ER degrader 5
Modify Date: 2024-04-07 12:06:39
ER degrader 5 structure
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Common Name | ER degrader 5 | ||
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| CAS Number | 2913192-47-7 | Molecular Weight | 464.48 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C26H18F2O4S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of ER degrader 5ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer[1]. |
| Name | ER degrader 5 |
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| Description | ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer[1]. |
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| Related Catalog | |
| In Vitro | ER degrader 5 (compound 27d) (5 days) 抑制 MCF-7 细胞的增殖，IC50 值为 55 nM[1]。 ER degrader 5 阻断 MCF-7 细胞 G0/G1 期细胞周期[1]。 ER degrader 5 (1 nM-10 μM; 24 h) 降解 MCF-7 细胞中的雌激素受体 (ER)[1]。 ER degrader 5 (1-10 μM; 24 h) 显着降低 MCF-7 细胞中GREB1，PGR 和 TFF1 的表达水平[1]。 Western Blot Analysis[1] Cell Line: MCF-7 cells Concentration: 1, 10, 100, 1000, 10000 nM Incubation Time: 24 hours Result: Degraded ER in a dose-dependent manner. Real Time qPCR[1] Cell Line: MCF-7 cells Concentration: 1, 5, 10 μM Incubation Time: 24 hours Result: Decreased the expression levels of GREB1, PGR, and TFF1 in a dose-dependent manner. |
| In Vivo | ER degrader 5 (compound 27d) (30 mg/kg; i.p. daily for 30 days) 显着抑制 MCF-7 异种移植模型中的肿瘤生长[1]。 ER degrader 5 (3 mg/kg; i.v.) 的半衰期为 1.23 小时，Cmax 为 4497 ng/mL[1]。 ER degrader 5 (30 mg/kg; p.o.) 产生 62.9% 的口服生物利用度[1]。 Animal Model: Female nude mice injected with MCF-7 cells[1] Dosage: 30 mg/kg Administration: I.p. daily for 30 days Result: Inhibited tumor growth and observed no significant body weight loss. |
| References |
| Molecular Formula | C26H18F2O4S |
|---|---|
| Molecular Weight | 464.48 |
| InChIKey | VMVZYLAEKNIDOM-BJMVGYQFSA-N |
| SMILES | Cc1cc(F)cc(C)c1C(=O)c1sc2cc(F)ccc2c1Oc1ccc(C=CC(=O)O)cc1 |