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Chemical Structure : EPI-7170
Catalog No.: PC-49412Not For Human Use, Lab Use Only.
EPI-7170 is a potent next-generation analog of Ralaniten (EPI-002) and inhibitor of androgen receptor N-terminal domain (AR-NTD), inhibits androgen-induced PSA-luciferase activity in transiently transfected LNCaP cells with IC50 of 1.08 uM.
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EPI-7170 is a potent next-generation analog of Ralaniten (EPI-002) and inhibitor of androgen receptor N-terminal domain (AR-NTD), inhibits androgen-induced PSA-luciferase activity in transiently transfected LNCaP cells with IC50 of 1.08 uM.
EPI-7170 has approximately 10 times better potency for inhibiting AR transcriptional activity compared to ralaniten.
EPI-7170 selectively inhibits the DNA damage repair (DDR) pathway in prostate cancer cells that express both full-length AR and AR-Vs, whereas enzalutamide has no effect.
EPI-7170 increase levels of γH2AX whereas enzalutamide has little added benefit in LNCaP95 cells.
EPI-7170 specifically inhibits AR-dependent proliferation and tumor growth.
EPI-7170 (25 mg/kg, oral) has antitumor activity on CRPC xenografts driven by AR and AR-Vs in vivo.
| M.Wt | 540.877 | |
| Formula | C22H28Cl3NO6S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Hirayama Y, et al. Mol Oncol. 2020 Oct;14(10):2455-2470.
2. Tien AH, et al. Mol Cancer Ther. 2022 Feb;21(2):294-309.
3. Carmen A Banuelos, et al. Cancers (Basel). 2020 Jul 21;12(7):1991.
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