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ADC抗体药物偶联物可降解/不可降解连接物(linker)的说明
发布时间:2020-10-28    &nbsp作者:axc  &nbsp分享到:

ADC抗体药物偶联物可降解/不可降解连接物(linker)的说明

西安齐岳生物供应带有一系列可裂解的连接物(pH连接物,二硫键,肽连接物,β-葡萄糖苷酸连接物),不可裂解的接头和中间接头模块。

选择抗体药物偶联物连接物时,需要考虑将单抗与*素分子连接起来,这个连接一定要稳定,要保证ADC会断掉。其次,在ADC通过内化作用进入到细胞内部时,连接物要保证*素分子被释放出来。

目前开发中的ADC药物所采取的连接物可以分为两种类型:可降解连接物(Cleavable Linkers,下图a)和不可降解连接物(Non-Cleavable Linkers下图b)。

image.png

可降解连接物:可降解连接物又可根据不同的技术路线分为以下几类:

1.Acid-sensitive linkers:这类linker的关键部分是一个腙基(hydrazone groups)。

2.Glutathione(谷胱甘肽,GSH)-sensitive disulfide linkersGSH是一种小分子化合物,

3.Lysosomal protease-sensitive peptide linkers

4.β-glucuronide(葡糖苷酸) linker:β-葡糖苷酸是β-葡糖醛酸糖苷酶的底物

不可降解的连接物:

与可降解的linker相比,不可降解的linker显然更加稳定。含有不可降解linkerADC在通过内化作用进入到细胞内部时,细胞的溶酶体会将ADC的抗体部分降解掉,linker-drug复合物无法被降解,所以不可降解的linker要保证linker-drug复合物仍然能够具有损伤的能力。

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产品cas 产品名称
S-acetyl-PEG3-acid S-acetyl-PEG3-acid
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581065-97-6 SPDP-PEG-acid (PEG1-PEGn)
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133701-24-3 (2-pyridyldithio)-PEG1-hydrazine
874302-76-8 (2-pyridyldithio)-PEG1-PNB
581065-93-2 (2-pyridyldithio)-PEG4 acid
1305053-43-3 (2-pyridyldithio)-PEG4-NHS ester
2170240-99-8 (2-pyridyldithio)-PEG4-alkyne
2144777-73-9 (2-pyridyldithio)-PEG2-t-butyl ester
2100306-79-2 N-Boc-N-bis(PEG3-N3)
2112731-81-2 N-(N3-PEG2)-N-bis(PEG4-t-butyl ester)
2182602-15-7 N-(t-butyl ester-PEG3)-N-bis(PEG3-N3)
2086689-00-9 2-(N3-PEG3-amido)-1,3-bis(t-butyl ester)
2093153-07-0 N-(N3-PEG2)-N-Boc-PEG3-t-butyl ester
2093153-07-0  N-(N3-PEG2)-N-Boc-PEG3-t-butyl ester
2100306-63-4 N-(Boc-PEG1)-N-bis(PEG2-alkyne)
2112737-71-8 N-(Aminooxy-PEG2)-N-bis(PEG3-alkyne)
2112737-60-5 N-(t-Boc-Aminooxy-PEG2)-N-bis(PEG3-alkyne)
2100306-69-0 N-(t-butyl ester-PEG2)-N-bis(PEG2-alkyne)
2112732-01-9 N-(alkyne-PEG4-carbonyl)-N-bis(PEG1-methyl ester)
2112737-19-4 N-(Aminooxy-PEG3)-N-bis(PEG4-t-butyl ester)
2183440-74-4 N-(N3-PEG3)-N-(PEG2-NH-Boc)-PEG3-acid
2054339-01-2 N-Boc-N-bis(PEG2-acid)
2055046-22-3 N-Methyl-N-bis(PEG3-OH)
2112737-74-1 N-(Tos-PEG4)-N-bis(PEG4-t-butyl ester)
1393330-33-0 Bromo-PEG-acid (PEG1-PEGn)
1135131-50-8 Bromo-PEG-CH2CO2H (PEG1-PEGn)
1393330-36-3 Bromo-PEG-t-butyl ester (PEG1-PEGn)
157759-50-7 Bromo-PEG-CH2CO2tBu (PEG1-PEGn)
1144106-65-9 Bromo-PEG-N3 (PEG1-PEGn)
31255-10-4 Bromo-PEG-bromide (PEG1-PEGn)
110429-45-3 Bromo-PEG-methyl (PEG1-PEGn)
164332-88-1 Bromo-PEG-N-Boc (PEG1-PEGn)
203740-63-0 Bromo-PEG-alkyne (PEG1-PEGn)
57159-62-3 Bromoacetamido-PEG-NHS ester (PEG1-PEGn)
1353011-95-6 Chloroacetamido-PEG4-NHS ester
1365655-90-8 Chloroacetamido-PEG4-t-Butyl Ester
16024-60-5 Methyl-PEG-PEG-CH2COOH (PEG1-PEGn)
1778219-81-0 Methyl-PEG-t-butyl ester (PEG1-PEGn)
31576-51-9 Methyl-PEG-amine (PEG1-PEGn)
1263044-81-0 Methyl-PEG-maleimide (PEG1-PEGn)
89635-82-5 Methyl-PEG-alkyne (PEG1-PEGn)
50586-80-6 Methyl-PEG-tosyl (PEG1-PEGn)
441771-60-4 Methyl-PEG-thiol (PEG1-PEGn)
1449390-68-4 Methyl-PEG4-hydrazide
787524-78-1 Methyl-PEG4-sulfonic acid
105108-59-6 Methyl-PEG3-4-nitrophenyl carbonate
1835759-87-9 Methyl-PEG3-ONHBoc
557756-85-1 Fmoc-amino-PEG4-propanoic acid
1609651-90-2 Alkyne-PEG4-Maleimide
1621096-79-4 TCO-PEG4-NHS
1644644-96-1 Methyltetrazine NHS ester
112247-65-1 Biotin-NH-CH2CH2-S-S-Pyr
1151451-77-2 Benzaldehyde-PEG4-N3
2062663-64-1 Bromo-PEG6-N3
1313026-32-2 Folate-PEG3-N3
56282-36-1 HS-PEG3-OH
1146245-73-9 Mal-PEG2-oxyamine
2055041-37-5 Mal-PEG1-Val-Cit-PABC-OH
2249935-92-8 Mal-PEG1-Val-Cit-PABC-PNP
1870916-87-2 MC-Val-Ala-PAB
1639939-40-4 MC-Val-Ala-PAB-PNP
1951424-92-2 Fmoc-Ala-Ala-Asn(Trt)-OH
2098907-84-5 Acid-propionylamino-Val-Cit-OH
2055041-40-0 N3-PEG1-Val-Cit-PABC-OH
252378-67-9 Boc-Aminooxy-PEG2-bromide
1235514-18-7 Boc-aminooxy-PEG3-amine
1884578-00-0 Boc-Val-Ala-PAB-PNP
173323-22-3 Bromoacetamide-PEG3-acetic acid
932741-11-2 Bromoacetamide-PEG3-alkyne
1260139-70-5 Bromoacetamido-PEG4-NHS
1698019-89-4 Bromoacetamide-PEG8-acid
1803279-86-8 DBCO-C4-SulfoNHS ester
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1394238-91-5 Fmoc-Val-Ala-PAB
1394238-92-6 Fmoc-Val-Ala-PAB-PNP

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