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CDK12-IN-5

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Catalog No. T40290Cas No. 2651200-35-8

CDK12-IN-5 is a potent CDK12 inhibitor with potential anticancer and antitumor activity, and can be used orally in the study of breast and ovarian cancer.

CDK12-IN-5

CDK12-IN-5

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Purity: 99.37%
Catalog No. T40290Cas No. 2651200-35-8
CDK12-IN-5 is a potent CDK12 inhibitor with potential anticancer and antitumor activity, and can be used orally in the study of breast and ovarian cancer.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$168In StockIn Stock
5 mg$419In StockIn Stock
10 mg$679In StockIn Stock
25 mg$1,390In StockIn Stock
50 mg$2,190In StockIn Stock
100 mg$2,970-In Stock
1 mL x 10 mM (in DMSO)$463In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.37%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
CDK12-IN-5 is a potent CDK12 inhibitor with potential anticancer and antitumor activity, and can be used orally in the study of breast and ovarian cancer.
Targets&IC50
CDK12:23.9 nM, CDK9-cyclinT1:127 μM, CDK2-CyclinE:173 μM
In vitro
CDK12-IN-5 (Example 426) selectively suppresses BRCA1 mRNA levels in MDA-MB-231 cells (IC50 = 3.23 nM) without affecting CAL-120 cells. It exhibits antiproliferative effects on both MDA-MB-231 (IC50 = 4.19 nM) and CAL-120 cells (IC50 = 3.57 nM). Additionally, CDK12-IN-5 demonstrates high selectivity for CDK12 inhibition with an IC50 to DC50 CDK12 ratio of 32[1].
Chemical Properties
Molecular Weight454.36
FormulaC18H15F5N8O
Cas No.2651200-35-8
SmilesFC=1C=CC=2N=C(NC2C1F)CNC3=NC(=NC4=C(C=NN34)C(F)(F)F)N5CCOCC5
Relative Density.1.77 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: 100 mg/mL (220.09 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 3.3 mg/mL (7.26 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2009 mL11.0045 mL22.0090 mL110.0449 mL
5 mM0.4402 mL2.2009 mL4.4018 mL22.0090 mL
10 mM0.2201 mL1.1004 mL2.2009 mL11.0045 mL
20 mM0.1100 mL0.5502 mL1.1004 mL5.5022 mL
50 mM0.0440 mL0.2201 mL0.4402 mL2.2009 mL
100 mM0.0220 mL0.1100 mL0.2201 mL1.1004 mL

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In Vivo Formulation Calculator (Clear solution)

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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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