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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
FW-04-806
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
72263-05-9
- 规格：
500 μg/1 mg
| 规格： | 500 μg | 产品价格： | ￥1800.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥2880.0 |
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Conglobatin
CAS No. : 72263-05-9
MCE 国际站：Conglobatin
产品活性：Conglobatin (FW-04-806) 是一种从 Streptomyces conglobatus 培养物中分离得到的大环内酯双内酯。Conglobatin 是一种具有口服活性的 Hsp90 抑制剂，可以与 Hsp90 的 N 末端域结合，并破坏 Hsp90-Cdc37 复合物的形成。Conglobatin 可诱导人乳腺癌细胞和食道鳞状细胞癌细胞凋亡，并在体内表现出抗肿瘤活性。
研究领域：Cell Cycle/DNA Damage | Metabolic Enzyme/Protease | Apoptosis
In Vitro: Conglobatin (6.25-100 μM; 48 h) markedly inhibits the proliferation of SKBR3 and MCF-7 cells, with IC50s of 12.11 and 39.44 μM, respectively.
Conglobatin inhibits cell proliferation in EC109, KYSE70, KYSE450, KYSE150, KYSE180, and KYSE510 cells, with IC50s of 16.43, 15.89, 10.94, 10.50, 10.28, and 9.31 μM, respectively.
Conglobatin (10-40 μM; 24 h) displays obvious arrest of SKBR3 and MCF-7 cells in the G2/M phase. Conglobatin induces apoptosis through caspase-dependent pathways in SKBR3 and MCF-7 cells.
Conglobatin (10-40 μM; 3-24 h) reduces Hsp90 client protein levels and induces proteasome-dependent degradation.
Conglobatin binds to the N-terminal of Hsp90, does not affect ATP-binding capability of Hsp90, but inhibits Hsp90/Cdc37 chaperone/co-chaperone interactions.
In Vivo: Conglobatin (50-200 mg/kg; i.g. q3d for 24 d) inhibits the tumor growth of SKBR3 and MCF-7 human breast cancer xenograft models in a dose-dependent manner.
Conglobatin (4-8 mg/kg; i.p. daily for 21 days) inhibits tumor growth in EC109 and KYSE510 tumor xenograft models with low toxicity
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