Apoptone
Apoptone (HE3235) is an orally active 3β-androstanediol analog. Apoptone reduces the expression of androgen receptor (Androgen receptor) and decreases intratumoral androgen levels. Apoptone exhibits anticancer activity against castration-resistant prostate cancer.
For research use only. We do not sell to patients.
- CAS No.: 183387-50-0
- Formula: C21H32O2
- Molecular Weight:316.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Apoptone (2 h) binds to recombinant androgen receptor (IC50 1500 nM) and estrogen receptor α (IC50 200 nM)[1].
Apoptone transactivates mutant androgen receptor (EC50 0.48 nM), androgen/glucocorticoid receptor (EC50 11.4 nM), estrogen receptor α/β (EC50 0.8 nM), and estrogen receptor β (EC50 164 nM) in the corresponding transfected cell lines[1].
Apoptone potently inhibits the proliferation of LNCaP prostate cancer cells in vitro, with an EC50 of 6 nM[1].
Apoptone (1-50 nM; 3 d) inhibits the proliferation of castration-resistant prostate cancer C4-2B cells in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Apoptone (160 mg/kg; i.p.; once daily, 5 days/week; 4 weeks) inhibits subcutaneous castration-resistant prostate cancer growth by 43% in castrated male CB-17 SCID mice, with significant reductions in intratumoral androgens, AR mRNA, and nuclear AR localization, alongside transiently elevated serum PSA levels[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB-17 SCID (male; castrated; implanted subcutaneously with ~20 mg LuCaP35V tumor bits)[2]
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Dosage:160 mg/kg
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Administration:i.p.; once daily, 5 days/week; 4 weeks
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Result:Prolonged tumor doubling time to 18.2 ± 6.28 days (control = 10.44 ± 1.8 days; P < .0001), resulting in 43% tumor growth inhibition.
Increased serum PSA levels 1 to 3 weeks after treatment initiation (P < .0001); reached PSA index at sacrifice of 0.18 ± 0.07 ng/mL per cubic millimeter (control = 0.07 ± 0.02 ng/mL per cubic millimeter; P < .0001).
Reduced intratumoral testosterone levels by 93% (0.10 ± 0.05 pg/mg vs control 1.47 ± 0.67 pg/mg; P = .006) and dihydrotestosterone levels by 85% (0.64 ± 0.17 pg/mg vs control 4.28 ± 1.04 pg/mg; P < .0001).
Reduced androgen receptor (AR) mRNA levels by 3.1-fold, and decreased nuclear AR immunoreactivity score to 198 ± 28 (control = 248 ± 8; P = .0048).
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 183387-50-0
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Molecular Weight 316.48
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Formula C21H32O2
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SMILES
O[C@@]1(C#C)CC[C@@]2([H])[C@]3([H])CC[C@@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@@]21C
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Synonyms
HE3235
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Ahlem C, et al. 17α-alkynyl 3α, 17β-androstanediol non-clinical and clinical pharmacology, pharmacokinetics and metabolism. Invest New Drugs. 2012 Feb;30(1):59-78. [Content Brief]
[2]. Koreckij TD, et al. HE3235 inhibits growth of castration-resistant prostate cancer. Neoplasia. 2009 Nov;11(11):1216-25. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Apoptone Related Classifications
HY-16247 Related Classifications
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