2. Others Vitamin D Related/Nuclear Receptor
  3. Drug Derivative Androgen Receptor
  4. 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.

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Apoptone

Apoptone Chemical Structure

CAS No. : 183387-50-0

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Apoptone Related Antibodies

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Description

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[1][2].

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.

Apoptone Related Antibodies
In Vivo

Apoptone (20-200 mg/kg; p.o.; daily; 28 days) produces dose- and time-dependent reductions in plasma testosterone, androstenedione, and DHEA concentrations in male beagle dogs, with up to 99.3% reduction in testosterone at the 200 mg/kg dose after 28 days[1].
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.

Animal Model: CB-17 SCID (male; castrated; implanted subcutaneously with ~20 mg LuCaP35V tumor bits)[2]
Dosage: 160 mg/kg
Administration: i.p.; once daily, 5 days/week; 4 weeks
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
Molecular Weight

316.48

Formula

C21H32O2
CAS No.
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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Apoptone Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Apoptone183387-50-0HE3235HE 3235HE-3235Drug DerivativeAndrogen ReceptorDrug derivativebreast cancerCYP1A2CYP2C9LNCaP cellsprostate cancerCYP2C19castration-resistant prostate cancerCYP3A4androgen receptorCYP2D6Inhibitorinhibitorinhibit

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