A031
A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP).
(Pink: Androgen Receptor Target protein ligand; Blue: 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
- Pureté et documentation
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Activité biologique
A031 (0.125-1.000 μM) shows inhibition to AR with an IC50 value less than 0.25 μM[1]. A031 (2 μM; 2-4.5 h) reduces the AR protein level in VCaP cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:VCaP cell lines
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Concentration:2 μM
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Incubation Time:2, 3.5 and 4.5 hours
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Result:Reduced the AR protein level, and AR proteins was almost degraded after 4.5 h treatment.
| Rats IV 1 mg/kg |
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| t1/2 (h) | 0.57 |
| Cmax (ng/mL) | 14366.2 |
| AUClast (h·ng/mL) | 1773.8 |
| AUCINF_pred (h·ng/mL) | 1773.8 |
| Vz_pred (L/kg) | 0.47 |
| Cl_pred (L/h/kg) | 0.57 |
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 zebrafish with human prostate cancer (VCap) cells transplantatio[1]
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Dosage:2.8, 8.3 and 25 μM
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Administration:Aqueous solution culture, at 35℃, for 5 days
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Result:Inihibited tumor growth with growth inhibition rates of 28%, 55% and 61% at 2.8, 8.3 and 25 μM, respectively.
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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