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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 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 |
| 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]. |
| Synonyms | YJ 1206 |
| Molecular Weight | 894.01 |
| Formula | C49H52FN11O5 |
| Cas No. | 3053716-98-3 |
| Smiles | O=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 | store 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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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