DOLASTATIN 15
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- CAS号:
- 123884-00-4
- 英文名:
- DOLASTATIN 15
- 英文别名:
- DLS 15;Nsc 617668;DOLASTATIN 15;(5S)-1-[(2S)-O-(N,N-VAL-VAL-N-ME-VAL-PRO-PRO)-2-HYDROXYISOVALERYL]-2-OXO-4-METHOXY-5-BENZYL-3-PYRROLINE;(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;(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-[(2S)-O-(N,N-Dimethyl-Val-Val-N-Me-Val-Pro-Pro)-2-hydroxyisovaleryl]-2-oxo-4-methoxy-5-benzyl-3-pyrroline;L-Proline, N,N-dimethyl-L-valyl-L-valyl-N-methyl-L-valyl-L-prolyl-, (1S)-1-[[(2S)-2,5-dihydro-3-methoxy-5-oxo-2-(phenylmethyl)-1H-pyrrol-1-yl]carbonyl]-2-methylpropyl ester;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*))-;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*))-
- 中文名:
- DOLASTATIN 15
- 中文别名:
- 多拉司他汀 15
- CBNumber:
- CB4385736
- 分子式:
- C45H68N6O9
- 分子量:
- 837.06
- MOL File:
- 123884-00-4.mol
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DOLASTATIN 15化学性质
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沸点:
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954.0±65.0 °C(Predicted)
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密度:
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1.20±0.1 g/cm3(Predicted)
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储存条件:
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−20°C
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溶解度:
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Methanol: soluble
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酸度系数(pKa):
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13.88±0.46(Predicted)
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形态:
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White solid.
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DOLASTATIN 15性质、用途与生产工艺
Dolastatin 15 (DLS 15)，一种从 Dolabella auricularia 中提取的去甲肽，是一种有效的抗有丝分裂剂 (antimitotic)，在结构上与抗微管蛋白剂 Dolastatin 10 有关。Dolastatin 15 诱导多发性骨髓瘤细胞周期阻滞和凋亡。Dolastatin 15 可作为 ADC 细胞毒素。
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.
DOLASTATIN 15
上下游产品信息
上游原料
下游产品
123884-00-4, DOLASTATIN 15 相关搜索:
- 药靶配体
- 目录肽
- 目录多肽
- 多肽
- BioChemical
- Cell Biology
- Cell Signaling and Neuroscience
- Cytoskeleton and Extracellular Matrix
- Microtobule Inhibitors
- C45H68N6O9
- 多拉司他汀 15
- 123884-00-4
- L-Proline, N,N-dimethyl-L-valyl-L-valyl-N-methyl-L-valyl-L-prolyl-, (1S)-1-[[(2S)-2,5-dihydro-3-methoxy-5-oxo-2-(phenylmethyl)-1H-pyrrol-1-yl]carbonyl]-2-methylpropyl ester
- DLS 15
- 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
- (5S)-1-[(2S)-O-(N,N-VAL-VAL-N-ME-VAL-PRO-PRO)-2-HYDROXYISOVALERYL]-2-OXO-4-METHOXY-5-BENZYL-3-PYRROLINE
- (5S)-1-[(2S)-O-(N,N-DIMETHYL-VAL-VAL-N-ME-VAL-PRO-PRO)-2-HYDROXYISOVALERYL]-2-OXO-4-METHOXY-5-BENZYL-3-PYRROLINE
- Nsc 617668
- 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*))-
- 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*))-
- (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
- DOLASTATIN 15