A BMI1 inhibitor
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PTC-596

Item No. 33529

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-fluoro-2-(6-fluoro-2-methyl-1H-benzimidazol-1-yl)-N4-[4-(trifluoromethyl)phenyl]-4,6-pyrimidinediamine
CAS Number
1610964-64-1
Synonyms
  • Unesbulin
Molecular Formula
C19H13F5N6
Formula Weight
420.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 5 mg/ml
λmax
222, 262, 300 nm
SMILES
FC1=CC2=C(N=C(C)N2C3=NC(NC4=CC=C(C(F)(F)F)C=C4)=C(F)C(N)=N3)C=C1
InChi Code
InChI=1S/C19H13F5N6/c1-9-26-13-7-4-11(20)8-14(13)30(9)18-28-16(25)15(21)17(29-18)27-12-5-2-10(3-6-12)19(22,23)24/h2-8H,1H3,(H3,25,27,28,29)
InChi Key
TWLWOOPCEXYVBE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $87

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    5 mg

    $348

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    10 mg

    $566

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    25 mg

    $978

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    Cayman Chemical
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    Product Description

    PTC-596 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.1,2 It inhibits proliferation of MOLM-13 acute myeloid leukemia (AML) and Rec-1 mantle cell lymphoma (MCL) cancer cells (IC50s = 22.4 and 136 nM, respectively). It also induces BMI1 degradation in, and apoptosis of, the same cells. PTC-596 reduces microtubule polymerization and induces cell cycle arrest at the G2/M phase in MM.1S multiple myeloma cells.3 It decreases the number of side population cells, a unique cell population with stem-like characteristics, in Rec-1 cells (IC50 = 138 nM).2 PTC-596 (5 mg/kg, p.o.) increases survival in a MOLM-13 mouse xenograft model.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nishida, Y., Maeda, A., Kim, M.J., et al. The novel BMI-1 inhibitor PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells. Blood Cancer J. 7(2), e527 (2017).

    2. Maeda, A., Nishida, Y., Weetall, M., et al. Targeting of BMI-1 expression by the novel small molecule PTC596 in mantle cell lymphoma. Oncotarget. 9(47), 28547-28560 (2018).

    3. Nagai, Y., Mimura, N., Rizq, O., et al. The combination of the tubulin binding small molecule PTC596 and proteasome inhibitors suppresses the growth of myeloma cells. Sci. Rep. 11(1), 2074 (2021).