DOLASTATIN 15
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： |
| 酸度系数(pKa) | 13.88±0.46(Predicted) |
| 形态 | 白色固体。 |
DOLASTATIN 15 用途与合成方法
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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.
