HE-3235 (Synonyms: Apoptone,17α-Ethynyl-5α-androstane-3α,17ß-diol) |
Catalog No.GC14221
One-Click Copy Product Info
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HE-3235, analogue synthétique du 3β-androstanediol, est un agent anticancéreux biodisponible par voie orale. HE-3235 est actif dans des modèles rongeurs de cancer de la prostate et du sein.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 183387-50-0
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 183387-50-0 | SDF | |
| Synonymes | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1596 mL | 15.7978 mL | 31.5956 mL |
| 5 mM | 631.9 μL | 3.1596 mL | 6.3191 mL |
| 10 mM | 316 μL | 1.5798 mL | 3.1596 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)