聚乙二醇衍生物偶联Cancer drugs方法和步骤

2017-5-11 0:06:55      点击:

聚乙二醇衍生物偶联Cancer drugs方法和步奏

对抗癌药物喜树碱进行的各种PEG修饰研究也已经进入临床试验。例如:研究人员在喜树碱的20-位羟基处进行PEG修饰,先将喜树碱与连接臂(氨基保护的甘氨酸)反应,再与PEG-乙酸通过酰胺键连接制备成前药,可以在体内缓慢释放出游离的喜树碱,使体内喜树碱的浓度维持较长时间,从而有效地杀伤癌细胞,并且明显表现出了被动靶向作用和缓控释作用.
PEG修饰喜树碱的合成路线:
 
 
采用mPEG修饰紫杉醇。先将PEG与丁二酸酐反应,引入活泼基团羧基,再用NHS进一步活化制备成PEG活性酯,并采用多种氨基酸作为连接臂,这种方法采用酯键和酰胺键连接载体和药物,易于水解。PEG-紫杉醇的合成路线见图。修饰后获得了优于紫杉醇的抑瘤活性,PEG修饰后的紫杉醇水溶性大大提高,而且体外急性毒性实验证明其不良反应也较紫杉醇改善了很多。其他关于PEG-紫杉醇前药的制备也被陆续报道。研究显示,经过适当PEG修饰后的紫杉醇较修饰前靶向性更强,而且具有更好的水溶性,提高了药物对肿瘤部位的选择性和治疗效果。
PEG-紫杉醇的合成路线:
 
上海炎怡生物科技有限公司在2008年提供定制合成PEG修饰剂的服务,我们提供国内种类最为齐全的PEG衍生物及PEG交联物产品,其产品种类多达3000多种,PEG分子量从350到40000不等,链接基团包括有氨基化PEG、羧基化PEG、生物素化PEG、马来酰亚胺PEG、巯基PEG、磷脂PEG、荧光PEG、电极化学PEG、聚合物PEG、多臂PEG及单分散PEG产品等,同时我们还可以为客户定制复杂PEG交联产品,我们将努力为广大客户提供种类最为齐全、产品质量最好、价格最据竞争力的PEG产品,我们将致力于打造中国第一PEG产品品牌。
 
产品概况:
mPEG-Amine             mPEG-NH2 MW:2000
Amine-PEG-Amine   NH2-PEG-NH2 ,MW:2000
Amine-PEG-Acid          NH2-PEG-COOH ,MW:2000
Amine-PEG-Thiol         NH2-PEG-SH ,MW:2000
Amine-PEG-Alkyne      NH2-PEG-Alkyne MW:2000
Iodoacetyl-PEG-Amine
Amine-PEG-FA
Biotin-PEG-Amine    Biotin-PEG-NH2
Maleimide-PEG-Amine        MAL-PEG-NH2
Amine-PEG-Silane        NH2-PEG-Silane
Amino-PEG-hydroxyl          NH2-PEG-OH
4 arm PEG Amine
8 arm PEG Amine
OPSS-PEG-NH2
Azide-PEG-Amine   N3-PEG-NH2
DBCO-PEG-Amine    DBCO-PEG-NH2 ,MW:2000
Fluorescein-PEG-Amine   FITC-PEG-NH2 ,MW:2000
Rhodamine-PEG-Amine     RB-PEG-NH2,MW:5000
DSPE-PEG-NH2, MW:2000
PLA(2000)-PEG(2000)-NH2
 
