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CAS No. : 1000023-05-1
MCE 国际站:Voruciclib hydrochloride
产品活性:Voruciclib hydrochloride 是一种具有口服活性和选择性 CDK 抑制剂,Ki 为 0.626 nM-9.1 nM。Voruciclib hydrochloride 可以有效阻断 MCL-1 的转录调节子 CDK9。Voruciclib hydrochloride 抑制多种弥漫性大 B 细胞淋巴瘤 (DLBCL) 模型中 MCL-1 的表达。
研究领域:Cell Cycle/DNA Damage
作用靶点:CDK
In Vitro: Voruciclib hydrochloride (0.5-5 µM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes.
Ki values for each target such as CDK9/cyc T2, CDK9/cyc T1, CDK6/cyc D1, CDK4/cyc D1, CDK1/cyc B, and CDK1/cyc A for Voruciclib hydrochloride are 0.626 nM, 1.68 nM, 2.92 nM, 3.96 nM, 5.4 nM, 9.1 nM, respectively.
In Vivo: Combination of Voruciclib hydrochloride (200 mpk; Oral gavage) and Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) leads to enhance tumor growth inhibition compared to either drug alone in U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), and NU-DHL-1 models (five days per week for 3 weeks) of DLBCL.
相关产品:Natural Product-like Compound Library | Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Orally Active Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | SY-5609 | CLK1/2-IN-1 | MFH290 | SB-218078 | Toyocamycin | (S)-LY3177833 hydrate | Dinaciclib | EGFR/HER2/CDK9-IN-2 | CDK8-IN-11 | SNS-032 | M2N12 | Palbociclib-d8 | EGFR/CDK2-IN-1 | BSJ-04-132 | (E/Z)-Zotiraciclib | CCT-251921 | BS-181 | Ribociclib-d8 | CDK9-IN-9 | Flavopiridol | SRI-29329 | dCeMM4 | GSK 3 Inhibitor IX | CDK9-IN-7 | PROTAC CDK9 degrader-8 | BSJ-03-204 | Amantadine-d6 | K00546 | Abemaciclib metabolite M18 hydrochloride | Ribociclib-d6
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