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Conglobatin  ≥90%

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包装规格：1mg in glass bottle
产品描述：基本信息 产品编号：C10844 产品名称：Conglobatin CAS: 72263-05-9 储存条件 粉末 -20℃ 四年 分子式： C28H38N2O6 分子量 498.61 化学名：  3,5,7,11,13,15-Hexamethyl-8,16-bis(1,3-oxazol-5-ylmethyl)-1,9-dioxacyclohexadeca-3,11-diene-2,10-dione     Solubility (25°C)   体外 DMSO   Ethanol   Water   体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   生物活性 产品描述 一种从 Streptomyces conglobatus 培养物中分离得到的大环内酯双内酯。 靶点/IC50 HSP90   体外研究 Conglobatin (6.25-100μM; 48 h) markedly inhibits the proliferation of SKBR3 and MCF-7 cells, with IC50s of 12.11 and 39.44μM, 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 9.31μM, respectively. Conglobatin (10-40μM; 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 (10-40μM; 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, 100μM 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, 40μM 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 Animal Model: SKBR3 and MCF-7 cells Dosage: 10, 20, 40μM Administration: 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 timedependent manner in MCF-7 cells   体内研究 Conglobatin (50-200mg/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 (4-8mg/kg; i.p. daily for 21 days) inhibits tumor growth in EC109 and KYSE510 tumor xenograft models with low toxicity Animal Model: BALB/c (nu/nu) athymic mice with SKBR3 and MCF-7 tumor xenograft Dosage: 50, 100, 200mg/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.
保存条件：-20℃

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