2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  3. HSP Apoptosis
  4. Conglobatin

Conglobatin  (Synonyms: FW-04-806)

目录号: HY-119906 纯度: 95.48%
COA 产品使用指南

摩尔计算器

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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Conglobatin Chemical Structure

Conglobatin Chemical Structure

CAS No. : 72263-05-9

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规格 价格 是否有货 数量
500 μg ￥7800
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Conglobatin 相关抗体

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo[1][2][3].

IC50 & Target[2]

HSP90

 

体外研究
(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[2].
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[3].
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[2].
Conglobatin (10-40 μM; 3-24 h) reduces Hsp90 client protein levels and induces proteasome-dependent degradation[2].
Conglobatin binds to the N-terminal of Hsp90, does not affect ATP-binding capability of Hsp90, but inhibits Hsp90/Cdc37 chaperone/co-chaperone interactions[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Conglobatin 相关抗体:

Cell Proliferation Assay[2]

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[2]

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[2]

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
(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[2].
Conglobatin (4-8 mg/kg; i.p. daily for 21 days) inhibits tumor growth in EC109 and KYSE510 tumor xenograft models with low toxicity[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (nu/nu) athymic mice with SKBR3 and MCF-7 tumor xenograft[2]
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.
分子量

498.61

Formula

C28H38N2O6
CAS 号
性状

固体

颜色

White to off-white

结构分类
初始来源

Streptomyces conglobatus
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (100.28 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0056 mL 10.0279 mL 20.0558 mL
5 mM 0.4011 mL 2.0056 mL 4.0112 mL
查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Conglobatin 相关分类

完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0056 mL 10.0279 mL 20.0558 mL 50.1394 mL
5 mM 0.4011 mL 2.0056 mL 4.0112 mL 10.0279 mL
10 mM 0.2006 mL 1.0028 mL 2.0056 mL 5.0139 mL
15 mM 0.1337 mL 0.6685 mL 1.3371 mL 3.3426 mL
20 mM 0.1003 mL 0.5014 mL 1.0028 mL 2.5070 mL
25 mM 0.0802 mL 0.4011 mL 0.8022 mL 2.0056 mL
30 mM 0.0669 mL 0.3343 mL 0.6685 mL 1.6713 mL
40 mM 0.0501 mL 0.2507 mL 0.5014 mL 1.2535 mL
50 mM 0.0401 mL 0.2006 mL 0.4011 mL 1.0028 mL
60 mM 0.0334 mL 0.1671 mL 0.3343 mL 0.8357 mL
80 mM 0.0251 mL 0.1253 mL 0.2507 mL 0.6267 mL
100 mM 0.0201 mL 0.1003 mL 0.2006 mL 0.5014 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Conglobatin72263-05-9FW-04-806HSPApoptosisHeat shock proteinsmacrolidedilactoneStreptomycesconglobatusHsp90breastcanceresophagealsquamouscellcarcinomaantitumorInhibitorinhibitorinhibit

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