SMARCA2 PROTAC YD23

Chemical Structure : SMARCA2 PROTAC YD23

CAS No.: 2951015-29-3

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货号: PC-23133Not For Human Use, Lab Use Only.

SMARCA2 PROTAC YD23 is a potent and selective proteolysis targeting chimera (PROTAC) targeting SMARCA2 with DC50 of 64 nM in H1792 cells and Dmax of 88%.

规格	价格	库存
2 mg	￥3580	In stock
5 mg	￥5580	In stock
10 mg	￥8980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

SMARCA2 PROTAC YD23 is a potent and selective proteolysis targeting chimera (PROTAC) targeting SMARCA2 with DC50 of 64 nM in H1792 cells and Dmax of 88%.
YD23 selectively degrades SMARCA2 and inhibits the growth of SMARCA4-mutant lung cancer cell lines.
YD23 exhibits DC50 of 297 nM and a Dmax of 95% in H1975 SMARCA4-WT cells, minimal impact on SMARCA4 up to 10 μM.
YD23 potently degraded SMARCA2 with a median DC50 of 92.8 nM and achieving a Dmax of 90% on an additional panel of ten SMARCA4-WT cell lines.
YD23 selectively inhibits growth of SMARCA4-mutant lung cancer cell lines with IC50 of 0.11 uM (SMARCA4-WT cells, IC50=6 uM).
SMARCA2 degradation disrupts chromatin accessibility at enhancers to disable cell cycle transcriptional programs.
YD23 (12.5 mg/kg) inhibits growth of SMARCA4-mutant xenograft models of lung cancer.

物理化学性质&存储条件

分子量	738.78
分子式	C38H39FN8O7
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	4-((2-(2-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)-2-fluorophenoxy)ethoxy)ethyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

参考文献

1. Kotagiri S, et al. Cell Chem Biol. 2024 Oct 1:S2451-9456(24)00396-9.