Galeterone (TOK-001) 是一种口服有效的分子胶降解剂,能降解雄激素受体（AR）及其剪接变体（AR-Vs）和激酶Mnk1/2,并兼具CYP17抑制活性。它可诱导细胞凋亡、抑制肿瘤生长,用于去势抵抗性前列腺癌（CRPC）和胰腺导管腺癌（PDAC）的研究。
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英文别名 (English Synonym) |
TOK-001 |
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中文名称 (Chinese Name) |
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靶点 (Target) |
Androgen Receptor |
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通路 (Pathway) |
Endocrinology and Hormones |
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CAS号 (CAS NO.) |
851983-85-2 |
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分子式 (Formula) |
C26H32N2O |
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分子量 (Molecular Weight) |
388.56 |
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纯度 (Purity) |
≥98% |
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溶解性 (Solubility) |
溶于DMSO |
-25~-15℃保存，有效期3年
[1] Thankan RS, Thomas E, Purushottamachar P, Weber DJ, Njar VCO. Salinization Dramatically Enhance the Anti-Prostate Cancer Efficacies of AR/AR-V7 and Mnk1/2 Molecular Glue Degraders, Galeterone and VNPP433-3β Which Outperform Docetaxel and Enzalutamide in CRPC CWR22Rv1 Xenograft Mouse Model. Bioorg Chem. 2023 Oct,139:106700. doi: 10.1016/j.bioorg.2023.106700. Epub 2023 Jun 25. PMID: 37392559, PMCID: PMC10528634.[2]Bruno RD, Vasaitis TS, Gediya LK, Purushottamachar P, Godbole AM, Ates-Alagoz Z, Brodie AM, Njar VC. Synthesis and biological evaluations of putative metabolically stable analogs of VN/124-1 (TOK-001): head to head anti-tumor efficacy evaluation of VN/124-1 (TOK-001) and abiraterone in LAPC-4 human prostate cancer xenograft model. Steroids. 2011 Nov,76(12):1268-79. doi: 10.1016/j.steroids.2011.06.002. Epub 2011 Jun 24. PMID: 21729712, PMCID: PMC3171567.
