| Identification | Back Directory | [Name]
PTC-028 | [CAS]
1782970-28-8 | [Synonyms]
PTC-028
CS-1497
PTC028;PTC 028
6-(5,6-Difluoro-2-methyl-1H-benzimidazol-1-yl)-N-[4-(trifluoromethyl)phenyl]-2-pyrazinamine
2-Pyrazinamine, 6-(5,6-difluoro-2-methyl-1H-benzimidazol-1-yl)-N-[4-(trifluoromethyl)phenyl]- | [Molecular Formula]
C19H12F5N5 | [MOL File]
1782970-28-8.mol | [Molecular Weight]
405.32 |
| Hazard Information | Back Directory | [Uses]
PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. PTC-028 selectively inhibits cancer cells whereas normal cells remain unaffected. PTC-028 downregulates BMI-1, inducing caspase-mediated apoptosis[1]. | [in vivo]
PTC-028 (15 mg/kg; administered orally twice weekly) causes ~94% (0.169 g) reduction in tumor weight compared to the control (average tumor weight, ~3g) [1].
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No obvious toxicity is noted in the animals during therapy experiments as assessed by mean body weight[1].
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PTC-028 (10 mg/kg or 20mg/kg; single oral doses) is administrated to the CD-1 mice. The Cmax is reached at both dose levels 1h post dose after which plasma concentrations slowly reduce[1]. | Animal Model: | Female athymic nude mice with implanted OV90 cells[1] | | Dosage: | 15 mg/kg | | Administration: | Orally administered; twice weekly | | Result: | Caused ~94% (0.169 g) reduction in tumor weight. |
| Animal Model: | Female CD-1 mice[1] | | Dosage: | 10 mg/kg or 20mg/kg | | Administration: | Oral administered; single dose | | Result: | Total plasma AUC0-24h were 10.9 and 26.1 μg?h/mL at doses of 10 and 20 mg/kg. The Cmax for PTC-028 at 10 and 20 mg/kg was 0.79 and 1.49 ug/mL, respectively. |
| [References]
[1] Dey 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. 2018 Jan;17(1):39-49. DOI:10.1158/1535-7163.MCT-17-0574 |
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