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.
For research use only. We do not sell to patients.
- Purity: 95.48%
- CAS No.: 72263-05-9
- Formula: C28H38N2O6
- Molecular Weight:498.61
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HSP90 |
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.
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.
Chemical Information
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CAS No. 72263-05-9
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Appearance Solid
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Molecular Weight 498.61
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Formula 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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Synonyms
FW-04-806
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Structure Classification
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Initial Source
Streptomyces conglobatus
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 |
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| 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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