Varilutamide
Varilutamide (ONC1-13B) is an orally active androgen receptor (AR) inhibitor. Varilutamide shows a rat AR IC50 of 7.9 μM, inhibits DHT-stimulated PSA expression and prostate cancer cell proliferation, suppresses tumor growth and PSA expression and weakly induces lower CYP3A activity. Varilutamide can be used for the research of castration-resistant prostate cancer and prostate cancer.
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- CAS No.: 1351185-54-0
- Formule: C22H16F4N4O3S
- Masse moléculaire:492.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
CYP3A |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
30 nM
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Inhibition of DHT-induced proliferation of human LNCaP prostate cancer cells assessed as viable cell number after 5 day incubation in the presence of 1 nM DHT.
Inhibition of DHT-induced proliferation of human LNCaP prostate cancer cells assessed as viable cell number after 5 day incubation in the presence of 1 nM DHT.
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24494031 |
In Vitro
Varilutamide (ONC1-13B) (1 nM-10 μM; 24 h) potently inhibits DHT-induced PSA expression in LNCaP prostate cancer cells[1].
Varilutamide (1 nM-10 μM; 5 days) inhibits DHT-induced proliferation of LNCaP prostate cancer cells with an IC50 of 30 nM[1].
Varilutamide (1 nM-100 μM) binds to rat androgen receptor ligand-binding domain with an IC50 of 7.9 μM[1].
Varilutamide (1 nM-100 μM) acts as a full androgen receptor antagonist, inhibiting ligand-dependent coactivator recruitment with an IC50 of 19.9 μM without inducing coactivator recruitment on its own[1].
Varilutamide (10 μM; 60 min) inhibits [3H] GABA binding to rat cerebral cortex membrane homogenates by 42%[1].
Varilutamide (1-10 μM; 48 h) induces CYP3A activity in human cryopreserved hepatocytes at 10 μM but shows no significant induction at 1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP prostate cancer cells
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Concentration:1, 10, 100 nM; 1, 10 μM
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Incubation Time:5 days
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Result:Inhibited DHT-induced cell proliferation with an IC50 of 30 nM.
Parmacokinetics
| Species | Dose | Route | Plasma Concentration | T1/2 | Cmax | AUCINF_obs | MRTINF_obs | CL | Vss_obs | Tmax | Brain Concentration |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | / | 4.1 h | 531 ng/mL | 2572 ng/mL·h | 5.3 h | 6.4 mL/min/kg | 2.0 L/kg | / | / |
| Rat[1] | 5 mg/kg | p.o. | / | 5.2 h | 1062 ng/mL | 13105 ng/mL·h | 7 h | / | / | 2 h | / |
| Rat[1] | 30 mg/kg | p.o. | / | 4 h | 7162 ng/mL | 95000 ng/mL·h | 4 h | / | / | 4 h | / |
| Rat[1] | 100 mg/kg | p.o. | / | 8 h | 16357 ng/mL | 268000 ng/mL·h | 10 h | / | / | 4 h | / |
| Rat[1] | 300 mg/kg | p.o. | / | 6 h | 20533 ng/mL | 314000 ng/mL·h | 7 h | / | / | 4 h | / |
| Rat[1] | 2 mg/kg | i.v. | 746 ng/mL | / | / | / | / | / | / | / | 145 ng/g |
| Dog[1] | 10 mg/kg | p.o. | 1.25 μg/mL | / | / | / | / | / | / | / | / |
| Mice[1] | 20 mg/kg | p.o. | 76.2 ng/mL | / | / | / | / | / | / | / | / |
| Mice[1] | 40 mg/kg | p.o. | 456.4 ng/mL | / | / | / | / | / | / | / | / |
| Mice[1] | 50 mg/kg | p.o. | 154.4 ng/mL | / | / | / | / | / | / | / | / |
In Vivo
Varilutamide (30-300 mg/kg; p.o.; once daily for 14 or 60 days) dose-dependently reduces the weight of androgen-dependent reproductive organs and epididymal sperm concentration in male rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17-SCID (male; subcutaneous implantation of 2×106 LNCaP-Z2 tumor cells)[1]
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Dosage:20 mg/kg (once daily); 50 mg/kg (once daily); 20 mg/kg (twice daily)
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Administration:p.o.; daily or twice daily for 21 days
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Result:Reduced mean tumor weight significantly compared to vehicle.
Reduced mean plasma PSA significantly compared to vehicle.
Reduced tumor Ki-67 proliferative activity.
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Animal Model:male rats[1]
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Dosage:30 mg/kg (14 days); 100 mg/kg (14 days); 300 mg/kg (14 days); 30 mg/kg (60 days); 300 mg/kg (60 days)
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Administration:p.o.; once daily for 14 days or 60 days
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Result:Reduced relative weight of epididymis, prostate, and seminal vesicles dose-dependently compared to vehicle control after 14 days.
Reduced mean epididymal sperm concentration.
Chemical Information
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CAS No. 1351185-54-0
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Masse moléculaire 492.45
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Formule C22H16F4N4O3S
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SMILES
O=C1[C@]2(CCOC2)N(C3=CC(F)=C(C=C3)C(NC)=O)C(N1C4=CC(C(F)(F)F)=C(C=C4)C#N)=S
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Synonyms
ONC1-13B
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Varilutamide Related Classifications
HY-114246 Related Classifications
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Keywords
- Varilutamide
- 1351185-54-0
- ONC1-13B
- Androgen Receptor
- Cytochrome P450
- PSA
- androgen receptor
- LNCaP-Z2 xenograft mice
- PathHunter? NHR cells
- castration-resistant prostate cancer
- CYP3A
- rat cerebral cortex membrane homogenates
- prostate cancer
- human cryopreserved hepatocytes
- LNCaP prostate cancer cells
- Inhibitor
- inhibitor
- inhibit