Conglobatin
Based on 1 Customer Validation
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 95.0%
- CAS 番号: 72263-05-9
- 分子式: C28H38N2O6
- 分子量:498.61
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
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.
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Cell Line:SKBR3 and MCF-7 cells
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Concentration:6.25, 12.5, 25, 50, 100 μM
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Incubation Time:48 hours
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Result:Inhibited the proliferation of SKBR3 and MCF-7 cells in a dose-dependent manner.
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Cell Line:SKBR3 and MCF-7 cells
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Concentration:10, 20, 40 μM
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Incubation Time:24 hours
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Result:Increased the G2/M cell population and decreased the population in the S and G0/G1 phases.
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Cell Line:SKBR3 and MCF-7 cells
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Concentration:10, 20, 40 μM
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Incubation Time:3, 6, 12, 24 hours
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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 (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.
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Animal Model:BALB/c (nu/nu) athymic mice with SKBR3 and MCF-7 tumor xenograft[2]
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Dosage:50, 100, 200 mg/kg
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Administration:Oral gavage every 3 days for 24 days
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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.
化学情報
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CAS 番号 72263-05-9
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性状 Solid
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分子量 498.61
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分子式 C28H38N2O6
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Color White to off-white
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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
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別名
FW-04-806
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Structure Classification
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Initial Source
Streptomyces conglobatus
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Westley JW, et, al. Conglobatin, a novel macrolide dilactone from Streptomyces conglobatus ATCC 31005. J Antibiot (Tokyo). 1979 Sep;32(9):874-7. [Content Brief]
[2]. Huang W, et, al. FW-04-806 inhibits proliferation and induces apoptosis in human breast cancer cells by binding to N-terminus of Hsp90 and disrupting Hsp90-Cdc37 complex formation. Mol Cancer. 2014 Jun 14;13:150. [Content Brief]
[3]. Li LY, et, al. Macrolide analog F806 suppresses esophageal squamous cell carcinoma (ESCC) by blocking β1 integrin activation. Oncotarget. 2015 Jun 30;6(18):15940-52. [Content Brief]
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 |
Conglobatin 関連分類
HY-119906 関連分類
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