 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 1062243-51-9 |
| Molecular formula(MF) | C27H35F2N7O3 |
| Molecular Weight(MW): | 543.61 |
| Alias |
| In vitro | DMSO | 100 mg/mL (183.95 mM) |
|---|---|---|
| Ethanol | 100 mg/mL (183.95 mM) | |
| Water | <1 mg/mL |
| Description | RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM. | ||
|---|---|---|---|
| Features | A selective PLK1 inhibitor. Demonstrates greater potency than BI2536. Potential use in nasopharyngeal carcinomas. | ||
| Targets |
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| In vitro |
RO3280 shows the strong anti-proliferative activity against lung cancer cell line H82, colorectal cancer cell HT-29, breast cancer cell MDA-MB-468, prostate cancer cell PC3 and skin cancer cell A375 with IC50s of 5, 10, 19, 12 and 70 nM, respectively. [1] |
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| In vivo | RO3280 displays robust antitumor activity in nude mouse implanted with HT-29 human colorectal tumors ranging from 72% tumor growth inhibition when dosed once weekly at 40 mg/kg, to complete tumor regression when dosed more frequently.. [1] |