Anticancer agent 340
Anticancer agent 340 is an orally active antitumor agent. Anticancer agent 340 can bind to both the androgen receptor (AR) and BRD4 protein simultaneously, dose-dependently inducing the formation of the AR-BRD4 ternary complex, inhibiting the expression of the downstream target gene HEXIM1 (Gene X), and activating the Caspase 3/7 pathway to initiate apoptosis. Its proliferation inhibition and apoptosis activities are both significantly AR expression-dependent. Anticancer agent 340 can be used to study AR/BRD4 driven malignancies such as castration-resistant prostate cancer (CRPC).
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- No. CAS: 3032493-76-5
- Fòrmula: C49H51ClN10O4S
- Peso molecular:911.51
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Almacenamiento:
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Actividad biológica
Descripciòn
In Vitro
Anticancer agent 340 (compound I-49) (0.1 nM-10 μM; 6 days) exhibits potent inhibitory activity against AR-dependent prostate cancer cells , and its antiproliferative activity depends on the expression of full-length AR[1].
Anticancer agent 340 (serial dilutions; 72 h) exhibits potent inhibitory activity against the proliferation of T-Rex 293 cell line SC cells[1].
Anticancer agent 340 (serial dilutions; 24-48 h)-induced apoptosis in 22RV1 parental cells depends on the expression level of full-length AR (FL-AR) [1].
Anticancer agent 340 (serial dilutions; 16 h) effectively inhibits the expression of downstream target genes of EP (BRD4), validating the target engagement of PROTAC[1].
Anticancer agent 340 (serial dilutions; 1 h) dose-dependently induces the formation of the AR-compound-EP ternary complex; neither AR ligand alone nor EP ligand alone can induce the formation of the ternary complex[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LnCaP95 parental cells
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Concentration:0.1 nM-10 μM
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Incubation Time:4 h
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Result:Had a GI₅₀ of 37 nM in LnCaP95 parental cells.
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Cell Line:T-Rex 293 cell line SC cells
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Concentration:serial dilutions
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Incubation Time:72 h
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Result:Strongly inhibited cell proliferation.
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Cell Line:22RV1 parental cells
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Concentration:serial dilutions
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Incubation Time:24-48 h
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Result:Showed an EC₅₀ of 126 nM in FL-AR-overexpressing 22RV1 cells.
Significantly reduced apoptosis activity in FL-AR-underexpressing cells.
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Cell Line:TReX293 cells
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Concentration:serial dilutions
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Incubation Time:16 h
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Result:Dose-dependently reduced Gene X mRNA levels.
In Vivo
Anticancer agent 340 (10-100 mg/kg; p.o.; once daily; for 3 days) can effectively penetrate tumor tissue in vivo and inhibit the expression of downstream genes of EP (BRD4), demonstrating good PD efficacy[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 immunodeficient mice were subcutaneously implanted with 5×106 VCaP cells suspended in 50% Matrigel[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o., once daily
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Result:Dose-dependently inhibited the growth of castrated VCaP tumors.
Dose-dependently reduced plasma PSA concentration.
Dose-dependently induces the formation of the AR-compound-BRD4 ternary complex in tumor tissue.
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Animal Model:CB17.SCID immunodeficient mice were subcutaneously implanted with 5×106 VCaP cells suspended in 50% Matrigel[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o., once daily; for 3 days
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Result:Dose-dependently reduced Gene X mRNA levels in tumor tissue.
Chemical Information
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No. CAS 3032493-76-5
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Peso molecular 911.51
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Fòrmula C49H51ClN10O4S
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SMILES
CC(C)([C@H](C1(C)C)OC2=CC(Cl)=C(C=C2)C#N)[C@H]1NC(C3=CN=C(N=C3)N(CC4)CCC4(C5)CC5OC6=CC=C(C7=N[C@@H](CC8=NC=CO8)C9=NN=C(C)N9C%10=C7C(C)=C(C)S%10)C=C6)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Anticancer agent 340 Related Classifications
HY-184865 Related Classifications
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