Voruciclib |
| カタログ番号GC45983 |
ボルシクリブは、Ki 値が 0.626 nM ～ 9.1 nM の経口活性および選択的 CDK 阻害剤です。 Voruciclib は、MCL-1 の転写調節因子である CDK9 を強力にブロックします。ボルシクリブは、びまん性大細胞型B細胞リンパ腫（DLBCL）の複数のモデルでMCL-1の発現を抑制します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1000023-04-0
Sample solution is provided at 25 µL, 10mM.
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Voruciclib is a pan-inhibitor of cyclin-dependent kinases (CDKs; Kis = 0.626-9.1 nM).1 It is selective for CDKs over male germ cell associated kinase (MAK) and intestinal cell kinase (ICK; Kis = 259 and 481 nM, respectively), in a panel of 48 kinases. Voruciclib decreases myeloid cell leukemia-1 (Mcl-1) levels and increases cleaved poly(ADP-ribose) polymerase (PARP) levels in six diffuse large B-cell lymphoma (DLBCL) cell lines when used at concentrations ranging from 0.5 to 5 μM. It reduces tumor growth by 56.3% in a Ri-1 mouse xenograft model when administered at a dose of 200 mg/kg.
|1. Dey, J., Deckwerth, T.L., Kerwin, W.S., et al. Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk diffuse large B-cell lymphoma to BCL2 inhibition. Sci. Rep. 7(1), 18007 (2017).
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