Onvansertib (PCM-075, NMS-1286937, NMS-P937) is a first-in-class, third-generation, oral, highly selective PLK1 inhibitor that induces tumor cell arrest in the G2/M phase and triggers apoptosis. It has a median IC50=136nM against a variety of CRC cell lines and inhibits xenograft models such as HT-29, HCT-116, and Colo-205 well.
| Molecular Weight | 532.52 |
| Formula | C24H27F3N8O3 |
| CAS Number | 1034616-18-6 |
| Solubility (25°C) | DMSO 21 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related PLK Products |
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| 3MB-PP1
3MB-PP1 is a bulky purine analog and inhibitor of Polo-like kinase 1 (Plk1) that blocks mitotic progression and cytokinesis by targeting Plk1 in cells expressing the analog-sensitive Plk1 allele. 3MB-PP1 also specifically inhibits the activity of Leu93 mutant Zipper-interacting Ssn3 (Cdk8). 3MB-PP1 inhibits the activity of Leu93 mutant Zipper-interacting Ssn3 (Cdk8). In addition, 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits the Leu93 mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used in the mycelium of Candida albicans. 3MB-PP1 can be used in studies related to mycelium formation and cell division in Candida albicans. |
| CYC-800
CYC-800 is a PLK1 inhibitor that can be used in tumor-related studies. |
| SOL-686
SOL-686 is a PLK1 inhibitor that can be used in glioma-related studies. |
| BAL0891
BAL0891 is a potential first-in-class PLK1/TTK inhibitor with antiproliferative activity for studies related to solid tumors. |
| Plogosertib
Plogosertib is a selective, potent, orally active, ATP-competitive PLK1 inhibitor with an IC50 value of 3 nM.In addition, Plogosertib exhibits antiproliferative and anticancer activity and can be used in a variety of tumor studies. |
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