CONGLOBATIN
CONGLOBATIN Basic information
- Product Name:
- CONGLOBATIN
- Synonyms:
-
- (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
- FW-04-806
- CONGLOBATIN
- Conglobatin, >=99%
- 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)-
- Conglobactin
- (3E,5R,7S,8S,11E,13R,15S,16S)-3,5,7,11,13,15-hexamethyl-8,16-bis[(1,3-oxazol-5-yl)methyl]-1,9-dioxacyclohexadeca-3,11-diene-2,10-dione
- NGLOBATIN
- CAS:
- 72263-05-9
- MF:
- C28H38N2O6
- MW:
- 498.61
- Product Categories:
-
- Antibiotic
- Mol File:
- 72263-05-9.mol
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CONGLOBATIN Chemical Properties
- Density
- 1.060±0.06 g/cm3 (20 ºC 760 Torr)
- storage temp.
- -20°C
- solubility
- DMF: soluble; DMSO: soluble; Ethanol: soluble; Methanol: soluble
- form
- White to off-white solid.
- color
- White to off-white
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CONGLOBATIN Usage And Synthesis
Uses
Isolated from Streptomyces conglobatus, conglobatin has a unusual, dimeric, macrolide dilactone structure with pendant oxazole groups. Conglobatin exhibits an IC50 of 0.63 μg/ml in a NFAT-dependant transcription assay. No toxicity was observed at doses up to 1000 mg/kg when administered to mice either orally or interperitoneally.
Uses
Conglobatin is a macrolide dilactone from Streptomyces. It exhibits anticancer and immunosuppressant properties.
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]
| 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. |
IC 50
HSP90
CONGLOBATINSupplier
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