带有断裂连接子和非断裂连接子Linker偶联小分子化科研ADCs介绍
作者:zhn
发布时间:2022-09-02
19:07:20
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产品名称:带有断裂连接子和非断裂连接子Linker偶联小分子化科研ADCs介绍
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带有断裂连接子和非断裂连接子Linker偶联小分子化科研ADCs介绍 抗体-科研偶联物(ADCs)是一类重要的靶向生物科研。ADCs由单克隆抗体和细胞性科研(小分子化)组成,通过半、赖氨酸或其他工程化残基,通过多种连接子(linker)连接在一起。因此,可以实现ADC作为化疗科研的性递送至细胞,从而靶位点的药理活性,同时使非靶免受化疗损伤,由于ADCs的结构复杂,其稳定性要求过了分子各部分的简单总和,因为单克隆抗体、小分子化和连接子的稳定性对ADCs的性、和潜在的抗科研抗体(ADA)反应都有影响,此外,由于其小分子化的独*力,ADCs在性、性和稳定性方面满足一些苛刻的标准,以实现将细胞性科研且选择性地递送至靶点。 偶联小分子化被定义为与抗体偶联的小分子化。偶联小分子化活性ADC科研成分,是亲和力捕获-LC-MS分析中可能的分析物,这使得具有变化DAR的ADC能定量偶联小分子化。越来越多的人对测量循环中的偶联小分子化以定义ADC的峰值感兴趣。 小分子化通过连接子与抗体偶联,连接子是ADC的重要组成部分。连接子可以是不同类型的,例如腙(hydrazone)连接子、二硫化物(disulfide)连接子和断裂或非断裂的肽连接子。这些连接子释放活性小分子化的方式在体内有的不同。腙连接子对pH敏感,在较低pH下,通过在包涵体和/或溶酶体等隔间中断裂释放活性小分子化。二硫键利用细胞内的还原环境释放小分子化。已知断裂的肽连接子被溶酶体蛋白酶酶切,而非断裂的连接子通过溶酶体隔间中抗体的降解释放活性小分子化。近发现基于肽的连接子(断裂和非断裂)更常用,因为它们显示出更高的血浆稳定性和更高的活性。总体而言,由于代ADC中使用了化学不稳定的肼和某些二硫键,通过创建酶促断裂和非断裂的连接子,连接子稳定性得到了。二硫键的化学性质也随着保护基团的引入而得到,例如,链间二硫键的减少,随后加入含有炔基的二硫代苯基马来酰亚胺键,使得能够与含有叠氮化物基团的小分子化偶联。 连接子部分的特征在很上决定了偶联小分子化生物分析的分析策略。例如,根据连接子是否可断裂,采用不同的样品制备方法。如果连接子是可断裂 (如二肽型可切割连接蛋白),则溶酶体酶(如蛋白酶B)能够性地切割连接蛋白,释放小分子化用于LC-MS检测,这是在抗性mAb亲和捕获法从基质中捕获ADCs后实现的。如果连接子不可断裂,而该酶不能从连接子上断裂小分子化,那么在从基质中捕获抗性单克隆抗体后,将应用抗体的蛋白酶(例如胰蛋白酶)消化,并且肽偶联的小分子化是由LC-MS/MS检测的替代分析物(图1)。基于抗性单克隆抗体捕获的LC-MS/MS分析能够检测与单克隆抗体偶联的小分子化。然而,如果使用抗小分子化单克隆抗体作为捕获试剂,可检测样品中潜在的类型小分子化分子,包括未偶联的小分子化、与单克隆抗体偶联的小分子化、与连接子偶联的小分子化以及与小分子化偶联的单克隆抗体的分解代谢物。 图1带有断裂连接子和非断裂连接子的ADCs上偶联小分子化定量分析的样品制备以及SIL‐IS选项流程 西安齐岳生物提供了多种化学用途的接头分子,以抗体-科研偶联物(ADC)研究项目。化学连接剂的纯度均> 95%,是成功ADC的基本组成部分,齐岳生物提供的ADC-linker抗体偶联科研均,可咨询订购。 cas:799840-96-3|DM4|含硫醇美登素衍生物 cas:139504-50-0|Mertansine|DM1 cas:57103-68-1|Maytansinol|美登醇 Maytansinoid AP-3|66547-09-9出售 cas:228266-40-8/HTI-286/抗微管剂 cas:745017-94-1/MMAF/微管蛋白聚合剂 Auristatin F/163768-50-1/澳瑞他汀F cas:474645-27-7/MMAE/抗体偶联科研ADC cas:160800-57-7/Auristatin E cas110417-88-4尾海兔素Dolastatin10 PHA-tetra-EG-OPFP抗体科研偶联物ADC PHA-di-EG-OPFP抗体科研偶联物ADC ALD-tetra-EG-OPFPADCLinker ALD-di-EG-OPFP抗体科研偶联物 ALD-di-EG-OSu抗体科研偶联物ADC ALD-BZ-OSu抗体科研偶联物 N3-tetra-EG-OPFP抗体科研偶联物 