Size | Price | Stock |
---|---|---|
5mg | $134 | In-stock |
10mg | $209 | In-stock |
50mg | $770 | In-stock |
100 mg | Get quote | |
200 mg | Get quote | |
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Cat. No. : | HY-10014 |
M.Wt: | 441.45 |
Formula: | C18H21F2N5O4S |
Purity: | >98 % |
Solubility: | 10 mM in DMSO |
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].
In Vitro: 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].
In Vivo: R547 has significant in vivo efficacy with daily oral and once weekly i.v. dosing[4].
R547 inhibits phosphorylation of retinoblastoma protein in tumors[4].
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