X15695 | ERα degrader | Probechem Biochemicals

Chemical Structure : X15695

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X15695 (X 15695)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	314.67
分子式	C14H7ClF4N2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

X15695 (X 15695)

生物&药学活性

物理化学性质&存储条件

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X15695 (X 15695)

生物&药学活性

物理化学性质&存储条件

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