VPC-18005

• CAT Number: I045526
• CAS Number: 2242480-48-2
• Molecular Formula: C15H17N3O3S
• Molecular Weight: 319.38
• Purity: ≥95%
• Synonyms: 2-[(2Z)-4-oxo-2-[(Z)-(4-propan-2-ylphenyl)methylidenehydrazinylidene]-1,3-thiazolidin-5-yl]acetic acid
• InChI: InChI=1S/C15H17N3O3S/c1-9(2)11-5-3-10(4-6-11)8-16-18-15-17-14(21)12(22-15)7-13(19)20/h3-6,8-9,12H,7H2,1-2H3,(H,19,20)(H,17,18,21)/b16-8-
• InChIKey: DTEAZCJUKPARQD-PXNMLYILSA-N
• SMILES: CC(C)C1=CC=C(C=C1)C=NN=C2NC(=O)C(S2)CC(=O)O

VPC-18005 (Cat No.: I045526) is a small-molecule inhibitor designed to target the DNA-binding activity of the androgen receptor (AR), a key driver in prostate cancer progression. Unlike traditional anti-androgens that block ligand binding, VPC-18005 interferes with AR’s interaction with genomic DNA, thereby suppressing transcription of androgen-responsive genes. This novel mechanism offers potential advantages in overcoming resistance to current AR-directed therapies, including castration-resistant prostate cancer. As an experimental therapeutic, VPC-18005 highlights the promise of direct transcriptional disruption in oncology drug development.

Reference

[1]. Miriam S Butler, et al. Discovery and characterization of small molecules targeting the DNA-binding ETS domain of ERG in prostate cancer. Oncotarget. 2017 Jun 27;8(26):42438-42454.
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[2]. Haneen Amawi, et al. The use of zebrafish model in prostate cancer therapeutic development and discovery. Cancer Chemother Pharmacol. 2021 Mar;87(3):311-325.
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