Voruciclib

SKU: orb1310062

Description

Voruciclib is a potent and selective orally bioavailable CDK inhibitor, with particular activity against CDK9 (Ki values 0.626-9.1 nM). It suppresses MCL-1 expression and has demonstrated efficacy in both in vitro and in vivo models of diffuse large B-cell lymphoma (DLBCL).

Research Area

Cell Biology

Key Properties

• CAS Number: 1000023-04-0
• MW: 469.84
• Purity: 99.99%
• Formula: C₂₂H₁₉ClF₃NO₅
• SMILES: CN1CC[C@H]([C@@H]1CO)c1c(O)cc(O)c2c1oc(cc2=O)-c1ccc(cc1Cl)C(F)(F)F
• Target: CDK
• Solubility: DMSO:42.5 mg/mL (90.46 mM)

Bioactivity

• Target IC50:
  CDK1-CyclinA:9.1 nM(Ki)|CDK1-CyclinB:5.4 nM(Ki)|CDK9-CyclinT1:1.68 nM(Ki)|CDK4-CyclinD1:3.96 nM(Ki)|CDK6-CyclinD1:2.92 nM(Ki)|CDK9-CyclinT2:0.626 nM(Ki)
• In Vivo:
  In ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice, Combination of 200 mpk Voruciclib hydrochloride and Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) causes increase tumor growth inhibition compared to either drug alone in U2932, RIVA, SU-DHL-4, and NU-DHL-1 models of DLBCL .
• In Vitro:
  Voruciclib hydrochloride has Ki values for CDK inhibitor such as CDK9/cyc T2 of 0.626 nM, CDK9/cyc T1 of 1.68 nM, CDK6/cyc D1 of 2.92 nM, CDK4/cyc D1 of 3.96 nM, CDK1/cyc B of 5.4 nM, and CDK1/cyc A of 9.1 nM.Voruciclib (0.5-5 μM; 6 hours) displays targeted downregulation of MCL-1 in both ABC and GCB subtypes.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, MCL-1, large, multiple, inhibit, orally, models, lymphoma, B-cell, clinical, CDK1/cyc A, CDK1/cycB, CDK1/CyclinB, CDK, CDK9, CDK9/cyc T2, CDK9/CycT1, CDK9/CycT2, CDK4/Cyc D1, CDK6/cycD1, Cyclin dependent kinase, DLBCL, diffuse, stage, Voruciclib

Compound Identifiers

PubChem CID

67409219