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HE-3235 (Synonyms: Apoptone,17α-Ethynyl-5α-androstane-3α,17ß-diol)

Catalog No.GC14221

HE-3235, synthetic analogue of 3β-androstanediol, is an orally bioavailable anticancer agent. HE-3235 is active in rodent models of prostate and breast cancer.

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HE-3235 Chemical Structure

Cas No.: 183387-50-0

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1mg
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5mg
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10mg
$342.00
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25mg
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Sample solution is provided at 25 µL, 10mM.

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Background

HE-3235 is a novel antagonist of androgen receptor.

Androgen receptor (AR) is an adrenal hormone belongs to the steroid hormone receptor family of molecules. AR is responsible for mediating the physiologic effects of androgens by binding to specific DNA sequences that influence transcription of androgen-responsive genes. Variations in the AR gene may lead to genetic predisposition to prostate cancer development and severity [2].

In vitro: In LNCaP cells expressing a mutated androgen receptor, HE3235 significantly inhibited activity for AED-stimulated LNCaP proliferation. This inhibitory activity is accompanied by an increase in the number of apoptotic cells [1].

In vivo: Animal studies have confirmed the cytoreductive activity of HE3235 on LNCaP tumours. The results suggest that this compound may be of clinical use in castration-resistant prostate cancer. In castrated male mice implanted subcutaneously with LuCaP35V CaP xenografts, treatment with HE3235 significantly prolonged the tumor doubling time of LuCaP35V, decreased androgen receptor expression, and lowered levels of intratumoral testosterone by 89% and dihydrotestosterone by 63% in both the presence and the absence of AED. HE3235 inhibited tumor growth in the bone environment. HE3235 inhibited the growth of subcutaneous CRPC as well as CRPC in the bone environment. HE3235 exhibited a wide range of effects, including alteration of androgen receptor signaling and reductions in levels of intratumoral androgens. Weights of tumored tibiae of HE3235-treated animals were lower than those of control [3].

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)[J]. British journal of cancer, 2009, 100(7): 1068-1072.
[2] Gelmann E P.  Molecular biology of the androgen receptor[J]. Journal of Clinical Oncology, 2002, 20(13): 3001-3015.
[3 Gelmann E P.  Molecular biology of the androgen receptor[J]. Journal of Clinical Oncology, 2002, 20(13): 3001-3015.] Koreckij T D, Trauger R J, Montgomery R B, et al. HE3235 inhibits growth of castration-resistant prostate cancer[J]. Neoplasia, 2009, 11(11): 1216IN22-1225IN23.

Chemical Properties

Cas No. 183387-50-0 SDF
Synonyms Apoptone,17α-Ethynyl-5α-androstane-3α,17ß-diol
Chemical Name (3α,5α,17α)-pregn-20-yne-3,17-diol
Canonical SMILES 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
Formula C21H32O2 M.Wt 316.5
Solubility ≤10mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.1596 mL 15.7978 mL 31.5956 mL
5 mM 0.6319 mL 3.1596 mL 6.3191 mL
10 mM 0.316 mL 1.5798 mL 3.1596 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

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