Chemical Structure : X15695
CAS No.:
353258-25-0
X15695
(X 15695)
Catalog No.: PC-20995Not For Human Use, Lab Use Only.
X15695 is a potent, selective and orally active estrogen receptor alpha (ERα) degrader, destabilizes ERα and stabilizes p53, inhibits ER+ breast cancer cell growth.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
X15695 is a potent, selective and orally active estrogen receptor alpha (ERα) degrader, destabilizes ERα and stabilizes p53, inhibits ER+ breast cancer cell growth.
X15695 efficiently degrades ERα and attenuates estrogen-mediated target gene expression as well as transactivation by the AR.
X15695 reactivates p53, also disrupts key cellular protein–protein interactions such as BAG1–mortalin (GRP75) interaction as well as wild-type p53–mortalin or mutant p53–BAG2 interactions.
X15695 induces cell-cycle arrest and inhibits proliferation of AR+ and ER+ prostate and breast cancer cells.
X15695 (30 mg/kg/day, oral) effectively inhibited tumor growth in mouse tumor xenograft experiments using LAPC-4 cells.
X15695 is selective for ER+ breast cancer, with no any significant effect on the other tumors cell lines.
Physicochemical Properties
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M.Wt
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314.67
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Formula
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C14H7ClF4N2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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FC(C1=CN2C(C(Cl)=C1)=NC(C3=CC=C(F)C=C3)=C2)(F)F
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References
1. Mengwu Pan, et al. Cancer Res Commun. 2023 Jul 27;3(7):1378-1396.
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