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MedKoo product information: HE-3235
HE3235 is an orally bioavailable adrenal steroid analogue with potential antineoplastic activity. Androstane steroid HE3235 appears to bind the androgen receptor (AR), down-regulating anti-apoptotic genes, such as Bcl-2, while increasing the expression of pro-apoptotic genes, such as caspases. In vitro and in vivo studies indicate that this agent inhibits androstenediol-dependent LNCaP cell tumor growth. In addition, HE3235 may potentiate chemotherapeutic agents by down-regulating ABCG2, the gene encoding the multi-drug resistant (MDR) protein MDR2. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
Current developer: Harbor Biosciences.
1: Koreckij TD, Trauger RJ, Montgomery RB, Pitts TE, Coleman I, Nguyen H, Reading CL, Nelson PS, Vessella RL, Corey E. HE3235 inhibits growth of castration-resistant prostate cancer. Neoplasia. 2009 Nov;11(11):1216-25. PubMed PMID: 19881957; PubMed Central PMCID: PMC2767223.
2: Trauger R, Corey E, Bell D, White S, Garsd A, Stickney D, Reading C, Frincke J. Inhibition of androstenediol-dependent LNCaP tumour growth by 17alpha-ethynyl-5alpha-androstane-3alpha, 17beta-diol (HE3235). Br J Cancer. 2009 Apr 7;100(7):1068-72. PubMed PMID: 19337256; PubMed Central PMCID: PMC2669987.
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