner. PTC-028 reduces microtubule polymerization and induces cell cycle arrest at the G2/M phase in MDS-L myelodysplastic syndrome cells when used at concentrations of 3 and 0.03 µM, respectively.2 It reduces tumor growth in a OV-90 orthotopic mouse model of ovarian cancer when administered biweekly at a dose of 15 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dey, A., Xiong, X., Crim, A., et al. Evaluating the mechanism and therapeutic potential of PTC-028, a novel inhibitor of BMI-1 function in ovarian cancer. Mol. Cancer Ther. 17(1), 39-49 (2018).

    2. Zhong, C., Kayamori, K., Koide, S., et al. Efficacy of the novel tubulin polymerization inhibitor PTC-028 for myelodysplastic syndrome. Cancer Sci. 111(12), 4336-4347 (2020).