1. Cell Cycle/DNA Damage
  2. CDK
  3. Voruciclib

Voruciclib 

Cat. No.: HY-12422 Purity: 99.52% ee.: 99.80%
Handling Instructions

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

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Voruciclib Chemical Structure

Voruciclib Chemical Structure

CAS No. : 1000023-04-0

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10 mM * 1  mL in DMSO USD 569 In-stock
Estimated Time of Arrival: December 31
1 mg USD 280 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Voruciclib is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL)[1].

IC50 & Target[1]

CDK9/cyc T2

0.626 nM (Ki)

CDK9/CycT1

1.68 nM (Ki)

CDK6/cycD1

2.92 nM (Ki)

CDK4/Cyc D1

3.96 nM (Ki)

CDK1/cycB

5.4 nM (Ki)

CDK1/cyc A

9.1 nM (Ki)

In Vitro

Voruciclib (0.5-5 µM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes[1].
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[1].

Cell Viability Assay[1]

Cell Line: U2932, RIVA, OCI-LY10 cells (ABC subtype), NU-DHL-1, SU-DHL-4, SU-DHL-6 cells (GCB subtype)
Concentration: 0.5 µM, 1 µM, 2 µM, 3 µM, 4 µM, 5 µM
Incubation Time: 6 hours
Result: Showed targeted downregulation of MCL-1 in both ABC and GCB subtypes.
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[1].

Animal Model: ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice
Dosage: 200 mpk
Administration: Oral gavage; U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), OCI-LY10 (six days per week for 2 weeks), NU-DHL-1 (five days per week for 3 weeks)
Result: Enhanced tumor growth inhibition in U2932, RIVA, SU-DHL-4 and NU-DHL-1 models except in OCI-LY10 model.
Clinical Trial
Molecular Weight

469.84

Formula

C₂₂H₁₉ClF₃NO₅

CAS No.

1000023-04-0

SMILES

O=C1C=C(C2=CC=C(C(F)(F)F)C=C2Cl)OC3=C([[email protected]]4[[email protected]](CO)N(C)CC4)C(O)=CC(O)=C13

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (266.05 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1284 mL 10.6419 mL 21.2838 mL
5 mM 0.4257 mL 2.1284 mL 4.2568 mL
10 mM 0.2128 mL 1.0642 mL 2.1284 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

VoruciclibCDKCyclin dependent kinaseclinicalstageorallyCDK9MCL-1multiplemodelsdiffuselargeB-celllymphomaDLBCLInhibitorinhibitorinhibit

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