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Dolastatin 15, a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the anti-tubulin agent Dolastatin 10. Dolastatin 15 can be used as an ADC cytotoxin and it induces cell cycle arrest and apoptosis in multiple myeloma cells.
Dolastatin 15, a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the anti-tubulin agent Dolastatin 10. Dolastatin 15 can be used as an ADC cytotoxin and it induces cell cycle arrest and apoptosis in multiple myeloma cells.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
100 mg | 询价 | 期货 | |
500 mg | 询价 | 期货 |
产品描述 | Dolastatin 15, a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the anti-tubulin agent Dolastatin 10. Dolastatin 15 can be used as an ADC cytotoxin and it induces cell cycle arrest and apoptosis in multiple myeloma cells. |
体外活性 | Dolastatin 15 shows growth inhibitory activity against all four SCLC cell lines (NCI-H69, NCI-H82, NCI-H345, NCI-H446) (IC50: 0.039-28.8 nM), which were 2.7-9.2-fold higher than the values for dolastatin 10. Dolastatin 15 induces cell cycle arrest at the G2/M phase followed by apoptosis in various human myeloma cell lines (RPMI8226, U266, and IM9) and it also induces apoptosis of myeloma cells via activation of both mitochondrial- and Fas (CD95)/Fas-L (CD95-L)-mediated pathways [2]. All four SCLC cell lines underwent G2/M arrest within 24 hours of exposure to dolastatin 15 [4]. |
体内活性 | Dolastatin 15, using a non-cleavable linker, conjugates to Trastuzumab via lysine residues at the drug C-terminus. Trastuzumab-amide-C-term-Dol15 produced target-dependent growth inhibition of cells endogenously expressing high HER2 levels (i.e., SK-BR-3, SK-OV-3) in vitro. This ADC was effective at varying doses (i.e., 10 and 20 mg/kg) in the SK-OV-3 human ovarian cancer xenograft [3]. |
别名 | DLS 15 |
分子量 | 837.072 |
分子式 | C45H68N6O9 |
CAS No. | 123884-00-4 |
存储 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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