PTC-028
PTC-028 Basic information
- Product Name:
- PTC-028
- Synonyms:
-
- PTC-028
- PTC028;PTC 028
- CS-1497
- 2-Pyrazinamine, 6-(5,6-difluoro-2-methyl-1H-benzimidazol-1-yl)-N-[4-(trifluoromethyl)phenyl]-
- 6-(5,6-Difluoro-2-methyl-1H-benzimidazol-1-yl)-N-[4-(trifluoromethyl)phenyl]-2-pyrazinamine
- inhibit,Inhibitor,PTC 028,PTC-028,PTC028,Apoptosis
- 6-(5,6-Difluoro-2-methyl-1H-benzo[d]imidazol-1-yl)-N-(4-(trifluoromethyl)phenyl)pyrazin-2-amine
- PTC-028, 10 mM in DMSO
- CAS:
- 1782970-28-8
- MF:
- C19H12F5N5
- MW:
- 405.32
- Product Categories:
-
- API
- Mol File:
- 1782970-28-8.mol
PTC-028 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMF: 20 mg/ml; DMSO: 1 mg/ml
- form
- A solid
- color
- White to off-white
PTC-028 Usage And Synthesis
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].
?
No obvious toxicity is noted in the animals during therapy experiments as assessed by mean body weight[1].
?
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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