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YJ1206

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Catalog No. T200845Cas No. 3053716-98-3
Alias YJ 1206

YJ1206 is a highly potent and selective CDK12/13 PROTAC degrader (IC50 =12.55 nM) with the advantages of oral administration and low toxicity, which triggers gene-length-dependent transcription elongation defects, leading to DNA damage and cell-cycle arrest, and inhibits the proliferation of a subpopulation of prostate cancer cells. YJ1206 can synergize with AKT pathway inhibitors to effectively inhibit prostate cancer.

YJ1206

YJ1206

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Purity: 97.14%
Catalog No. T200845Alias YJ 1206Cas No. 3053716-98-3
YJ1206 is a highly potent and selective CDK12/13 PROTAC degrader (IC50 =12.55 nM) with the advantages of oral administration and low toxicity, which triggers gene-length-dependent transcription elongation defects, leading to DNA damage and cell-cycle arrest, and inhibits the proliferation of a subpopulation of prostate cancer cells. YJ1206 can synergize with AKT pathway inhibitors to effectively inhibit prostate cancer.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$42-In Stock
5 mg$93-In Stock
10 mg$133-In Stock
25 mg$223-In Stock
50 mg$392-In Stock
100 mg$668-In 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:97.14%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
YJ1206 is a highly potent and selective CDK12/13 PROTAC degrader (IC50 =12.55 nM) with the advantages of oral administration and low toxicity, which triggers gene-length-dependent transcription elongation defects, leading to DNA damage and cell-cycle arrest, and inhibits the proliferation of a subpopulation of prostate cancer cells. YJ1206 can synergize with AKT pathway inhibitors to effectively inhibit prostate cancer.
Targets&IC50
CDK12/13 (VCaP prostate cancer cells):12.55  nM
In vitro
VCaP and 22Rv1 prostate cancer cells were treated with YJ1206 at concentrations ranging from 0 to 500 nM for 4 to 15 hours. Experiments included Western blot, RNA-seq, proteomics, and qPCR to evaluate degradation of CDK12/13 and downstream effects. YJ1206 showed an IC₅₀ of 12.55 nM in VCaP cells and exhibited potent antiproliferative activity[1].
In vivo
In CD-1 immunocompetent mice bearing VCaP-CRPC, WA74 PDX, or PC310 PDX prostate tumor xenografts, YJ1206 was administered orally at 100 mg/kg, 3 times per week, for up to 21 days. Tumor samples were analyzed by Western blot, H&E staining, IHC, and TUNEL assays. YJ1206 significantly suppressed tumor growth with minimal observed toxicity[1].
SynonymsYJ 1206
Chemical Properties
Molecular Weight894.01
FormulaC49H52FN11O5
Cas No.3053716-98-3
SmilesO=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC(F)=C(C2)N4CCC(CC4)N5CCN(CC5)C6=CC=C(N(C(NCC7=CC=CC=C7)=O)[C@@H]8CC[C@@H](NC9=NC%10=C(C=N9)C=CC=C%10)CC8)C=N6
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: 50 mg/mL (55.93 mM), Sonication and heating are recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.1186 mL5.5928 mL11.1856 mL55.9278 mL
5 mM0.2237 mL1.1186 mL2.2371 mL11.1856 mL
10 mM0.1119 mL0.5593 mL1.1186 mL5.5928 mL
20 mM0.0559 mL0.2796 mL0.5593 mL2.7964 mL
50 mM0.0224 mL0.1119 mL0.2237 mL1.1186 mL

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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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