ADC药物靶点蛋白 - 北京百普赛斯生物科技股份有限公司

背景

ADC药物的三大元件包括：1、特异性靶向抗体 2、毒素 3、可裂解/不可裂解的连接子。特异性靶点识别及有效的毒素作用使ADC成为名副其实的“生物导弹”。ADC药物设计同时需要考虑靶点的合理选择；抗体、连接子、小分子药物及它们之间的合理组合；抗体偶联技术以及ADC药物的耐药性等问题。其中，靶点的选择、连接子的选择以及临床前的药效评价是ADC研发过程中关注的焦点。>>>点击查看“ADC药物开发策略、创新技术及工艺放大质控关键点分享”直播回放

为满足ADC药物研发需求，ACROBiosystems可提供：

多种高质量靶点蛋白；
分子互作服务；
用于Linker酶切的MMP/Cathepsin/PLAU；
抗小分子药物抗体和抗独特型抗体及开发服务便于ADC 耐药性研究。

这一系列产品可满足从ADC从抗体制备，筛选到后期的生产质控全流程，协助加速ADC药物研发。

热门产品

ADC热门靶点蛋白

产品特点

● 50 +ADC热门靶点蛋白全覆盖；
● 多种属，多标签；
● 高纯度经MALS验证；
● 高生物活性经ELISA/SPR/BLI/FACS等验证。

应用场景

免疫、抗体筛选、细胞功能验证、质控

特色产品

✔ 行业鲜有LIV-1系列蛋白，覆盖Human、Mouse、Cynomolgus、Rat等种属，表达区间根据SGN-LIV1A结合表位设计

多肽Linker裂解酶

产品特点

●产品类型丰富：MMPs、Cathepsin以及uPA系列
蛋白产品；
●采用HEK293表达，更接近蛋白天然构象；
●高酶活：酶活> 2,500 pmol/min/µg。

应用场景

✔ 用于酶切验证，以评估Linker的酶切效果，保证payload在胞内高效释放。

PK分析相关抗体

产品特点

●产品丰富：抗MMAE抗体和多种抗独特型抗体；
●高特异性；
●高灵敏度和高稳定性。

应用场景

✔ ADC药物临床前和临床免疫原性分析的阳性参照
✔ 药代动力学分析
✔ 抗Payload抗体—定性进行DAR值的检测

特色产品

高灵敏度单克隆抗MMAE抗体（Cat.No.MME-M5252），活性经与Disitamab Vedotin (RC-48)结合验证，线性区间为0.1-2 ng/mL。

分子互作及ADA开发服务

SPR/BLI亲和力检测服务：

●免费提供检测用蛋白
●专业的技术团队
●个性化的方案设计及报告形式

ADA一站式开发服务：

开发范围：
抗独特型单/多克隆抗体、血药浓度定量检测试剂盒，满足客户多样化需求
应用场景
✔ ADA检测：包括筛选、验证、滴度和中和抗体试验
✔ PK检测：代替抗原包板、bridging ELISA

产品列表

ADC靶点蛋白
多肽Linker裂解酶
PK分析相关抗体

类型	分子	货号	产品描述	订购/预购
Cathepsin	Cathepsin B	CTB-H5222	Human Cathepsin B / CTSB Protein, His Tag (active enzyme)	订购
	Cathepsin L	CT1-H5222	Human Cathepsin L / CTSL1 Protein, His Tag	订购
	Cathepsin S	CTS-H5224	Human Cathepsin S / CTSS Protein, His Tag	订购
PLAU	PLAU	PLU-H5229	Human PLAU / uPA Protein, His Tag	订购
PLAU	PLAU	PLU-H5228	Human PLAU / uPA Protein, His Tag (activated by trypsin) (active enzyme)	订购
MMPs	MMP-1	MM1-H5222	Human MMP-1 Protein, His Tag	订购
	MMP-2	MM2-H5225	Human MMP-2 Protein, His Tag	订购
	MMP-2	MM2-H82E3	Biotinylated Human MMP-2 Protein, His,Avitag™	预购
	MMP-2	MM2-M52H3	Mouse MMP-2 Protein, His Tag	预购
	MMP-9	MM9-H5221	Human MMP-9 Protein, His Tag (active enzyme)	订购

