DOLASTATIN 15
| 中文名称 | DOLASTATIN 15 |
|---|---|
| 中文同义词 | 多拉司他汀 15;化合物 Dolastatin 15 |
| 英文名称 | DOLASTATIN 15 |
| 英文同义词 | Dolastatin 15 (5S)-1-[(2S)-O-(N,N-Dimethyl-Val-Val-N-Me-Val-Pro-Pro)-2-hydroxyisovaleryl]-2-oxo-4-methoxy-5-benzyl-3-pyrroline;DOLASTATIN 15;(5S)-1-[N,N-Dimethyl-L-Val-L-Val-N-methyl-L-Val-L-Pro-L-Pro-L-Hyiv-]-5-benzyl-4-methoxy-1H-pyrrol-2(5H)-one;L-Proline, 1-(1-(N-(N-(N,N-dimethyl-L-valyl)-L-valyl)-N-methyl-L-valyl)-L-prolyl)-, 1-((2,5-dihydro-3-methoxy-5-oxo-2-(phenylmethyl)-1H-pyrrol-1-yl)carbonyl)-2-methylpropyl ester, (S-(R*,R*))-;L-Proline, 1-(1-(N-(N-(N,N-dimethyl-L-valyl)-L-valyl)-N-methyl-L-valyl)-L-propyl)-, 1-((2,5-dihydro-3-methoxy-5-oxo-2-(phenylmethyl)-1H-pyrrol-1-yl)carbonyl)-2-methylpropyl ester, (S-(R*,R*))-;Nsc 617668;(5S)-1-[(2S)-O-(N,N-DIMETHYL-VAL-VAL-N-ME-VAL-PRO-PRO)-2-HYDROXYISOVALERYL]-2-OXO-4-METHOXY-5-BENZYL-3-PYRROLINE;(5S)-1-[(2S)-O-(N,N-VAL-VAL-N-ME-VAL-PRO-PRO)-2-HYDROXYISOVALERYL]-2-OXO-4-METHOXY-5-BENZYL-3-PYRROLINE |
| CAS号 | 123884-00-4 |
| 分子式 | C45H68N6O9 |
| 分子量 | 837.06 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 123884-00-4.mol |
| 结构式 |  |
DOLASTATIN 15 性质
| 沸点 | 954.0±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.20±0.1 g/cm3(Predicted) |
| 储存条件 | −20°C |
| 溶解度 | 可溶于甲醇： |
| 形态 | 白色固体。 |
| 酸度系数(pKa) | 13.88±0.46(Predicted) |
|
Auristatin
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Dolastatin 15 (DLS 15) induces cell cycle arrest at the G2/M phase followed by apoptosis in various human myeloma cell lines (RPMI8226, U266, and IM9). Dolastatin 15 induces apoptosis of myeloma cells via activation of both mitochondrial- and Fas (CD95)/Fas-L (CD95-L)-mediated pathways.
Dolastatin 15 (DLS 15) displays growth inhibitory activity against all four SCLC cell lines (NCI-H69, NCI-H82, NCI-H345, NCI-H446) with IC
50
values ranging from 0.039-28.8 nM, which were 2.7-9.2-fold higher than the values for dolastatin 10. All four SCLC cell lines underwent G2/M arrest within 24 hours of exposure to dolastatin 15.
Dolastatin 15 conjugates to Trastuzumab via lysine residues at the drug C-terminus using a non-cleavable linker (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.
安全信息
| 安全说明 | 22-24/25 |
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| WGK Germany | 3 |
| 提供商 | 语言 |
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英文
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