PTC-028

A BMI1 inhibitor

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5mg

￥1037.00

830.00

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10mg

￥1625.00

1300.00

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25mg

￥3312.00

2650.00

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50mg

￥5500.00

4400.00

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100mg

￥8637.00

6910.00

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200mg

￥0.00

0.00

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500mg

￥0.00

0.00

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Background

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 ?M 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 ?M, 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

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 cancerMol. 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 syndromeCancer Sci.111(12)4336-4347(2020)