Apoptone

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WARNING: This product is for research use only, not for human or veterinary use.

Description:Apoptone, also known as 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.

Price and Availability

Apoptone (HE-3235), purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide).

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 205485Name: ApoptoneCAS#: 183387-50-0Chemical Formula: C21H32O2Exact Mass: 316.24023Molecular Weight: 316.47758Elemental Analysis:C, 79.70; H, 10.19; O, 10.11

Synonym:HE3235, HE-3235, HE3235, Apotone

IUPAC/Chemical Name:(3R,5S,8R,9S,10S,13S,14S,17R)-17-ethynyl-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthrene-3,17-diol

InChi Key:CKAXZOYFIHQCBN-JRRMKBMNSA-N

InChi Code:InChI=1S/C21H32O2/c1-4-21(23)12-9-18-16-6-5-14-13-15(22)7-10-19(14,2)17(16)8-11-20(18,21)3/h1,14-18,22-23H,5-13H2,2-3H3/t14-,15+,16+,17-,18-,19-,20-,21-/m0/s1

SMILES Code:O[C@@H]1CC[C@]2(C)[C@@]3([H])CC[C@]4(C)[C@](O)(C#C)CC[C@@]4([H])[C@]3([H])CC[C@@]2([H])C1

Technical Data

Additional Information

HE3235 is a n 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.  

References

1: Koreckij TD, Trauger RJ, Montgomery RB, Pitts TE,Coleman I, Nguyen H, Reading CL, Nelson PS, Vessella RL, Corey E. HE3235inhibits growth of castration-resistant prostate cancer. Neoplasia. 2009Nov;11(11):1216-25. PubMed  PMID: 19881957; PubMed Central PMCID:PMC2767223.