 
可用于药物偶联的PEG目录:
mPEG-NH2 MW:2000
NH2-PEG1000-NH2
NH2-PEG2000-COOH
NH2-PEG-SH ,MW:5000
NH2-PEG10000-Alkyne
NH2-PEG5000-VA,
NH2-PEG-Folate ,MW:2000
mPEG-NHS MW:2000
NHS-PEG-NHS ,MW:3400
NHS-PEG-ACLT ,MW:3400
NHS-PEG5000-MAL
VS-PEG-NHS,MW:2000
Acryloyl-PEG3400-NHS
Lipoic acid-PEG-NHS,MW:3400
Folate-PEG2000-NHS
mPEG-COOH,MW:750
COOH-PEG-COOH ,MW:550
COOH-PEG-MAL ,MW:2000
Iodoacetyl-PEG-COOH,MW:3400
Acryloyl-PEG-COOH,MW:3400
Lipoic acid-PEG-COOH,MW:5000
Alkyne-PEG2000-COOH
Biotin-PEG1000-COOH
Folate-PEG3400-COOH
mPEG- Biotin,MW:10000
Biotin-PEG-NHS ,MW:2000
Biotin-PEG5000-MAL
Biotin-PEG-NH2 ,MW:1000
Biotin-PEG2000-Biotin
Biotin-PEG-SC, MW:2000
Biotin-PEG-SVA, MW 2000
Biotin-PEG-OH, MW 2000
Biotin-PEG5000-Folate
mPEG-MAL MW:20000
MAL-PEG-MAL ,MW:5000
MAL-PEG-OH ,MW:3400
MAL-PEG-NH2 ,MW:2000
MAL-PEG-Alkyne MW:2000
MAL-PEG-OPSS,MW:5000
MAL-PEG-SH, MW:2000
MAL-PEG-Folate, MW:5000
mPEG-SH MW:1000
HS-PEG-SH ,MW:750
HS-PEG-COOH ,MW:2000
HS-PEG-SGA ,MW:3400
Alkyne-PEG-SH,MW:10000
HS-PEG-NHS  MW:2000
HS-PEG2000-Biotin
HS-PEG5000-Silane
HS-PEG2000-Folate
Mpeg1000- Silane
Silane-PEG3400-Silane
Silane-PEG2000-Biotin
Silane-PEG3400-NHS
Silane-PEG3400-COOH
NH2-PEG2000-Silane
MAL-PEG2000-Silane
HO-PEG2000-COOH
HO-PEG1000-NHS
HO-PEG3400-NH2
HO-PEG3400-OH
HO-PEG2000-Alkyne
HO-PEG1000-SH
TBOC-PEG5000-OH
FMOC-PEG3400-OH
TBOC-PEG2000-NH2
FMOC-PEG2000-NH2
TBOC-PEG3400-COOH
FMOC-PEG5000-COOH
TBOC-PEG3400-MAL
FMOC-PEG1000-MAL
TBOC-PEG2000-BIOTIN
FMOC-PEG2000-BIOTIN
TBOC-PEG20000-NHS
FMOC-PEG5000-NHS
4 arm PEG5000 Amine
4 arm PEG5000 COOH
4 arm PEG2000 NHS
4 arm PEG1000 SGA
4 arm PEG3400 MAL
4 arm PEG2000 SH
4 arm PEG2000 Biotin
4 arm PEG3400 Azide
4 Arm PEG1000 Alkyne
4 Arm PEG3400 OPSS
4 Arm PEG5000 Acrylate
8 arm PEG5000 NH2
8 arm PEG2000 COOH
8 arm PEG5000 MAL
8 arm PEG2000 SH
8 arm PEG Biotin
8 Arm PEG Acrylate
8 Arm PEG Hydrazide
8 Arm PEG Azide
8 Arm PEG Alkyne
OPSS-PEG2000-NHS
OPSS-PEG2000-OPSS
OPSS-PEG-SVA
OPSS-PEG-NH2
OPSS-PEG-COOH
OPSS-PEG-Biotin
OPSS-PEG-Silane
mPEG-N3
N3-PEG-N3
N3-PEG5000-NHS
N3-PEG2000-SH
N3-PEG3400-NH2
N3-PEG-OH
N3-PEG5000-MAL
N3-PEG2000-COOH
N3-PEG-Alkyne
N3-PEG-Biotin
N3-PEG-OPSS
N3-PEG-Silane
mPEG-DBCO
DBCO-PEG-NH2
DBCO-PEG-MAL
DBCO-PEG-NHS
DBCO-PEG-Biotin ,MW:2000
DBCO-PEG-Silane ,MW:2000
DBCO-PEG-Folate
DBCO-PEG-Cholesterol
mPEG-FITC
FITC-PEG-NHS
FITC-PEG-MAL
FITC-PEG-NH2
FITC-PEG-SH
FITC-PEG-COOH
FITC-PEG-Biotin
FITC-PEG-N3
FITC-PEG-Folate
FITC-PEG-Cholesterol
FITC-PEG-Alkyne
FITC-PEG-OPSS
FITC-PEG-FA
FITC-PEG-OH
mPEG-RB
RB-PEG-OH
RB-PEG-NH2
RB-PEG-COOH
RB-PEG-MAL
RB-PEG-NHS
RB-PEG-SH
RB-PEG-Biotin
CY3-PEG-NH2
CY3-PEG-COOH
CY3-PEG-NHS
CY3-PEG-SH, MW:2000
CY3-PEG-Biotin
CY5-PEG-NH2
CY5-PEG-COOH
CY5-PEG-NHS
CY5-PEG-SH, MW:2000
CY5-PEG-Biotin
mPEG2000-Dopamine
mPEG-SSA
mPEG-SS
mPEG-ALD
mPEG-Bromide
mPEG-Hyaluronate
AC-PEG-SCM
AC-PEG-NH2
Chloride-PEG-Chloride
Cholesterol-PEG-SH
Cholesterol-PEG-NHS
Cholesterol-PEG-Biotin
Cholesterol-PEG-MAL
Cholesterol-PEG-COOH
Cholesterol-PEG-NH2
mPEG-Cholesterol
mPEG-Cholesterol, MW:2000

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