Estrogen receptor modulator 10

CAS: 2991504-90-4 F: C32H37F9N4O3S W: 728.71

Estrogen receptor modulator 10 (compound G-5b) is an Estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=

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Bioactivity	Estrogen receptor modulator 10 (compound G-5b) is an Estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 can induce apoptosis. Estrogen receptor modulator 10 can block cells at the G1/G0 phase. Estrogen receptor modulator 10 can be used in cancer studies[1].
Target	IC50=6.7 nM, DC50=0.4 nM
Invitro	Estrogen receptormodulator 10 (20-100 nM, 2-48 h) 在 T47D 细胞中以剂量依赖性的方式显著降低 ER 的活性，在MCF-7 细胞中对细胞 ER 的降解水平比在 T47D 细胞中晚[1]。Estrogen receptormodulator 10 (10 nM, 24 h) 在 MCF-7 和T47D 细胞中能够降低 E2 刺激产生的TFF-1 (trefoil factor 1)、 PgR (progesterone receptor) and GRBE1 (growth regulation by estrogen in breast cancer 1) 的表达[1]。Estrogen receptormodulator 10 (4-100 nM, 24 h) 在 MCF-7 细胞中能够诱导细胞凋亡，显著增强了 caspase-3 和 caspase-9 的活性[1]。Estrogen receptormodulator 10 (4-100 nM, 24 h) 在 MCF-7 细胞中能够抑制G1/G0 期蛋白的表达。[1]。Estrogen receptormodulator 10 (0.2-1 nM, 6 d) 显著抑制了由 E2 介导的 MCF-7 和 T47D 细胞的增殖。[1]。Estrogen receptormodulator 10 (4-100 nM, 24 h) 在 MCF-7 细胞中显著降低了细胞迁移和增殖细胞核抗原水平[1]。Estrogen receptormodulator 10 (20-100 nM, 24 h) 在 MCF-7 细胞中降低了细胞质和细胞核中的 ER，促进 ER 从细胞核转到细胞质中。ER通过蛋白酶体途径迅速降解，而不影响相应mRNA的表达[1]。 0 --> Estrogen receptor modulator 10 相关抗体: Cell Viability Assay[1] Cell Line:
In Vivo	Estrogen receptormodulator 10 (30 mg/kg, 肌肉注射 (i.m.), 单剂量) 在雌性 Sprague-Dawley小鼠中有良好的药代动力学特性[1]。 Animal Model:
Name	Estrogen receptor modulator 10
CAS	2991504-90-4
Formula	C32H37F9N4O3S
Molar Mass	728.71
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Bingsi Wang, et al.A novel scaffold long-acting selective estrogen receptor antagonist and degrader with superior preclinical profile against ER+ breast cancer,European Journal of Medicinal Chemistry,2023.

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