2951015-29-3
Chemical Structure
YD23
- CAS No.: 2951015-29-3
- Formula:C38H39FN8O7
- Molecular Weight:738.76
IUPAC Name: 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
InChIKey: DMUYROJVOXZRNE-UHFFFAOYSA-N
SMILES: O=C1N(C2CCC(NC2=O)=O)C(C3=C1C=CC=C3NCCOCCOC4=C(F)C=C(CN5CCN(C6=C(N)N=NC(C7=C(O)C=CC=C7)=C6)CC5)C=C4)=O
Biological Activity: YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC)[1][2].
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YD23 | 98.80% | YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC). | ||||||||||||||||||||
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- [1]. Kotagiri S, et al. Novel SMARCA2 degrading bifunctional molecules as therapeutics in SMARCA4 mutant lung cancer[J]. Cancer Research, 2023, 83(7_Supplement): 1138-1138.
- [2]. Kotagiri S, et al. Enhancer reprogramming by novel SMARCA2 degrading PROTACs underlies therapeutic utility in SMARCA4 mutant tumors[J]. Cancer Research, 2023, 83(7_Supplement): 6289-6289.
Keywords
