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ZB716(Fulvestrant-3 Boronic Acid)

产品编号: DC22301 Featured
ZB716(Fulvestrant-3 Boronic Acid)
结构式
1853279-29-4
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中国地区超过5000个高品质化合物库存
应用领域
ZB716是一种甾体，口服生物可利用的SERD（选择性雌激素受体下调因子），以高亲和力与ER结合，并对表达ER的乳腺癌细胞发挥其抗雌激素作用。
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 1853279-29-4
名称:
别名: ZB-716,ZB 716
SMILES: C1=C2C(C[C@H](CCCCCCCCCS(CCCC(F)(F)C(F)(F)F)=O)[C@]([H])3[C@@]2([H])CC[C@@](C)2[C@]3([H])CC[C@H]2O)=CC(B(O)O)=C1
分子式: C32H48BF5O4S
分子量: 634.59
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: ZB716 is a steroidal, orally bioavailable SERD (selective estrogen receptor downregulator) that binds to ER with high affinity and exerts its antiestrogenic effect on ER-expressing breast cancer cells. In both tamoxifen-naive and tamoxifen-resistant breast cancer cells, ZB716 potently inhibits cell proliferation and effectively degrades the hormone receptor in a dose-dependent manner. ZB716 is shown to have far superior oral bioavailability in mice when compared to fulvestrant.. ZB716 was previously reported as an orally bioavailable SERD structurally analogous to fulvestrant.The ability of ZB716 to inhibit cell growth and downregulate ER expression in endocrine resistant, ERα mutant breast cancer cells was demonstrated. Moreover, in the MCF-7 xenograft and two patient derived xenograft models, orally administered ZB716 showed superior efficacy in blocking tumor growth when compared to fulvestrant. Importantly, such enhanced efficacy of ZB716 was shown to be attributable to its markedly higher bioavailability, as evidenced in the final plasma and tumor tissue concentrations of ZB716 in mice where drug concentrations were found significantly higher than in the fulvestrant treatment group.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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MSDS_1123_DC22301_1853279-29-4
COA
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