中文名称: | 贝伐单抗 | ||||
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英文名称: | Bevacizuab | ||||
CAS No: | 216974-75-3 | 分子量: | 149.14D | ||
CAS No: | 216974-75-3 | ||||
分子量: | 149.14D |
基本信息
产品编号:B10424 |
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产品名称:Bevacizuab |
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CAS: |
216974-75-3 |
储存条件 |
粉末 |
-20℃(避光) |
四年 |
分子式: |
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分子量 |
149.14 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内 |
现配现用 |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
生物活性
产品描述 |
一种人源化的单克隆抗体,高亲和力且特异性地与所有 VEGF-A 结合。 |
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靶点/IC50 |
VEGFR2 |
VEGF-A |
VEGF |
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体外研究 |
人源VEGF的Gly88对bevacizumab的结合是基本必需的,同时也保证了bevacizumab结合的种属特异性,大鼠和小鼠的VEGF在该对应位置为丝氨酸残基。bevacizumab可与所有人源VEGF-A亚型(和具有生物活性的蛋白水解片段)结合、中和,而不中和其他VEGF基因家族成员,如VEGF-B或VEGF-C。 |
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体内研究 |
在人体中,bevacizumab的终末半衰期为17-21天。在裸鼠中,Bevacizumab抑制人源肿瘤细胞系的生长,在剂量为1-2mg/kg(一周给药两次)时,达到最大抑制作用。半最大抑制作用所需剂量为0.1-0.5mg/kg。在Macaca fascicularis (cynomolgus monkey)中对bevacizumab进行安全性评估研究,对其进行bevacizumab给药4-13周后,年轻成年的食蟹猴骨骺发育不良:肥大的软骨细胞剂量依赖式增多,生长区血管浸润受到抑制。长期bevacizumab的给药抑制了雌性系统的血管生长、卵巢和子宫的体重下降,黄体缺失。生长板和卵巢的改变为可逆性改变,停止治疗可逐渐恢复。除此以外,在药物浓度高达50mg/kg,也没有其他与给药相关的副作用被观察到。皮下注射后,rhuMAb VEGF(bevacizumab)在大鼠中的生物利用度为69%,而在小鼠和食蟹猴中为100%。Bevacizumab与灵长类VEGF结合,与兔子VEGF低亲和力结合,而不与大鼠、小鼠VEGF结合。 |
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特征 |
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推荐实验方法(仅供参考)
细胞实验: |
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Objective |
Effects of bevacizumab on VEGF-induced HUVEC proliferation |
Cells |
Human umbilical vein endothelial cells (HUVECs) |
Concentrations |
0~500ng/mL |
Incubation Time |
96h |
Method |
50ng/ml of rhVEGF was pre-incubated with a concentration range of bevacizumab (0-500ng/ml) for 2h before added to HUVACs. The plate was continuously incubated for 4 days. The proliferation of cells was determined by using Alamar Blue dye. |
Objective |
Cell proliferation assay |
Cells |
non small cell lung cancer (NSCLC), colorectal cancer (CRC), breast cancer (BC) and renal cell carcinoma (RCC) |
Concentrations |
250μg/ml |
Incubation Time |
24, 48, 72 or 96 hours |
Method |
Between 2×103 and 5×103 cells/well (cell line/doubling time dependent) are seeded into 96 well plates and incubated overnight to adhere. Medium is then replaced by RPMI-1640 with reduced FBS and bevacizumab or VEGFA at the concentrations indicated (time point zero). After 24, 48, 72 or 96 hours in hypoxia, MTT (5mg/ml in PBS) is added and incubated for 2 hours at 37°C. The supernatant is removed and reaction products are solubilized for 1 h in 10% HCl, 0.1% NP-40 in isopropanol. Absorbance is measured at 570nm with a reference wavelength of 650nm using an ELISA reader. Each experimental condition is analyzed in triplicate and results are an average of a minimum of three biological repetitions.
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动物实验: |
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Objective |
To determine the antitumor response of bevacizumab and cisplatin as single agents or in combination in xenograft models of ovarian cancer |
Animal Models |
Nude mice were injected (i.p.) with 5×106 A2780 cells |
Formulation |
PBS |
Dosages |
5mg/kg |
Administration |
i.p. |
Objective |
To determine the pharmacokinetics of bevacizumab |
Animal Models |
Female nude mice |
Dosages |
9.3 mg/kg |
Administration |
i.v.or s.c.injection |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )