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Technical Data
| Formula | C27H35F2N7O3 |
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| Molecular Weight | 543.61 | CAS No. | 1062243-51-9 | |
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (183.95 mM) | |
| Ethanol | 100 mg/mL (183.95 mM) | |||
| Water | Insoluble | |||
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* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | RO3280 (Ro5203280) is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM. | ||
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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] | ||
| 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. |
Protocol (from reference)
Customer Product Validation
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Data from [Data independently produced by , , J Cell Mol Med, 2017, 21(4):758-767]
Selleck's Ro3280 has been cited by 6 publications
| Inhibition of PLK1 Destabilizes EGFR and Sensitizes EGFR-Mutated Lung Cancer Cells to Small Molecule Inhibitor Osimertinib [ Cancers (Basel), 2023, 15(9)2589] | PubMed: 37174055 |
| Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors [ J Med Chem, 2021, 10.1021/acs.jmedchem.1c01096] | PubMed: 34710325 |
| Targeting Polo-like kinase 1 and TRAIL enhances apoptosis in non-small cell lung cancer [ Oncotarget, 2018, 9(47):28731-28744] | PubMed: 29983892 |
| Targeted inhibition of Polo-like kinase 1 by a novel small-molecule inhibitor induces mitotic catastrophe and apoptosis in human bladder cancer cells. [Zhang Z, et al. J Cell Mol Med, 2017, 21(4):758-767] | PubMed: 27878946 |
| Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells. [ Int J Mol Sci, 2015, 16(1):1266-92] | PubMed: 25574601 |
| Mitotic entry: Non-genetic heterogeneity exposes the requirement for Plk1 [Aspinall CF, et al. Oncotarget, 2015, 6(34):36472-88] | PubMed: 26472023 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.