CONGLOBATIN
- CAS号:72263-05-9
- 英文名:CONGLOBATIN
- 中文名:CONGLOBATIN
- CBNumber:CB3460272
- 分子式:C28H38N2O6
- 分子量:498.61
- MOL File:72263-05-9.mol
- 密度 :1.060±0.06 g/cm3 (20 ºC 760 Torr)
- 储存条件 :-20°C
- 溶解度 :DMF: soluble; DMSO: soluble; Ethanol: soluble; Methanol: soluble
- 形态 :White to off-white solid.
- WGK Germany :3
- 海关编码 :29419000
CONGLOBATIN性质、用途与生产工艺
- 生物活性 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。
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靶点
HSP90
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体外研究
Conglobatin (6.25-100 μM; 48 h) markedly inhibits the proliferation of SKBR3 and MCF-7 cells, with IC 50 s of 12.11 and 39.44 μM, respectively.
Conglobatin inhibits cell proliferation in EC109, KYSE70, KYSE450, KYSE150, KYSE180, and KYSE510 cells, with IC 50 s 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.Cell Proliferation Assay
Cell Line: SKBR3 and MCF-7 cells Concentration: 6.25, 12.5, 25, 50, 100 μM Incubation Time: 48 hours Result: Inhibited the proliferation of SKBR3 and MCF-7 cells in a dose-dependent manner. Cell Cycle Analysis
Cell Line: SKBR3 and MCF-7 cells Concentration: 10, 20, 40 μM Incubation Time: 24 hours Result: Increased the G2/M cell population and decreased the population in the S and G0/G1 phases. Western Blot Analysis
Cell Line: SKBR3 and MCF-7 cells Concentration: 10, 20, 40 μM Incubation Time: 3, 6, 12, 24 hours Result: Decreased the levels of the client proteins HER2, p-HER2, Raf-1, Akt, and p-Akt in a dose and time-dependent manner in SKBR3 cells.
Reduced the the levels of the client proteins Raf-1, Akt, and p-Akt in a dose and time-dependent manner in MCF-7 cells. -
体内研究
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 toxicityAnimal Model: BALB/c (nu/nu) athymic mice with SKBR3 and MCF-7 tumor xenograft Dosage: 50, 100, 200 mg/kg Administration: Oral gavage every 3 days for 24 days Result: Showed inhibition of tumor growth at a rate of 39.1%, 52.7%, and 67.5% in the SKBR3 cell line groups and 27.3%, 39.8%, 54.3% in the MCF-7 cell line groups at the three increasing doses, respectively.
Was well tolerated.
- 更新日期：2024/04/30
- 产品编号：HY-119906
- 产品名称：Conglobatin
- CAS编号：
- 包装：2500 μg
- 价格：19354元
- 更新日期：2022/07/01
- 产品编号：HY-119906
- 产品名称：CONGLOBATIN Conglobatin
- CAS编号：72263-05-9
- 包装：500μg
- 价格：2500元
- 公司名称：CFMOT-PHYTO
- 联系电话：--
- 电子邮件：
- 国家：德国
- 产品数：1136
- 优势度：62
