VZ185 |
| Catalog No.GC65135 |
VZ185는 각각 4.5 및 1.8nM의 DC50을 갖는 BRD9 및 BRD7의 강력하고 빠르며 선택적인 von Hippel-Lindau 기반 이중 분해자 프로브입니다. VZ185는 EOL-1 및 A-402 세포에서 세포독성이며 EC50은 각각 3nM 및 40nM입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2306193-61-1
Sample solution is provided at 25 µL, 10mM.
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VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively[1].
Degradation analysis in a panel of other human cancer cell lines (EOL-1, A-204) confirms the potency of VZ185 (DC50 between 2 and 8 nM for BRD9). In vitro PK data further showed high stabilities of VZ185 in both plasma and microsomes from both human and mouse species, as well as high aqueous kinetic solubility (up to ~100 μM)[1].
[1]. Zoppi V, et al. Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7. J Med Chem. 2019 Jan 24;62(2):699-726.
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