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YJ1206
🥰Excellent
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
🥰Excellent
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 Size | Price | Availability | 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 |
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Purity:97.14%
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Product Introduction
Bioactivity
Chemical Properties
| 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 & Solubility Information
| 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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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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