GDC-0810

产品编号: DC23161 Featured
GDC-0810
结构式
1365888-06-7
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中国地区超过5000个高品质化合物库存
应用领域
Brilanestrant (ARN-810; GDC-0810) 是一种可口服的,选择性的雌激素降能器 (selective estrogen receptor degrader),IC50 值为 0.7 nM。
Cas No.: 1365888-06-7
名称: 2-Propenoic acid, 3-[4-[(1E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)-1-buten-1-yl]phenyl]-, (2E)-
别名: ARN-810;Brilanestrant
SMILES: O=C(C=CC1C=CC(C(=C(CC)C2C(Cl)=CC(F)=CC=2)C2C=CC3NN=CC=3C=2)=CC=1)O
分子式: C26H20ClFN2O2
分子量: 446.9006
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: GDC-0810 (ARN-810, Brilanestrant) is a non-steroidal, orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM (ER-α degradation), binds to ERα and ERβ with with Ki of 3.8 and 3.7 nM, respectively; dually antagonizes and induces proteasome-dependent degradation of ERα, exhibits robust in vitro activity against a variety of human breast cancer cell lines (MCF7 cell IC50=25 nM); demonstrates robust activity in models of tamoxifen-sensitive and tamoxifen-resistant breast cancer models.Breast CancerPhase 1 Discontinued
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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MSDS_1224_DC23161_1365888-06-7
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