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Chemical Structure : KCI807
Catalog No.: PC-35680Not For Human Use, Lab Use Only.
KCI807 (KCI-807) is a small molecule that selectively disrupts ELK1-dependent promoter activation by wild-type and variant androgen receptors (IC50=0.53 uM) without interfering with ELK1 activation by ERK.
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KCI807 (KCI-807) is a small molecule that selectively disrupts ELK1-dependent promoter activation by wild-type and variant androgen receptors (IC50=0.53 uM) without interfering with ELK1 activation by ERK.
KCI807 binds to AR (Kd=69.2 nM), blocking ELK1 binding, and selectively blocks recruitment of AR to chromatin by ELK1.
KCI807 primarily affects a subset of AR target growth genes selectively suppressing AR-dependent growth of PC cell lines with a better inhibitory profile than Enzalutamide.
KCI807 also inhibits in vivo growth of castration/enzalutamide-resistant cell line-derived and patient-derived tumor xenografts.
| M.Wt | 254.241 | |
| Formula | C15H10O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Rosati R, et al. Clin Cancer Res. 2018 Sep 5. pii: clincanres.0982.2018. doi: 10.1158/1078-0432.CCR-18-0982.
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