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DN1679

Catalog No. T217112 Copy Product Info
🥰Excellent
DN1679 is a potent, selective, and orally active CRBN-dependent dual degrader of CDK12/13 PROTAC. It exhibits DC50 values for CDK12/13 at 8.8/9.8 nM in MDA-MB-231 cells, 5.1/6.4 nM in MDA-MB-157 cells, and 17.2/15.8 nM in MDA-MB-468 cells. DN1679 downregulates mRNA levels of DNA damage response genes such as ATM, ATR, BRCA1, and RAD51. When used in combination with Olaparib, DN1679 shows a significant synergistic anti-tumor effect. It is applicable in research on triple-negative breast cancer.

DN1679

Copy Product Info
🥰Excellent
Catalog No. T217112

DN1679 is a potent, selective, and orally active CRBN-dependent dual degrader of CDK12/13 PROTAC. It exhibits DC50 values for CDK12/13 at 8.8/9.8 nM in MDA-MB-231 cells, 5.1/6.4 nM in MDA-MB-157 cells, and 17.2/15.8 nM in MDA-MB-468 cells. DN1679 downregulates mRNA levels of DNA damage response genes such as ATM, ATR, BRCA1, and RAD51. When used in combination with Olaparib, DN1679 shows a significant synergistic anti-tumor effect. It is applicable in research on triple-negative breast cancer.

DN1679
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction

Bioactivity
Description
DN1679 is a potent, selective, and orally active CRBN-dependent dual degrader of CDK12/13 PROTAC. It exhibits DC50 values for CDK12/13 at 8.8/9.8 nM in MDA-MB-231 cells, 5.1/6.4 nM in MDA-MB-157 cells, and 17.2/15.8 nM in MDA-MB-468 cells. DN1679 downregulates mRNA levels of DNA damage response genes such as ATM, ATR, BRCA1, and RAD51. When used in combination with Olaparib, DN1679 shows a significant synergistic anti-tumor effect. It is applicable in research on triple-negative breast cancer.
Targets&IC50
CDK12:8.8 nM (DC50)
In vitro
DN1679 inhibits the proliferation of MDA-MB-231, MDA-MB-157, and MDA-MB-468 cells with IC50 values of 31.7 nM, 49.1 nM, and 121.4 nM, respectively. It exhibits lower cytotoxicity against normal human cell lines (MCF10A and NCM460), with IC50 values of 236.9 nM and 378.5 nM, respectively.
Chemical Properties
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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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.
1 Enter information below:
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