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抗体偶联药物(ADC)靶点蛋白

背景
肿瘤细胞表面表达的靶抗原是抗体药物偶联物(ADC)识别肿瘤细胞并引导细胞毒性有效载荷进入癌细胞的关键因素。因此,选择适当的靶抗原是设计ADC药物的首要考量。理想的靶抗原应具备以下特征:
特异性表达:靶抗原应在肿瘤细胞中高度特异性或主要表达,而在正常组织中表达水平较低或几乎不表达[1],以减少脱靶效应及相关毒性。理想情况下,靶抗原应位于细胞表面或细胞外域,而非细胞内抗原,以便抗体药物偶联物能够在循环系统中有效识别并结合。
非分泌性:靶抗原应为非分泌型,避免抗原的过度分泌造成循环中抗原-抗体复合物的非特异性结合,这会导致ADC在肿瘤部位外的非特异性结合,从而降低药物的靶向性并可能增加安全性风险[2]
内化特性:靶抗原与抗体结合后,应能有效内化进入肿瘤细胞,确保ADC复合物通过内吞作用进入细胞,继而通过适当的细胞内转运途径促进细胞毒性载荷的迅速释放[3],以发挥抗肿瘤效应。
ACROBiosystems百普赛斯开发了90+高质量ADC药物靶点蛋白,覆盖Human、Mouse、Cynomolgus、Rat等多个种属及多种标签,具有高纯度及高生物活性,可用于免疫、抗体筛选、种属交叉验证、质控放行、药代动力学研究等多种应用场景。
产品优势

90+ ADC热门靶点蛋白全覆盖;

多种属,多标签;

蛋白均一结构及高纯度经SEC-MALS验证;

高生物活性经ELISA/SPR/BLI/FACS等验证。

验证数据

纯度经SEC-MALS验证

PSMA二聚体高纯度经SEC-MALS验证
PSMA二聚体经SEC-MALS验证

The purity of Mouse PSMA Protein, Fc Tag (Cat. No. PSA-M5266) is more than 90% and the molecular weight of this protein is around 240-280 kDa verified by SEC-MALS.

LRRC15高纯度经SEC-MALS验证
LRRC15 SEC-MALS验证高纯度

The purity of Biotinylated Human LRRC15, His,Avitag (Cat. No. LR5-H82E4) is more than 90% and the molecular weight of this protein is around 80-95 kDa verified by SEC-MALS.

与抗体的结合活性经ELISA验证

PSMA结合活性经ELISA验证

Immobilized Monoclonal Anti-Human PSMA Antibody, Human IgG1 at 2 μg/mL (100 μL/well) can bind Human PSMA, His Tag (Cat. No. PSA-H52H3) with a linear range of 2-39 ng/mL (QC tested).

申请 Protocol
TROP-2结合活性经ELISA验证

Immobilized Human TROP-2, His Tag (Cat. No. TR2-H5223) at 1 μg/mL (100 μL/well) can bind Mouse Monoclonal Antibody Against Human TROP-2, Mouse IgG1 with a linear range of 0.1-2 ng/mL (QC tested).

申请 Protocol
Claudin-18.2结合活性经ELISA验证

Immobilized Human Claudin-18.2 Full Length Protein-VLP (Cat. No. CL2-H52P7) at 5 μg/mL (100 μL/well) can bind Monoclonal Anti-Chimeric Claudin-18.2 Antibody, Human IgG1 with a linear range of 0.2-3 ng/mL (QC tested).

申请 Protocol
B7-H4结合活性经ELISA验证

Immobilized Human B7-H4, His Tag (Cat. No. B74-H5222) at 2 μg/mL (100 μL/well) can bind Anti-B7-H4 MAb (Human IgG1) with a linear range of 0.2-6 ng/mL (QC tested).

申请 Protocol

与抗体的结合活性经SPR验证

TROP-2结合活性经SPR验证

Captured Trop2 antibody on CM5 chip via anti-mouse antibodies surface can bind Human TROP-2, His Tag (Cat. No. TR2-H5223) with an affinity constant of 5.98 nM as determined in a SPR assay (Biacore T200) (Routinely tested).

申请 Protocol
CDH17结合活性经SPR验证

Anti-Cadherin-17 antibody captured on CM5 chip via Anti-human IgG Fc antibodies surface can bind Human Cadherin-17, His Tag (Cat. No. CA7-H52H3) with an affinity constant of 2.9 μM as determined in a SPR assay (Biacore 8K) (Routinely tested).

申请 Protocol
Nectin-4结合活性经SPR验证

Mouse Anti-Nectin-4 Antibody (Mouse IgG1) captured on CM5 chip via anti-mouse antibodies surface can bind Human Nectin-4, His Tag (Cat. No. NE4-H52H3) with an affinity constant of 58.2 nM as determined in a SPR assay (Biacore T200) (Routinely tested).

申请 Protocol
FRα结合活性经SPR验证

Biotinylated Human FOLR1, His,Avitag (Cat. No. FO1-H82E2) immobilized on SA Chip can bind Folic acid-BSA with an affinity constant of 83.8 pM as determined in a SPR assay (Biacore 8K) (Routinely tested).

申请 Protocol

与抗体的结合活性经BLI验证

B7-H3结合活性经BLI验证

Loaded Monoclonal Anti-Human B7-H3 / B7-H3 (4Ig) Antibody, Human IgG1 on Protein A Biosensor, can bind Human B7-H3 Protein, His Tag (Cat. No. B73-H52E2) with an affinity constant of 479 nM as determined in BLI assay (ForteBio Octet Red96e) (Routinely tested).

申请 Protocol
ROR1结合活性经BLI验证

Loaded Biotinylated Human / Cynomolgus / Rhesus macaque ROR1, His,Avitag (Cat. No. RO1-H82E6) on SA Biosensor, can bind Zilovertamab with an affinity constant of 0.252 nM as determined in BLI assay (ForteBio Octet Red96e) (Routinely tested).

申请 Protocol
产品活动
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参考文献
  • [1] Damelin Marc, Zhong Wenyan, Myers Jeremy, et al. Evolving Strategies for Target Selection for Antibody-Drug Conjugates.[J]. Pharmaceutical research, 2015, 32(11):3494-507. DOI: 10.1007/s11095-015-1624-3.
  • [2] Ritchie Michael, Tchistiakova Lioudmila, Scott Nathan, et al. Implications of receptor-mediated endocytosis and intracellular trafficking dynamics in the development of antibody drug conjugates.[J]. mAbs, 2013, 5(1):13-21. DOI: 10.4161/mabs.22854.
  • [3] Donaghy Heather, . Effects of antibody, drug and linker on the preclinical and clinical toxicities of antibody-drug conjugates.[J]. mAbs, 2016, 8(4):659-71. DOI: 10.1080/19420862.2016.1156829.
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