Aldoxorubicin 文献数量:1
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| 包装规格: | 2mg 5mg 10mg in glass bottle |
| 溶解性: | 溶于DMSO(75 mg/mL 超声) |
| 产品描述: | 基本信息 产品编号: A11022 产品名称: Aldoxorubicin CAS: 1361644-26-9 储存条件 粉末 -20℃ 四年 分子式: C37H42N4O13 溶于液体 分子量 750.75 化学名: N-[(E)-[1-[(2S,4S)-4-[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-3,4-dihydro-1H-tetracen-2-yl]-2-hydroxyethylidene]amino]-6-(2,5-dioxopyrrol-1-yl)hexanamide Solubility (25°C): 体外: DMSO 55mg/mL (73.26mM; Need ultrasonic) Ethanol Water 体内(现配现用): 1.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline, Solubility:≥2.5mg/mL(3.33mM);Clear solution 此⽅案可获得≥2.5mg/mL(3.33mM,饱和度未知)的澄清溶液。以1mL⼯作液为例,取100μL25.0mg/mL的澄清DMSO储备液加到400μLPEG300中,混合均匀;向上述体系中加⼊50μLTween-80,混合均匀;然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 2.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility:≥2.5mg/mL(3.33mM);Clear solution 此⽅案可获得≥2.5mg/mL(3.33mM,饱和度未知)的澄清溶液。以1mL⼯作液为例,取100μL25.0mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中,混合均匀。 3.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility:≥2.5mg/mL(3.33mM);Clear solution 此⽅案可获得≥2.5mg/mL(3.33mM,饱和度未知)的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例,取100μL25.0mg/mL的澄清DMSO储备液加到900μL⽟⽶油中,混合均匀。 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 1.3320mL 6.6600mL 13.3200mL 5mM 0.2664mL 1.3320mL 2.6640mL 10mM 0.1332mL 0.6660mL 1.3320mL 生物活性 产品描述 一种多柔比星的白蛋白结合前药,在酸性条件下从白蛋白中释放出来。 靶点 Topoisomerase II Daunorubicins/Doxorubicins 体外研究 Aldoxorubicin (INNO-206) (0.27 to 2.16μM) inhibits blood vessel formation and reduces multiple myeloma cell growth in a pH-dependent fashion 体内研究 Aldoxorubicin (INNO-206) (10.8mg/kg, i.v.) shows significantly smaller tumor volumes and IgG levels on days 28, and is well tolerated with 90% of mice surviving until the termination of the study in the mice bearing the LAGκ-1A tumor . Aldoxorubicin (INNO-206) shows a good safety profile at doses up to 260mg/mL doxorubicin equivalents, and is able to induce tumor regressions in breast cancer, small cell lung cancer and sarcoma in phase I study. Aldoxorubicin (INNO-206) shows superior activity over doxorubicin in a murine renal cell carcinoma model and in breast carcinoma xenograft models 推荐实验方法(仅供参考) Cell Assay Cells are seeded at 1×105 cells/100μL/well in 96-well plates in RPMI-1640 media with FBS for 24 hours before treatment. Cells are cultured in the presence of medium, Aldoxorubicin (INNO-206) or doxorubicin for 48 hours. Next, cell viability is quantified using the CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay. Each well is treated with MTS for 1 to 4 hours, after which absorbance at 490 nm is recorded using a 96-well plate reader. The quantity of formazan product as measured is directly proportional to the number of living cells. Data graphed are means±SEM using 3 replicates per data point Animal Administration For the LAGκ-1A experiment, Aldoxorubicin (INNO-206) is administered to SCID mice at 10.8mg/kg (doxorubicin equivalent dose of 8.0mg/kg) once weekly. Mice are treated with conventional doxorubicin at 4.0 and 8.0mg/kg once weekly. For the LAGκ-2 experiment, Aldoxorubicin (INNO-206) is administered once weekly (W) at doses of 2.7 and 5.4mg/kg, or on 3 consecutive days (W-F) weekly at doses of 0.9 and 1.8mg/kg. PS-341 is administered twice weekly (W, F) at a dose of 0.5mg/kg. Doxorubicin is administered to SCID mice at 2, 4, and 8mg/kg, and PLD is administered to SCID mice at 2mg/kg once weekly. Each drug is administered i.v. in a volume of 100μL |
| 保存条件: | -20℃ |
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