N3-tri-EG-OPFP抗体科研偶联物ADC N3-di-EG-OPFP抗体科研偶联物ADC-Linker MAL-tetra-EG-OPFP/ADC抗体科研偶联物 MAL-di-EG-OPFP抗体偶联科研ADC连接子定制 Protein G-Amanitin蛋白G预载鹅膏糖蛋白 Protein G-Duocarmycin双卡霉素预载蛋白G Protein G-MMAE可切割连接体 Protein G-DM1蛋白G预载MCC-DM1出售 ADCpre-screening kitGA预载连接器 Protein A-PBD/PBD预载蛋白A Protein A-Calicheamicin可切割连接体 Protein A-Duocarmycin双卡霉素预载蛋白A Protein A-MMAE可切割连接体 Protein A-DM1不可切割连接体- ADCpre-screening kitA预载A试剂盒 PNU159682-EDA-Gly3抗体科研偶联物ADC Gly3-MMAF|Gly5-Ahx-DM1ADC Gly3-vc-PAB-MMAE抗体科研偶联物ADC出售 DBCO-PEG8-VA-PAB-SG3199 DBCO-PEG4-vc-PAB-Ahx-DM1 DBCO-PEG4-GGFG-DX8951 DBCO-PEG4-DMAE-PNU159682 DBCO-PEG4-vc-PAB-MMADADC DBCO-PEG4-vc-PAB-MMAF DBCO-PEG4-VA-PBD抗体科研偶联物ADC产品 DBCO-PEG4-Ahx-DM1抗体科研偶联物 DBCO-PEG4-MMAF抗体科研偶联物ADC连接子 DBCO-PEG4-vc-PAB-MMAE抗体科研偶联物 MPB-MMAF抗体科研偶联物ADC MPB-vc-PAB-MMAE抗体科研偶联物ADC DGN549抗体偶联科研ADC MEDI4276 linker payload cas1600418-29-8/MC-GGFG-DX8951 CAS:1279680-68-0 /CL2A-SN 38 MA-PEG8-VA-PAB-SG3199齐岳试剂 MC-vc-PAB-Auristatin 0101 MC-vc-PAB-MMAD抗体科研偶联物 MA-PEG4-VA-PBD/CAS:863971-17-9 Boc-Val-Dil-Dap-OH抗体科研偶联物连接子 Boc-Val-Dil-Dap-Phe-OMe抗体科研结合物 Boc-Val-Dil-Dap-Doe抗体科研偶联物连接子 Boc-Val-Dil-Dap-Nrp抗体科研偶联物ADC Boc-N-Me-Val-Val-Dil-Dap-OH CAS1943604-24-7/Tubulysin IM-1 CAS1943604-24-7/Tubulysin IM-2 Tubulysin IM-3/CAS1639986-05-2 cas:157922-77-5/Duocarmycin TM cas1613286-57-9/Duocarmycin MA Duocarmycin DM抗体科研偶联物ADC素 cas108852-90-0奈莫柔比星Nemorubicin cas:202350-68-3/PNU-159682 cas108212-75-5/Calicheamicing1 cas:108212-76-6高活性抗的齐岳 cas:23109-05-9/a-Amanitin/α伞肽 cas:1222490-34-7/PBD-dimer齐岳厂家 OSu-Glu-vc-PAB-MMAE齐岳生物 cas:1228105-51-8/SMCC-DM1 CAS:1626359-62-3 /SPDB-DM4 Mylotarg-linker抗体科研偶联物素 OSu-Glu-vc-PAB-MMAD齐岳 sulfo-SPDB-DM4/CAS1626359-59-8 IMGN779-linker齐岳生物 CAS:646502-53-6/MC-vc-PAB-MMAE cas: 863971-19-1/MC-MMAF MC-vc-PAB-C6-a-amanitin抗体科研偶联物 MC-cleavable-linker-a-amanitin MC-vc-PAB-Tubulysin M cas:2100306-76-9 N-(N3-PEG3)-N-Biotin-PEG4-methyl ester cas:2353409-61-5 N-Desthiobiotin-N-bis(PEG4-NHS ester) cas:2353409-60-4 N-Desthiobiotin-N-bis(PEG4-t-butyl ester) cas:760952-64-5 Maleimide-PEG-Acid (PEG1-PEGn) cas:1807518-72-4 Maleimide-PEG-NHS ester (PEG1-PEGn) cas:660843-22-1 Maleimide-PEG2-amine cas:660843-21-0 Maleimide-PEG2-NH-Boc cas:2182602-20-4 Maleimide-amido-PEG9-NHBoc cas:756525-98-1 Maleimide-amido-PEG-Acid (PEG1-PEGn) cas:2182602-22-6 Maleimide-amido-PEG9-amine cas:955094-26-5 955094-26-5 cas:1431291-44-9 Maleimide-amido-PEG-TFP ester (PEG1-PEGn) cas:7423-55-4 3-Maleimidopropionic acid cas:731862-92-3 Maleimide-C6-amine TFA salt cas: 1823885-81-9 Maleimide-PEG1-Bromide cas:55750-62-4 3-Maleimido-propionic NHS ester cas:55750-63-5 Maleimide-heptanoic NHS ester cas:692739-25-6 6-Maleimidocaproic acid PFP ester cas:1807534-86-6 3,4-Dibromo-Maleimide-PEG2-Amine TFA salt cas:1807537-43-4 3,4-Dibromo-Maleimide-PEG2-Boc-Amine cas:2128735-20-4 N-Maleimide-N-bis(PEG2-amine) TFA salt cas:2128735-22-6 N-Maleimide-N-bis(PEG4-amine) TFA salt cas:2182601-73-4 N-Maleimide-N-bis(PEG2-NHS ester) cas:2112738-60-8 N-Maleimide-N-bis(PEG4-NHS ester) cas:2128735-26-0 2128735-26-0 cas:2100306-51-0 N-Maleimide-N-bis(PEG2-t-butyl ester) cas:5961-83-1 Acid-PEG-acid (PEG1-PEGn) cas:23243-68-7 PEG-(CH2CO2H)2 (PEG1-PEGn) cas: 2062663-61-8 Acid-PEG-NHS ester (PEG1-PEGn) cas:1807521-05-6 Fmoc-PEG-NHS ester (PEG1-PEGn) cas:2128735-25-9 Fmoc-PEG3-CH2CO2-NHS ester cas:2228857-30-3 Fmoc-NMe-PEG4-NHS ester cas:1027371-75-0 Methyl-PEG-NHS ester (PEG1-PEGn) cas:2144777-76-2 Alkyne-PEG4-CH2CO2-NHS cas:1260092-55-4 t-Boc-N-amido-PEG1-NHS ester cas:1835759-75-5 t-Butoxycarbonyl-PEG4-NHS ester cas:2320560-36-7 2-(N3-PEG3-amido)-1,3-bis(NHS Ester) cas:2093153-85-4 N-(N3-PEG2)-N-Boc-PEG3-NHS ester cas:2182601-73-4 N-Maleimide -N-bis(PEG2-NHS ester) cas:2128735-29-3 N-DBCO-N-bis(PEG2-NHS ester) cas:2055042-31-2 N-Boc-N-bis(PEG3-NHS ester) cas:1333154-70-3 NHS-PEG4-(Methyl-PEG4)3-ester cas:2141981-86-2 TCO-PEG-acid (PEG1-PEGn) cas:2141981-88-4 TCO-PEG-NHS ester (PEG1-PEGn) cas:2353409-48-8 TCO-PEG2-Sulfo-NHS ester cas:2353410-06-5 TCO-PEG8-TFP ester cas:1438415-89-4 TCO-PNB ester cas:2141981-87-3 TCO-PEG-amine (PEG1-PEGn) cas:2183440-30-2 TCO-PEG4-biotin