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首页-抗体药物偶连体和PROTACs-PROTAC-YDR1
YDR1

Chemical Structure : YDR1

CAS No.: 2951015-31-7

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YDR1

货号: PC-24492Not For Human Use, Lab Use Only.

YDR1 is potent, selective, and orally bioavailable SMARCA2 degrading PROTAC with DC50 of 6.3 nM (H322 cell ine), Dmax=99.4%, selectively inhibit gowth of SMARCA4 mutant lung cancer cell lines.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

YDR1 is potent, selective, and orally bioavailable SMARCA2 degrading PROTAC with DC50 of 6.3 nM (H322 cell ine), Dmax=99.4%, selectively inhibit gowth of SMARCA4 mutant lung cancer cell lines.
YDR1 potently degrades SMARCA2 in H322, HCC515, H2030, and H2126 cell lines with DC50 of 6.4 nM, 10.6 nM, 12.7 nM and 1.2 nM respectively, while achieving profound maximal degradation (Dmax) of 99.2%, 99.4%, 98.7% and 99.6% respectively.
YDR1 induces degradation of SMARCA2 in the classically accepted PROTAC fashion by E3 ligase-target protein-PROTAC ternary complex formation, ubiquitination, and via the proteasome.
YDR1 dose-dependently inhibits SMARCA4 mutant cell lines (H1568 and H1693) with average cellular IC50 of 78 nM respectively in clonogenic assays, with minimal impact on the growth of SMARCA4 WT cell lines.
YDR1 (40m/kg, oral gavage daily) moderately inhibited tumor growth in SMARCA4 mutant xenograft models of lung cancer.
YDR1 synergizes with sotorasib to inhibit growth of sotorasib-resistant KRASG12and SMARCA4 comutant cancer cells.

物理化学性质&存储条件

分子量 816.94
分子式 C44H49FN10O5
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

1H-Isoindole-1,3(2H)-dione, 5-[4-[[1-[4-[[4-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-1-piperazinyl]methyl]-2-fluorophenyl]-4-piperidinyl]methyl]-1-piperazinyl]-2-(2,6-dioxo-3-piperidinyl)-

参考文献

1. Kotagiri S, et al. J Med Chem. 2025 Apr 25. doi: 10.1021/acs.jmedchem.4c02577.

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