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BAVDEGALUTAMIDE

BAVDEGALUTAMIDE : Degrader (PROTAC) of AR

Structure

Information

  • AR (Mutant:WT, F877L, T878A, M896V, and H875Y)
  • Degrader (PROTAC)
  • up to 30 nM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Cell:
In the MCF-7 breast cancer cell line, bavdegalutamide treatment (30–300 nmol/L) resulted in the degradation of AR but not GR, another nuclear hormone receptor that is closely related to AR.
Potency assay, off target (cells): Unbiased proteomic screen of nearly 4,000 detectable proteins in VCaP cells showed that treatment with 10 nmol/L bavdegalutamide for 8 hours led to degradation of only AR when a filter of >2× degradation and a P value of <0.05 were applied
Probe Selectivity in Cell:
Treatment of Ramos cells with increasing concentrations of bavdegalutamide did not lead to degradation of G1–S phase transition 1 protein, IKZF3 (Aiolos), or IKZF1 (Ikaros), and only modest degradation of CK1α was observed at 300 to 1,000 nmol/L. In SK-N-DZ cells, SALL4 was modestly degraded at 1,000 nmol/L. Given that the in vitro functional efficacy of bavdegalutamide is in the range of 1 to 30 nmol/L, these data demonstrate at least a 10× window between AR and CK1α and SALL4 modulations.
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SERP ratings and comments

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