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Voruciclib

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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.

Voruciclib

Voruciclib

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Purity: 99.99%
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.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$147In StockIn Stock
5 mg$289-In Stock
10 mg$455-In Stock
25 mg$889-In Stock
1 mL x 10 mM (in DMSO)$298-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.99%
Appearance:Solid
Color:Yellow
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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
SmilesCN1CC[C@H]([C@@H]1CO)c1c(O)cc(O)c2c1oc(cc2=O)-c1ccc(cc1Cl)C(F)(F)F
Relative Density.1.493 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 42.5 mg/mL (90.46 mM), Sonication is recommended.
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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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
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