cas:1801863-88-6 TCO-PEG4-DBCO cas:2183440-37-9 TCO-PEG9-maleimide cas:2250217-32-2 TCO-PEG3-triethoxysilane cas:2243569-22-2 TCO-PEG-TCO (PEG1-PEGn) cas:2353409-81-9 Gly-Gly-Gly-PEG3-TCO cas:1802908-05-9 Methyltetrazine-PEG4-amine cas:1802907-91-0 Methyltetrazine-PEG-acid (PEG1-PEGn) cas:1616668-55-3 Tetrazine-NHS ester cas:1644644-96-1 Methyltetrazine-NHS ester cas:1682653-80-0 Tetrazine-PEG5-NHS ester cas:1802907-92-1 Methyltetrazine-PEG5-NHS ester cas:2353409-49-9 Methyltetrazine-PEG8-PFP ester cas:1802907-97-6 Methyltetrazine-PEG5-alkyne cas:1802908-04-8 Methyltetrazine-PEG4-N3 cas:1835759-81-3 Methyltetrazine-PEG4-biotin cas:2183440-28-8 Methyltetrazine-PEG12-DBCO cas:1802238-48-7 Methyltetrazine-DBCO cas:1802908-02-6 Methyltetrazine-PEG4-maleimide cas:2194563-84-1 Methyltetrazine-PEG4-NH-Boc cas:2183440-38-0 Methyltetrazine-PEG12-t-butyl ester cas:2353410-01-0 Methyltetrazine-PEG5-triethoxysilane cas:2353409-82-0 Gly-Gly-Gly-PEG4-methyltetrazine cas:139115-91-6 N-Boc-PEG-alcohol (PEG1-PEGn) cas:164332-88-1 N-Boc-PEG-bromide (PEG1-PEGn) cas:475591-59-4 Boc-NH-PEG2-NH-Boc cas:1260431-01-3 N-methyl-N-(t-Boc)-PEG4-acid cas:869310-84-9 t-Boc-N-amido-PEG-alkyne (PEG1-PEGn) cas:1817735-32-2 t-Boc-N-amido-PEG3-sulfonic acid cas:671802-00-9 Hydroxy-PEG-t-butyl ester (PEG1-PEGn) cas:287174-32-7 Hydroxy-PEG-CH2CO2tBu (PEG1-PEGn) cas:1820673-42-4 Hydroxy-PEG2-PFP ester cas:112724-27-3 Hydroxy-PEG2-sulfonic acid cas:1807512-36-2 N3-PEG3-(CH2)3OH cas:2228857-31-4 3-(N3-PEG5-amino)alkyne cas:57641-66-4 Bromo-PEG alcohol (PEG1-PEGn) cas:100688-48-0 Methyl-PEG-(CH2)3OH (PEG1-PEGn) cas:112-27-6 Hydroxy-PEG-hydroxy (PEG1-PEGn) cas:93673-82-6 Hydroxy-PEG-methyl ester (PEG1-PEGn) cas:54384-47-3 NH-bis(PEG-OH) (PEG1-PEGn) cas:2100306-85-0 N-(PEG1-OH)-N-Boc-PEG2-alkyne cas:2100306-77-0 Hydroxy-Amino-bis(PEG2-alkyne) cas:2100306-62-3 N-(alkyne-PEG2)-N-bis(PEG1-alcohol) cas:1398044-52-4 2-(N3-PEG2-amido)-1,3-propandiol cas:1415800-34-8 Hydroxy-Amino-bis(PEG1-t-butyl ester) cas:146651-71-0 N-Boc-Tris cas:2093154-01-7 