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CONGLOBATIN

生物活性 靶点 体外研究 体内研究 CONGLOBATIN 试剂级价格
CONGLOBATIN, 72263-05-9, 结构式
CONGLOBATIN
CAS号:
72263-05-9
英文名:
CONGLOBATIN
英文别名:
FW-04-806;CONGLOBATIN;Conglobactin;Conglobatin, >=99%;(3E,5R,7S,8S,11E,13R,15S,16S)-3,5,7,11,13,15-Hexamethyl-8,16-bis(5-oxazolylmethyl)-1,9-dioxacyclohexadeca-3,11-diene-2,10-dione;1,9-Dioxacyclohexadeca-3,11-diene-2,10-dione, 3,5,7,11,13,15-hexamethyl-8,16-bis(5-oxazolylmethyl)-, (3E,5R,7S,8S,11E,13R,15S,16S)-
中文名:
CONGLOBATIN
中文别名:
成球菌素
CBNumber:
CB3460272
分子式:
C28H38N2O6
分子量:
498.61
MOL File:
72263-05-9.mol

CONGLOBATIN化学性质

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.
安全信息
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。

靶点

HSP90

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 toxicity

Animal 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.

CONGLOBATIN 上下游产品信息

上游原料

下游产品

CONGLOBATIN 试剂级价格

更新日期产品编号产品名称CAS编号包装价格
2024/04/30HY-119906Conglobatin2500 μg19354元
2022/07/01HY-119906CONGLOBATIN
Conglobatin		72263-05-9500μg2500元

CONGLOBATIN 生产厂家

全球有 29家供应商   CONGLOBATIN国内生产厂家
供应商联系电话电子邮件国家产品数优势度
上海佰世凯化学科技有限公司 021-20908456 sales@BioChemBest.com 中国 6008 61
上海一飞生物科技有限公司 021-65675885 18964387627 info@efebio.com 中国 9708 58
上海瀚香生物科技有限公司 17754423994 17754423994 2853530910@QQ.com 中国 8011 62
上海芮晖化工科技有限公司 21-31433387 15618786686 sales@rechemscience.com 中国 2987 58
北京普西唐生物科技有限公司 010-60605840 18892239720 psaitong@jm-bio.com 中国 12308 58
西安莱茵生物科技有限公司 86-(0)29-85992781 17792393971 info@lynnchem.com 中国 4587 58
Novachemistry 44-20819178-90 02081917890 info@novachemistry.com 英国 4381 58
深圳聚合生化科技有限公司 +86-400-002-6226 13028896684 sales@rrkchem.com 中国 56057 58
BOC Sciences 16314854226; +16314854226 inquiry@bocsci.com 美国 19743 58
ChemeGen 中国 18818260767 sales@chemegen.com 中国 11289 58
孟成科技（上海）有限公司 400-820-6829 sales@mitachieve.com 中国 8864 58
上海传芊化工科技中心 15869524721 3525679403@qq.com 中国 3616 58
浙江珲达生物科技有限公司 0571-89903882 13626641628 jiangnan@huidabiotech.com 中国 3656 58
天津普西唐生物医药科技有限公司 010-60605840 psaitong@jm-bio.com 中国 29778 58
浙江珲达生物科技有限公司 0571-0571-89903882 15990081639 sunshixuan@huidabiotech.com 中国 3705 58
上海一研生物科技有限公司 021-69985186 13611928337 3427709316@qq.com 中国 7984 58
南京世洲生物科技有限公司 025-85560043 15850508050 cindy.huang@synzest.com 中国 12007 58
TargetMol中国（陶术生物） 15002134094 marketing@targetmol.cn 中国 28118 58
Aladdin Scientific +1-+1(833)-552-7181 sales@aladdinsci.com 美国 52927 58
Wuhan Topule Biopharmaceutical Co., Ltd +8618327326525 masar@topule.com 中国 8474 58
 

72263-05-9, CONGLOBATIN 相关搜索:

(E)-2-甲基-2-丁酸-2-甲丙酯
  • Antibiotic
  • 抑制剂
  • 微生物代谢物
  • 成球菌素
  • 72263-05-9
  • Conglobactin
  • 1,9-Dioxacyclohexadeca-3,11-diene-2,10-dione, 3,5,7,11,13,15-hexamethyl-8,16-bis(5-oxazolylmethyl)-, (3E,5R,7S,8S,11E,13R,15S,16S)-
  • Conglobatin, >=99%
  • CONGLOBATIN
  • FW-04-806
  • (3E,5R,7S,8S,11E,13R,15S,16S)-3,5,7,11,13,15-Hexamethyl-8,16-bis(5-oxazolylmethyl)-1,9-dioxacyclohexadeca-3,11-diene-2,10-dione
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