中文名称: 贝伐单抗
英文名称: Bevacizuab
CAS No: 216974-75-3
分子量: 149.14D
B10424 贝伐单抗 >95% (psaitong)
包装规格:
1mg
产品描述:

基本信息

产品编号:B10424

产品名称:Bevacizuab

CAS:

216974-75-3

 

储存条件

粉末

-20℃(避光)

四年

分子式:

 

分子量

149.14

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

 

Ethanol

 

Water

 

体内

现配现用

 

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。

 

 

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。

靶点/IC50

VEGFR2 
()

VEGF-A 
()

VEGF 
()

 

 

 

 

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

 

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。

特征

 

 

 

推荐实验方法(仅供参考)

细胞实验:

 

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.

 

 

 

动物实验:

 

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

保存条件:
-20℃ 避光
UN码:
HazardClass:
危害声明:
安全说明:
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摩尔浓度计算公式

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