N-Boc-N-bis(PEG3-OH) cas:2055042-60-7 N-(Boc-PEG3)-N-bis(PEG2-alcohol) cas:119580-47-1 N-Benzyl-N-bis(PEG1-OH) cas:1807539-02-1 Bis-PEG-PFP ester (PEG1-PEGn) cas:1347750-82-6 Thiol-PEG-acid (PEG1-PEGn) cas:1446282-39-8 Thiol-PEG3-t-butyl ester cas:1347750-79-1 Thiol-PEG3-N3 cas:1360716-36-4 Thiol-PEG3-phosphonic acid cas:441771-60-4 Thiol-PEG3-methyl cas:1314378-10-3 Lipoamido-PEG-acid (PEG1-PEGn) cas:1674386-82-3 Lipoamido-PEG2-alcohol cas:890016-39-4 Lipoamido-PEG3-N3 cas:1314378-19-2 Lipoamido-PEG3-maleimide cas:S-acetyl-PEG3-acid S-acetyl-PEG3-acid cas:1818294-25-5 S-acetyl-PEG6-tosyl cas:581065-97-6 SPDP-PEG-acid (PEG1-PEGn) cas:1334177-95-5 SPDP-PEG-NHS-ester (PEG1-PEGn) cas:851961-99-4 (2-pyridyldithio)-PEG4-alcohol cas:133701-24-3 (2-pyridyldithio)-PEG1-hydrazine cas:874302-76-8 (2-pyridyldithio)-PEG1-PNB cas:581065-93-2 (2-pyridyldithio)-PEG4 acid cas:1305053-43-3 (2-pyridyldithio)-PEG4-NHS ester cas:2170240-99-8 (2-pyridyldithio)-PEG4-alkyne cas:2144777-73-9 (2-pyridyldithio)-PEG2-t-butyl ester cas:2100306-79-2 N-Boc-N-bis(PEG3-N3) cas:2112731-81-2 N-(N3-PEG2)-N-bis(PEG4-t-butyl ester) cas:2182602-15-7 N-(t-butyl ester-PEG3)-N-bis(PEG3-N3) cas:2086689-00-9 2-(N3-PEG3-amido)-1,3-bis(t-butyl ester) cas:2093153-07-0 N-(N3-PEG2)-N-Boc-PEG3-t-butyl ester cas:2100306-63-4 N-(Boc-PEG1)-N-bis(PEG2-alkyne) cas:2112737-71-8 N-(Aminooxy-PEG2)-N-bis(PEG3-alkyne) cas:2112737-60-5 N-(t-Boc-Aminooxy-PEG2)-N-bis(PEG3-alkyne) cas:2100306-69-0 N-(t-butyl ester-PEG2)-N-bis(PEG2-alkyne) cas:2112732-01-9 N-(alkyne-PEG4-carbonyl)-N-bis(PEG1-methyl ester) cas:2112737-19-4 N-(Aminooxy-PEG3)-N-bis(PEG4-t-butyl ester) cas:2183440-74-4 N-(N3-PEG3)-N-(PEG2-NH-Boc)-PEG3-acid cas:2054339-01-2 N-Boc-N-bis(PEG2-acid) cas:2055046-22-3 N-Methyl-N-bis(PEG3-OH) cas:2112737-74-1 N-(Tos-PEG4)-N-bis(PEG4-t-butyl ester) cas:1393330-33-0 Bromo-PEG-acid (PEG1-PEGn) cas:1135131-50-8 Bromo-PEG-CH2CO2H (PEG1-PEGn) cas:1393330-36-3 Bromo-PEG-t-butyl ester (PEG1-PEGn) cas:157759-50-7 Bromo-PEG-CH2CO2tBu (PEG1-PEGn) cas:1144106-65-9 Bromo-PEG-N3 (PEG1-PEGn) cas:31255-10-4 