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Chemical Structure : Bavdegalutamide
CAS No.: 2222112-77-6
Catalog No.: PC-38047Not For Human Use, Lab Use Only.
Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR with DC50 of <1 nM.
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|---|---|---|---|
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | $528 | In stock | |
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Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR with DC50 of <1 nM.
At the dose of 0.01 nM-300 nM, ARV-110 leads to AR degradation in LNCaP cells in a dose-dependent manner.
In VCaP cells, ARV-110 leads to AR degradation in a time-dependent manner.
ARV-110 suppresses the expression of the AR-target gene PSA. ARV-110 inhibits AR-dependent cell proliferation and induces apoptosis at low nanomolar concentrations.
ARV-110 degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V, and H874V). retains activity even in a high androgen environment (R1881, 100 nM) in VCaP cells.
ARV-110 exhibits a greater than 90% AR degradation in LNCaP, VCaP, and prostate cancer PDX models.
ARV-110 exhibits significant inhibition of tumor growth and AR signaling in vivo.
| M.Wt | 812.3 | |
| Formula | C41H43ClFN9O6 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-((1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl)-6-(4-((4-(2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindolin-5-yl)piperazin-1-yl)methyl)piperidin-1-yl)pyridazine-3-carboxamide |
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1. Cancer Discov. 2020 Aug;10(8):1084.
2. Qi SM, et al. Front Pharmacol. 2021 May 7;12:692574.
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