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X15695

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

M.Wt 314.67
Formula C14H7ClF4N2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

FC(C1=CN2C(C(Cl)=C1)=NC(C3=CC=C(F)C=C3)=C2)(F)F

References

1. Mengwu Pan, et al. Cancer Res Commun. 2023 Jul 27;3(7):1378-1396.

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