RGB-286638
RGB-286638 is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.
RGB-286638 inhibited several tyrosine and serine/threonine non-CDK enzymes, i.e. GSK-3, TAK1, AMPK, Jak2, MEK1. RGB-286638 demonstrated equimolar (50nM) activity in freshly isolated tumor cells from MM patients, while manifesting less cytotoxicity in healthy donor PBMCs. Treatment with RGB-286638 resulted in rapid downregulation of p-RNAPII S2/S5 across all tested MM cell lines. RGB-286638 (50nM) reduced the phosphorylation of Rb at S807/811 in MM.1S and MM.1R cells, but had no effects on p-Rb S780.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | RGB-286638 |
|---|---|
| Iupac 化学名称 | RGB-286638 |
| 同义词 | RGB286638 |
| 英文同义词 | RGB286638 |
| 分子式 | C29H37Cl2N7O4 |
| 分子量 | 618.55 |
| Smile | COCCN1CCN(CC1)Cc2ccc(cc2)c3c4c([nH]n3)-c5cccc(c5C4=O)NC(=O)NN6CCOCC6 |
| InChiKey | XLSYZSRXVVCHLS-UHFFFAOYSA-N |
| InChi | InChI=1S/C29H35N7O4/c1-39-16-13-34-9-11-35(12-10-34)19-20-5-7-21(8-6-20)26-25-27(32-31-26)22-3-2-4-23(24(22)28(25)37)30-29(38)33-36-14-17-40-18-15-36/h2-8H,9-19H2,1H3,(H,31,32)(H2,30,33,38) |
| Cas号 | 784210-87-3 |
| MDL | MFCD18633230 |
| 相关CAS号 |
订购信息
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