1. Protein Tyrosine Kinase/RTK Autophagy Apoptosis
  2. VEGFR Autophagy Apoptosis
  3. Coibamide A

Coibamide A 是一种 N-甲基稳定的细胞毒性缩酚肽,具有强大的抗增殖活性。Coibamide A 通过 mTOR 独立机制诱导自噬体积累。Coibamide A 诱导细胞凋亡。Coibamide A 抑制 VEGFA/VEGFR2 表达并抑制胶质母细胞瘤异种移植物中的肿瘤生长。

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Custom Peptide Synthesis

Coibamide A Chemical Structure

Coibamide A Chemical Structure

CAS No. : 1029227-48-2

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target[2]

VEGFR2

 

体外研究
(In Vitro)

Coibamide A (0.3-1 nM; 3-60 小时) 抑制 MDA-MB-231 乳腺癌细胞的增殖[1]
Coibamide A (2.3-230 nM; 3 天) 在人 U87-MG 和 SF-295 胶质母细胞瘤细胞中产生浓度和时间依赖性细胞毒性死亡[2]
Coibamide A (10-300 nM; 72 小时) 以细胞类型特异性的方式诱导 caspase-3/7 的激活和细胞凋亡[2]
Coibamide A (20 nM; 48 小时) 在抗凋亡的 U87-MG 细胞中诱导自噬体积累[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 0.3, 1 nM
Incubation Time: 3-60 hours
Result: Showed a steady concentration-dependent decrease in proliferative activity relative to vehicle-treated cells

Cell Cytotoxicity Assay[2]

Cell Line: U87-MG and SF-295 cells
Concentration: 2.3 to 230 nM
Incubation Time: 3 days
Result: Induced concentration-dependent cytotoxicity with EC50 values of 28.8 nM and 96.2 nM for U87-MG and SF-295 cells, respectively.

Apoptosis Analysis[2]

Cell Line: U87-MG and SF-295 cells
Concentration: 10-300 nM
Incubation Time: 72 h
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

Cell Autophagy Assay[2]

Cell Line: U87-MG cell
Concentration: 20 nM
Incubation Time: 48 h
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.
体内研究
(In Vivo)

Coibamide A (300 μg/kg; 瘤内注射; 前两天, 之后每 48 小时注射一次, 持续 35 天) 抑制胶质母细胞瘤皮下小鼠模型的肿瘤生长[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
分子量

1287.63

Formula

C65H110N10O16

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Coibamide A
目录号:
HY-P3990
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