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Voruciclib hydrochloride

CAS No. : 1000023-05-1

產(chǎn)品活性：Voruciclib hydrochloride is an orally active and selective CDK inhibitor with K_i values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).

研究領(lǐng)域：Cell Cycle/DNA Damage

作用靶點：CDK

In Vitro: Voruciclib hydrochloride (0.5-5 µM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes.
K_i 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.

相關(guān)產(chǎn)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  |  SY-5609  |  CLK1/2-IN-1  |  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  |  BSJ-03-204  |  Amantadine-d₆  |  K00546  |  Abemaciclib metabolite M18 hydrochloride  |  Ribociclib-d₆  |  Lacto-N-fucopentaose I  |  CDK2/4/6-IN-2

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