Coibamide A

Product Name: Coibamide A
CAS No.: 1029227-48-2
Chemical 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
CBNumber: CB44675240
Molecular Formula: C65H110N10O16
Formula Weight: 1287.65
MOL File: 1029227-48-2.mol

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Coibamide A Property

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

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Hazard and Precautionary Statements (GHS)

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Coibamide A Chemical Properties,Usage,Production

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

Coibamide A Preparation Products And Raw materials

Raw materials

Preparation Products

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Coibamide A Suppliers

China 4 Global 4

Shenzhen Yuzhong Pharmaceutical Technology Co., Ltd.

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Nextpeptide Inc

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Biosynth Biological Technology (Suzhou) Co Ltd

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Fuan Bio

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1029227-48-2, Coibamide ARelated Search:

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

1029227-48-2

C65H110N10O16