Bromo-PEG-bromide (PEG1-PEGn) cas:110429-45-3 Bromo-PEG-methyl (PEG1-PEGn) cas:164332-88-1 Bromo-PEG-N-Boc (PEG1-PEGn) cas:203740-63-0 Bromo-PEG-alkyne (PEG1-PEGn) cas:57159-62-3 Bromoacetamido-PEG-NHS ester (PEG1-PEGn) cas:1353011-95-6 Chloroacetamido-PEG4-NHS ester cas:1365655-90-8 Chloroacetamido-PEG4-t-Butyl Ester cas:16024-60-5 Methyl-PEG-PEG-CH2COOH (PEG1-PEGn) cas:1778219-81-0 Methyl-PEG-t-butyl ester (PEG1-PEGn) cas:31576-51-9 Methyl-PEG-amine (PEG1-PEGn) cas:1263044-81-0 Methyl-PEG-maleimide (PEG1-PEGn) cas:89635-82-5 Methyl-PEG-alkyne (PEG1-PEGn) cas:50586-80-6 Methyl-PEG-tosyl (PEG1-PEGn) cas:441771-60-4 Methyl-PEG-thiol (PEG1-PEGn) cas:1449390-68-4 Methyl-PEG4-hydrazide cas:787524-78-1 Methyl-PEG4-sulfonic acid cas:105108-59-6 Methyl-PEG3-4-nitrophenyl carbonate cas:1835759-87-9 Methyl-PEG3-ONHBoc cas:557756-85-1 Fmoc-amino-PEG4-propanoic acid cas:1609651-90-2 Alkyne-PEG4-Maleimide cas:1621096-79-4 TCO-PEG4-NHS cas:1644644-96-1 Methyltetrazine NHS ester cas:112247-65-1 Biotin-NH-CH2CH2-S-S-Pyr cas:1151451-77-2 Benzaldehyde-PEG4-N3 cas:2062663-64-1 Bromo-PEG6-N3 cas:1313026-32-2 Folate-PEG3-N3 cas:56282-36-1 HS-PEG3-OH cas:1146245-73-9 Mal-PEG2-oxyamine cas:2055041-37-5 Mal-PEG1-Val-Cit-PABC-OH cas:2249935-92-8 Mal-PEG1-Val-Cit-PABC-PNP cas:1870916-87-2 MC-Val-Ala-PAB cas:1639939-40-4 MC-Val-Ala-PAB-PNP cas:1951424-92-2 Fmoc-Ala-Ala-Asn(Trt)-OH cas:2098907-84-5 Acid-propionylamino-Val-Cit-OH cas:2055041-40-0 N3-PEG1-Val-Cit-PABC-OH cas:252378-67-9 Boc-Aminooxy-PEG2-bromide cas:1235514-18-7 Boc-aminooxy-PEG3-amine cas:1884578-00-0 Boc-Val-Ala-PAB-PNP cas:173323-22-3 Bromoacetamide-PEG3-acetic acid cas:932741-11-2 Bromoacetamide-PEG3-alkyne cas:1260139-70-5 Bromoacetamido-PEG4-NHS cas:1698019-89-4 Bromoacetamide-PEG8-acid cas:1803279-86-8 DBCO-C4-SulfoNHS ester cas:1394238-91-5 Fmoc-Val-Ala-PAB cas:1394238-92-6 Fmoc-Val-Ala-PAB-PNP 温馨提示:西安齐岳生物科技有限公司供应的产品用于科研,不能用于其他用途,axc,2021.04.20 上一篇: 银催化DBCO转酰胺反应修饰氨基酸/多肽/ 下一篇: 多功能纳米探针CuPc@HG@BN铜酞菁功能化联系我们:
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