WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205485
CAS#: 183387-50-0
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.
MedKoo Cat#: 205485
Name: Apoptone
CAS#: 183387-50-0
Chemical Formula: C21H32O2
Exact Mass: 316.24023
Molecular Weight: 316.47758
Elemental Analysis: C, 79.70; H, 10.19; O, 10.11
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).
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
The following data is based on the product molecular weight 316.47758 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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.
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.