Antibodies
RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.
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| Description | RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM. | |||||
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| Targets | Polo-like kinase 1 | |||||
| IC50 | 3 nM [1] | |||||
| 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] | |||||
| 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] | |||||
| Features | A selective PLK1 inhibitor. Demonstrates greater potency than BI2536. Potential use in nasopharyngeal carcinomas. | |||||
| Animal Models | Human colorectal cancer xenografts HT-29 |
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| Dosages | 40 mg/kg |
| Administration | q4d i.v. |
| Molecular Weight (MW) | 543.61 |
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| Formula | C27H35F2N7O3 |
| CAS No. | 1062243-51-9 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | Ro5203280 |
| Solubility (25°C) * | In vitro | DMSO | 100 mg/mL (183 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 100 mg/mL (183 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | Benzamide, 4-[(9-cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methyl-4-piperidinyl)- |
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