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

Conglobatin  (Synonyms: FW-04-806)

製品番号: HY-119906 純度: 95.48%
COA 取扱説明書 Technical Support

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.

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Conglobatin

Conglobatin 構造式

CAS 番号 : 72263-05-9

容量 価格（税別） 在庫状況 数量
500 μg $210 在庫あり
1 mg $360 在庫あり
5 mg $938 在庫あり
10 mg $1500 在庫あり
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Conglobatin 関連抗体

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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製品説明

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

 

体外実験

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].

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

Conglobatin 関連抗体

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.
体内実験

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]

MedChemExpress (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

分子式

C28H38N2O6
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

C[C@@H](C[C@H](/C=C(C(O[C@H]1CC2=CN=CO2)=O)\C)C)[C@@H](OC(/C(C)=C/[C@@H](C[C@@H]1C)C)=O)CC3=CN=CO3
Structure Classification
Initial Source

Streptomyces conglobatus
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 50 mg/mL (100.28 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.2006 mL 1.0028 mL 2.0056 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

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In Vivo Dissolution Calculator
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純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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Conglobatin Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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