Coibamide A
Coibamide A Basic information
- Product Name:
- Coibamide A
- Synonyms:
-
- Coibamide A
- D-Alanine, N,N-dimethyl-L-valyl-(2R)-2-hydroxy-3-methylbutanoyl-N,O-dimethyl-L-seryl-N-methyl-L-leucyl-N-methyl-L-threonyl-N,O-dimethyl-L-seryl-N-methyl-L-isoleucyl-L-alanyl-N-methyl-L-leucyl-O-methyl-L-tyrosyl-N-methyl-, (11→5)-lactone
- CAS:
- 1029227-48-2
- MF:
- C65H110N10O16
- MW:
- 1287.65
- Mol File:
- 1029227-48-2.mol
Coibamide A Chemical Properties
- Boiling point:
- 1255.2±65.0 °C(Predicted)
- Density
- 1.18±0.1 g/cm3(Predicted)
- pka
- 13.26±0.70(Predicted)
- Sequence
- {NMe-Val}-{Hiv}-{NMe-Ser}-{NMe-Leu}-{NMe-Thr}-{NMe-Ser}-{NMe-Ile}-{NMe-Ala}-{NMe-Leu}-{NMe-Tyr}-{NMe-Ala} lactone bridge:Thr5-Ala11
Coibamide A Usage And Synthesis
Uses
Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A induces autophagosome accumulation via an mTOR-independent mechanism. Coibamide A induces apoptosis. Coibamide A inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts[1][2].
in vivo
Coibamide A (300 μg/kg; intratumoral injections; for the first two days, and then every 48 h afterward for 35 days) inhibits tumor growth in a subcutaneous mouse model of glioblastoma[1].
| Animal Model: | 8-week old female nude athymic mice with U87-MG cells[1] |
| Dosage: | 300 μg/kg |
| Administration: | Intratumoral injections; for the first two days, and then every 48 h afterward for 35 days |
| Result: | Remained stable at 200-300 mm3 without significant growth over 4 weeks of treatmen, whereas the tumors of vehicle-treated animals continued to grow at a steady rate consistent with this aggressive cancer cell type |
IC 50
VEGFR2
References
[1] Jeffrey D Serrill, et al. Coibamide A, a natural lariat depsipeptide, inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts. Invest New Drugs. 2016 Feb;34(1):24-40. DOI:10.1007/s10637-015-0303-x
[2] Andrew M Hau, et al. Coibamide A induces mTOR-independent autophagy and cell death in human glioblastoma cells. PLoS One. 2013 Jun 6;8(6):e65250. DOI:10.1371/journal.pone.0065250
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