3049076-98-1
Chemical Structure
YX-02-030
- CAS No.: 3049076-98-1
- Formula:C66H85Cl2N9O10S
- Molecular Weight:1267.41
InChIKey: FRCCOJQMSWWHQP-QOWPVYDQSA-N
SMILES: O=C(CN1CCN(C(N2[C@](C)(C3=CC=C(Cl)C=C3)[C@](C)(C4=CC=C(Cl)C=C4)N=C2C5=CC=C(C(C)(C)C)C=C5OCC)=O)CC1)NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O
Biological Activity: YX-02-030 is a VHL-dependent MDM2 PROTAC degrader with a Kd of 35 nM. YX-02-030 recruits the VHL E3 ligase to form a ternary complex, leading to ubiquitination and proteasome-mediated degradation of MDM2. YX-02-030 inhibits MDM2-p53 and VHL-HIF1α binding with IC50 values of 63 and 1350 nM. YX-02-030 activates TAp73, upregulates p53 family target genes and induces apoptosis. YX-02-030 demonstrates on-target efficacy in TNBC xenograft-bearing mice, extending survival without normal cell toxicity[1].
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YX-02-030 | 99.86% | YX-02-030 is a VHL-dependent MDM2 PROTAC degrader with a Kd of 35 nM. YX-02-030 recruits the VHL E3 ligase to form a ternary complex, leading to ubiquitination and proteasome-mediated degradation of MDM2. YX-02-030 inhibits MDM2-p53 and VHL-HIF1α binding with IC50 values of 63 and 1350 nM. YX-02-030 activates TAp73, upregulates p53 family target genes and induces apoptosis. YX-02-030 demonstrates on-target efficacy in TNBC xenograft-bearing mice, extending survival without normal cell toxicity. | ||||||||||||||||||||
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Keywords
