1332390-06-3
Chemical Structure
JNJ-pan-AR
- CAS No.: 1332390-06-3
- Formula:C25H24F3N5O2S
- Molecular Weight:515.55
InChIKey: IZKSMIBPGSWAMO-UHFFFAOYSA-N
SMILES: N#CC1=NC=C(N2C(C3(CCC3)N(C2=S)C4=CC=C(C=C4)OC5CCN(CC5)C)=O)C=C1C(F)(F)F
Biological Activity: JNJ-pan-AR is an orally active androgen receptor (AR) inhibitor with an IC50 of 19 nM and a Ki of 8.4 nM against human wild-type AR. JNJ-pan-AR abolishes androgen-induced KLK2 and KLK3 mRNA expression and reduces androgen-dependent colony formation in prostate cancer cells. JNJ-pan-AR blocks AR nuclear translocation, inhibits PSA protein expression, and represses the growth of AR-dependent tumor cells and ARF877L-driven tumor xenografts. JNJ-pan-AR blocks transactivation and signaling of wild-type AR and various mutant AR variants. JNJ-pan-AR is applicable for research on castration-resistant prostate cancer[1][2].
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JNJ-pan-AR | JNJ-pan-AR is an orally active androgen receptor (AR) inhibitor with an IC50 of 19 nM and a Ki of 8.4 nM against human wild-type AR. JNJ-pan-AR abolishes androgen-induced KLK2 and KLK3 mRNA expression and reduces androgen-dependent colony formation in prostate cancer cells. JNJ-pan-AR blocks AR nuclear translocation, inhibits PSA protein expression, and represses the growth of AR-dependent tumor cells and ARF877L-driven tumor xenografts. JNJ-pan-AR blocks transactivation and signaling of wild-type AR and various mutant AR variants. JNJ-pan-AR is applicable for research on castration-resistant prostate cancer. | |||||||||||||||||||||
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- [1]. Zhang Z, et al. Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC). J Med Chem. 2021;64(2):909-924. [Content Brief]
- [2]. Hertzog JR, et al. AKR1C3 mediates pan-AR antagonist resistance in castration-resistant prostate cancer. Prostate. 2020;80(14):1223-1232. [Content Brief]
Keywords
