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Voruciclib

Voruciclib
Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM) that represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma and effectively blocks CDK9, the transcriptional regulator of MCL-1.
Catalog No. T10096LCas No. 1000023-04-0
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Purity:99.89%
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Voruciclib

Catalog No. T10096LCas No. 1000023-04-0
Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM) that represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma and effectively blocks CDK9, the transcriptional regulator of MCL-1.
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Pack SizePriceAvailabilityQuantity
1 mg$147In Stock
5 mg$289In Stock
10 mg$455In Stock
25 mg$889In Stock
1 mL x 10 mM (in DMSO)$298In Stock
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Product Introduction

Bioactivity
Description
Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM) that represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma and effectively blocks CDK9, the transcriptional regulator of MCL-1.
Targets&IC50
CDK6-CyclinD1:2.92 nM(Ki), CDK9-CyclinT2:0.626 nM(Ki), CDK1-CyclinB:5.4 nM(Ki), CDK4-CyclinD1:3.96 nM(Ki), CDK9-CyclinT1:1.68 nM(Ki), CDK1-CyclinA:9.1 nM(Ki)
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[1].Voruciclib (0.5-5 μM; 6 hours) displays targeted downregulation of MCL-1 in both ABC and GCB subtypes[1].
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 [1].
Chemical Properties
Molecular Weight469.84
FormulaC22H19ClF3NO5
Cas No.1000023-04-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 42.5 mg/mL (90.46 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1284 mL10.6419 mL21.2838 mL106.4192 mL
5 mM0.4257 mL2.1284 mL4.2568 mL21.2838 mL
10 mM0.2128 mL1.0642 mL2.1284 mL10.6419 mL
20 mM0.1064 mL0.5321 mL1.0642 mL5.3210 mL
50 mM0.0426 mL0.2128 mL0.4257 mL2.1284 mL

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