YJ1206 | CDK12/13 PROTAC | Probechem Biochemicals

Chemical Structure : YJ1206

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YJ1206 (YJ-1206)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	867.94
分子式	C47H46FN9O7
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Chang Y, et al. Cell Rep Med. 2024 Sep 21:101752. doi: 10.1016/j.xcrm.2024.101752.

YJ1206 (YJ-1206)

生物&药学活性

物理化学性质&存储条件

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YJ1206 (YJ-1206)

生物&药学活性

物理化学性质&存储条件

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