Coibamide A
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.
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- CAS No.: 1029227-48-2
- Formule: C65H110N10O16
- Masse moléculaire:1287.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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VEGFR2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1.4 nM
Compound: 1; CbA
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Cytotoxicity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
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[PMID: 35059129] |
| MDA-MB-231 | IC50 |
66 nM
Compound: Coibamide A
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Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
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[PMID: 25488840] |
| NCI-H292 | IC50 |
124 nM
Compound: Coibamide A
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Cytotoxicity against human NCI-H292 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human NCI-H292 cells assessed as growth inhibition after 72 hrs by MTT assay
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[PMID: 25488840] |
| PANC-1 | GI50 |
3.1 nM
Compound: 1
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Growth inhibition of human PANC1 cells incubated for 72 hrs by MTT assay
Growth inhibition of human PANC1 cells incubated for 72 hrs by MTT assay
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[PMID: 30247036] |
| PC-3 | IC50 |
80 nM
Compound: Coibamide A
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Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay
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[PMID: 25488840] |
| SF-295 | IC50 |
219 nM
Compound: Coibamide A
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Cytotoxicity against human SF295 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human SF295 cells assessed as growth inhibition after 72 hrs by MTT assay
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[PMID: 25488840] |
Coibamide A (0.3-1 nM; 3-60 hours) inhibits proliferation of MDA-MB-231 breast cancer cells[1].
Coibamide A (2.3-230 nM; 3 days) produces concentration- and time-dependent cell death in human U87-MG and SF-295 glioblastoma cells[2].
Coibamide A (10-300 nM; 72 h) induces activation of caspase-3/7 and apoptosis in a cell type-specific manner[2].
Coibamide A (20 nM; 48 h) induces autophagosome accumulation in apoptotic-resistant U87-MG cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 breast cancer cells
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Concentration:0.3, 1 nM
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Incubation Time:3-60 hours
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Result:Showed a steady concentration-dependent decrease in proliferative activity relative to vehicle-treated cells
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Cell Line:U87-MG and SF-295 cells
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Concentration:2.3 to 230 nM
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Incubation Time:3 days
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Result:Induced concentration-dependent cytotoxicity with EC50 values of 28.8 nM and 96.2 nM for U87-MG and SF-295 cells, respectively.
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Cell Line:U87-MG and SF-295 cells
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Concentration:10-300 nM
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Incubation Time:72 h
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Result:An 89 kDa band corresponding to the caspase 3-cleaved form of PARP1 was readily detected by 48 h indicative of apoptotic cell death in SF-295 cells, whereas only trace levels of this fragment were observed in late, detaching U87-MG cell lysates
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Cell Line:U87-MG cell
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Concentration:20 nM
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Incubation Time:48 h
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Result:Caused a clear increase in LC3-II expression by 1 h, and this increase in LC3-II expression was generally sustained through 48 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:8-week old female nude athymic mice with U87-MG cells[1]
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Dosage:300 μg/kg
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Administration:Intratumoral injections; for the first two days, and then every 48 h afterward for 35 days
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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
Chemical Information
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CAS No. 1029227-48-2
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Masse moléculaire 1287.63
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Formule C65H110N10O16
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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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Sequence Shortening
{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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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