VZ185 是高效，快速，选择性的基于von Hippel-Lindau的BRD9和BRD7双降解探针，DC50 分别为 4.5 和 1.8 nM。VZ185对 EOL-1 和 A-402 细胞具有细胞毒性，EC50 分别为 3nM 和 40nM。
货号:ajcx38984
CAS:2306193-61-1
分子式:C53H67FN8O8S
分子量：995.21
溶解度:DMSO : 200 mg/mL (200.96 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.

Protocol:

BRD7 4.5nM(DC50)

BRD9 1.8nM(DC50)