Chemical Structure : AU-24118
货号: PC-22055Not For Human Use, Lab Use Only.
AU-24118 is a potent, selective, and orally bioavailable degrader of mSWI/SNF ATPases (SMARCA2, SMARCA4) and PBRM1.
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AU-24118 is a potent, selective, and orally bioavailable degrader of mSWI/SNF ATPases (SMARCA2, SMARCA4) and PBRM1.
AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase.
AU-24118 selectively degraded SMARCA2, SMARCA4, and PBRM1 in VCaP prostate cancer cells, through the CRBN-based proteasomal degradation machinery.
AU-24118 induces tumor regression as a single agent, as well as in combination with enzalutamide, in a VCaP CRPC model.
has increased efficacy compared to AU-15330 in terms of both target degradation efficiency as well as potency in vivo.
分子量 | 632.77 | |
分子式 | C37H40N6O4 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Tongchen He, et al. bioRxiv. [Preprint]. 2024 Mar 2:2024.02.29.582768.
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