Chemical Structure : YJ1206
CAS No.:
YJ1206
(YJ-1206)
Catalog No.: PC-23149Not For Human Use, Lab Use Only.
YJ1206 is a selective, orally bioavailable CDK12/13 PROTAC degrader, shows potent degradation effects and inhibits VCaP cell viability (IC50=12.5 nM).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
YJ1206 is a selective, orally bioavailable CDK12/13 PROTAC degrader, shows potent degradation effects and inhibits VCaP cell viability (IC50=12.5 nM).
YJ1206 demonstrated the best PK properties, with a bioavailability over 39% by oral gavage.
YJ1206 treatment significantly increased the transcripts at the TSSs in VCaP cells, while a distinct reduction toward the TESs of the long genes ATM and ATR was observed in a time-dependent manner.
YJ1206 combined with AKT inhibitors (uprosertib, capivasertib, and MK2206) triggers a synergistic effect in vitro, The combination regimen of CDK12/13 degraders with AKT inhibitors suppresses tumor growth in vivo.
Physicochemical Properties
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M.Wt
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867.94
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Formula
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C47H46FN9O7
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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3-benzyl-1-(6-(1-(2-((2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindolin-4-yl)oxy)acetyl)piperidin-4-yl)pyridin-3-yl)-1-((1r,4r)-4-(quinazolin-2-ylamino)cyclohexyl)urea
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References
1. Chang Y, et al. Cell Rep Med. 2024 Sep 21:101752. doi: 10.1016/j.xcrm.2024.101752.
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