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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

YJ1206

🥰Excellent
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 SizePriceAvailabilityQuantity
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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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].
AliasYJ 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.
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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