A031
A031 is a PROTAC degrader targeting the androgen receptor. A031 induces time-dependent degradation of androgen receptor protein. A031 exerts tumor growth inhibitory effects in a zebrafish model xenografted with human prostate cancer cells. A031 can be used in studies related to prostate cancer.
(Pink: Androgen Receptor ligand (HY-175937); Blue: VHL and VHL ligand (HY-112078); Black: linker).
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- CAS No.: 2682255-44-1
- Formule: C50H61ClN10O7S
- Masse moléculaire:981.60
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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
In Vitro
A031 (2.0 μM; 2-4.5 h) induces time-dependent degradation of AR protein in AR-positive human prostate cancer VCaP cells, with near-complete degradation observed after 4.5 h of treatment with 2.0 μM A031[1].
A031 (2.0 μM) acts as a bona fide AR degrader in AR-positive human prostate cancer VCaP cells, as its AR-degrading activity is blocked by proteasome and NEDD8 pathway inhibitors but not by VHL-3 pre-treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AR-positive human prostate cancer VCaP cells
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Concentration:0.125 μM; 0.25 μM; 0.5 μM; 1.0 μM
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Incubation Time:4 days
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Result:Inhibited VCaP cell viability in a dose-dependent manner.
Achieved a cell inhibition rate of 69.56% at 1.0 μM.
Showed a good inhibition rate even at 0.125 μM.
Had an IC50 for cell inhibition of less than 0.25 μM.
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Cell Line:AR-positive human prostate cancer VCaP cells
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Concentration:2.0 μM
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Incubation Time:2 h, 3.5 h, 4.5 h
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Result:Reduced AR protein levels within 2 h of treatment.
Almost completely degraded AR protein after 4.5 h of treatment.
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax | AUClast | AUCinf | Vz | CL |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 0.57 h | 14366.2 ng/mL | 1773.8 ng·h/mL | 1773.8 ng·h/mL | 0.47 L/kg | 0.57 L/h/kg |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:wild-type AB strain (2 days post-fertilization)[1]
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Dosage:2.8 μM; 8.3 μM; 25 μM
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Administration:static exposure; 2 days
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Result:Achieved a 28% tumor growth inhibition rate with a tumor fluorescence intensity of 379577 pixels.
Achieved a 55% tumor growth inhibition rate with a tumor fluorescence intensity of 240013 pixels.
Achieved a 61% tumor growth inhibition rate with a tumor fluorescence intensity of 208489 pixels.
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Animal Model:wild-type AB strain (3 days post-fertilization)[1]
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Dosage:6.25 μM; 12.5 μM; 25 μM; 50 μM; 100 μM
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Administration:static exposure; 5 days
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Result:Caused 0% mortality and no toxic phenotypes at 6.25 μM, 12.5 μM, and 25 μM.
Caused obvious precipitation at 50 μM and 100 μM, with mortality data not reported.
Determined a minimal toxic concentration (MTC) of 25 μM.
Chemical Information
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CAS No. 2682255-44-1
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Masse moléculaire 981.60
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Formule C50H61ClN10O7S
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SMILES
O=C(N([C@@H]1C2)[C@H](CC1)C[C@@H]2OC3=CC(Cl)=C(C=C3)C#N)C4=CN=C(N5CCN(CC5)CCOCC(N[C@@H](C(C)(C)C)C(N6[C@@H](C[C@H](C6)O)C(N[C@H](C7=CC=C(C8=C(N=CS8)C)C=C7)C)=O)=O)=O)N=C4
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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)
A031 Related Classifications
HY-148777 Related Classifications
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