3032493-76-5
Chemical Structure
Anticancer agent 340
- CAS No.: 3032493-76-5
- Formula:C49H51ClN10O4S
- Molecular Weight:911.51
InChIKey: MFQCZZWWLAYIPM-ZCTOLVMZSA-N
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
Biological Activity: 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)[1].
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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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Keywords
