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HE-3235 (CAS 183387-50-0) LS-H164

Androgen receptor antagonist
LS-H164-1 / 1 mg / $175
LS-H164-5 / 5 mg / $235
LS-H164-10 / 10 mg / $305
LS-H164-25 / 25 mg / $465
USA Shipment Only
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Description: HE-3235 is a synthetic adrenal hormone, an androstanediol analog, that acts as an androgen receptor antagonist. In an androgen receptor-dependent manner, it downregulates anti-apoptotic genes, while increasing the expression of pro-apoptotic genes, thus stimulating apoptosis. HE-3235 has been shown to inhibit androstenediol-dependent LNCaP cell tumor growth both in vitro (IC50 = 6 nM) and in xenograft models in vivo. H164_ChemicalStructureImage.png
(3α,5α,17α)-pregn-20-yne-3,17-diol
Apoptone
17α-Ethynyl-5α-androstane-3α,17ß-diol
biochemical, chemical, antagonist
LS-H164
183387-50-0
C21H32O2
≥95%
A crystalline solid
0
C[C@@]12[C@](CC[C@]2(C#C)O)([H])[C@]3([H])CC[C@@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC1
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
CKAXZOYFIHQCBN-JRRMKBMNSA-N
Shipped at 4°C, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: AR / Androgen Receptor related products

Usage Information

HE-3235 is supplied as a crystalline solid. A stock solution may be made by dissolving the HE-3235 in the solvent of choice. HE-3235 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of HE-3235 in these solvents is approximately 10 mg/ml. HE-3235 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, HE-3235 should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. HE-3235 has a solubility of approximately 0.14 mg/ml in a 1:6 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Trauger, R., Corey, E., Bell, D., et al. Inhibition of androstenediol-dependent LNCaP tumour growth by 17α-ethynyl-5α-androstane-3α,17β-diol (HE3235). Br. J. Cancer 100(7), 1068-1072 (2009).
  2. Koreckij, T. D., Trauger, R. J., Montgomery, R. B., et al. HE3235 inhibits growth of castration-resistant prostate cancer. Neoplasia 11(11), 1216-1225 (2009).

 


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