Imlunestrant (LY3484356) | SERD and ER inhibitor | Probechem Biochemicals

Chemical Structure : Imlunestrant

CAS No.: 2408840-26-4

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Imlunestrant (LY3484356, LY-3484356)

货号: PC-73421Not For Human Use, Lab Use Only.

Imlunestrant (LY3484356) is a potent, oral, selective estrogen receptor degrader (SERD) and pure estrogen receptor antagonist with Ki values of 0.64 nM and 2.8 nM against WT ERα and Y537S mutant ERα proteins, respectively.

规格	价格	库存
2 mg	￥2980	In stock
5 mg	￥4880	In stock
10 mg	￥7580	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

Imlunestrant (LY3484356) is a potent, oral, selective estrogen receptor degrader (SERD) and pure estrogen receptor antagonist with Ki values of 0.64 nM and 2.8 nM against WT ERα and Y537S mutant ERα proteins, respectively.
LY 3484356 is a potent and highly efficient degrader of wild type ERα and Y537N mutant ERα proteins in cells, with IC50 values 3.0 nM and 9.6 nM, respectively.
LY3484356 is also a potent inhibitor of ERα-mediated transcription in vitro and in vivo.
LY 3484356 inhibits cell proliferation in wild type ERα and ESR1 Y537N mutant breast cancer cell lines with IC50 of 3 and 17 nM, respectively. LY3484356 has IC50 of <100 nM against a panel of ER+ breast cancer cell lines.
LY3484356 has demonstrated sustained and prolonged target inhibition in ESR1 wild type (MCF7) and ESR1 Y537S mutant (ST941/C) xenograft tumors.
LY3484356 demonstrated significant tumor growth inhibition and tumor regressions in wild type ESR1 breast cancer xenograft models such as MCF7, T47D and ZR-75-1, as well as ESR1 mutant breast cancer PDX models.
LY3484356 has shown synergy or additivity in combination with CDK4/6 inhibitor abemaciclib, mTOR inhibitor everolimus and PIK3CA inhibitor alpelisib in inhibiting cell proliferation in ER+ breast cancer cell lines in vitro and tumor growth inhibition in relevant xenograft or PDX models in vivo.

物理化学性质&存储条件

分子量	524.516
分子式	C29H24F4N2O3
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	(5R)-5-(4-{2-[3-(fluoromethyl)azetidin-1- yl]ethoxy}phenyl)-8-(trifluoromethyl)-5H- [1]benzopyrano[4,3-c]quinolin-2-ol

参考文献

1. Shripad V. Bhagwat, et al. Cancer Res (2021) 81 (13_Supplement): 1236.

Imlunestrant (LY3484356, LY-3484356)

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物理化学性质&存储条件

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Imlunestrant (LY3484356, LY-3484356)

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物理化学性质&存储条件

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