| Bioactivity | R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively[1][2][3][4][5]. | ||||||||||||
| Invitro | R547 effectively inhibits CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclin D1 (Ki = 1–3 nmol/L) and is inactive (Ki > 5,000 nmol/L) against a panel of >120 unrelated kinases in cell-free assays[4].R547 effectively inhibits the proliferation of tumor cell lines independent of multidrug resistant status, histologic type, retinoblastoma protein, or p53 status, with IC50s <0.60 μM[4].R547 reduces phosphorylation of the cellular retinoblastoma protein at specific CDK phosphorylation sites at the same concentrations that induced cell cycle arrest[4].R547 has anti-proliferative activity in tumor cells independent of p53, retinoblastoma, or MDR status[4].R547 blocks tumor cells in G1 plus G2 and induces apoptosis[4].R547 induces apoptosis as measured by DNA fragmentation[4].R547 inhibits phosphorylation of retinoblastoma protein in humantumor cells[4]. Cell Cytotoxicity Assay[4] Cell Line: | ||||||||||||
| Name | R547 | ||||||||||||
| CAS | 741713-40-6 | ||||||||||||
| Formula | C18H21F2N5O4S | ||||||||||||
| Molar Mass | 441.45 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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