货号	产品描述	中和活性	Affinity K_D, nM	应用
MME-M5252^NEW	Anti-MMAE Antibodies	/	/	PK assay; ELISA
ADB-Y19	Anti-Adalimumab Antibodies	Neutralizing Antibody	0.0013	ADA assay; Neutralizing assay; Indirect ELISA
ADB-Y23b	Anti-Adalimumab Antibodies	Non-Neutralizing Antibody	/	PK bridging ELISA with ADB-BY17; Indirect ELISA
ADB-BY17	Biotinylated Anti-Adalimumab Antibodies	Neutralizing Antibody	/	PK bridging ELISA with ADB-Y23b
BEB-Y9	Anti-Bevacizumab Antibodies	Neutralizing Antibody	1.92	ADA assay; Indirect ELISA
BEB-Y10	Anti-Bevacizumab Antibodies	Neutralizing Antibody	/	PK bridging ELISA with BEB-BY13; Neutralizing assay; Indirect ELISA
BEB-BY13	Biotinylated Anti-Bevacizumab Antibodies	Neutralizing Antibody	/	PK bridging ELISA with BEB-Y10
CEB-Y27	Anti-Cetuximab Antibodies	Neutralizing Antibody	0.007	ADA assay; Neutralizing assay; Indirect ELISA
CEB-Y29	Anti-Cetuximab Antibodies	Neutralizing Antibody	/	PK bridging ELISA with CEB-BY31; Neutralizing assay; Indirect ELISA
CEB-BY31	Biotinylated Anti-Cetuximab Antibodies	Non-Neutralizing Antibody	/	PK bridging ELISA with CEB-Y29
RIB-Y35c	Anti-Rituximab Antibodies	Neutralizing Antibody	/	ADA assay; Neutralizing assay; Indirect ELISA
TRB-Y1b	Anti-Trastuzumab Antibodies	Neutralizing Antibody	/	PK bridging ELISA with TRB-Y5b; Neutralizing assay; Indirect ELISA
TRB-Y5b	Anti-Trastuzumab Antibodies	Non-Neutralizing Antibody	/	PK bridging ELISA with TRB-Y1b

ADC药物靶点蛋白

Coagulation Factor III

靶点蛋白验证数据

高纯度—MALS 验证

The purity of Human Her2, His Tag (Cat. No. HE2-H5225) was more than 90% and the molecular weight of this protein is around 80-95 kDa verified by SEC-MALS.

高亲和力—ELISA验证

Immobilized Human TROP-2, His Tag (Cat. No. HE2-H5225) 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

Immobilized Human PSMA, His Tag (Cat. No. PSA-H52H3) at 2 μg/mL (100 μL/well) can bind Monoclonal Anti-Human PSMA Antibody, Human IgG1 with a linear range of 0.3-39 ng/mL (Routinely tested).

申请 Protocol

高亲和力—SPR验证

Anti-LIV-1 mAb captured on CM5 chip via anti-human IgG Fc antibody can bind Human LIV-1, His Tag (Cat. No. LV1-H5223) with an affinity constant of 5.24 nM as determined in a SPR assay (Biacore T200) (Routinely tested).

申请 Protocol 点击咨询SPR服务

Herceptin (Trastuzumab) captured on CM5 chip via anti-human IgG Fc antibodies surface, can bind Human Her2, His Tag (Cat. No. HE2-H5225) with an affinity constant of 1.07 nM as determined in a SPR assay.

申请 Protocol 点击咨询SPR服务

高亲和力—BLI验证

Loaded Mouse Nectin-4, His Tag (Cat. No. NE4-M52H3) on HIS1K Biosensor, can bind Human Nectin-1, Fc Tag (Cat. No. PV1-H5253) with an affinity constant of 0.12 μM as determined in BLI assay (ForteBio Octet Red96e) (Routinely tested).

申请 Protocol 点击咨询BLI服务

高亲和力—FACS验证

2e5 of anti-ROR1 CAR-293 cells were stained with 100 μL of 10 μg/mL of Human / Cynomolgus / Rhesus macaque ROR1 (39-151, Ig-like domain), His Tag (Cat. No. RO1-H5221) and negative control protein respectively, washed and then followed by PE-anti-His Tag and analyzed with FACS (Routinely tested).

申请 Protocol

多肽Linker裂解酶

在ADC设计开发中，Linker的结构及化学性质直接影响ADC的稳定性、安全性和特异性。Linker分为可裂解和不可裂解Linker。多肽Linker是目前ADC开发中广泛应用的一种可裂解Linker，在设计时，需综合考虑选择合适的裂解酶用于Linker的裂解。

ACROBiosystems开发了一系列用于裂解酶切Linker的MMPs、Cathepsin以及uPA蛋白产品。

相关阅读：

不同Linker裂解酶：针对多肽Linker“量体裁衣”

更多anti-payload antibodies（Anti-Dxd antibody/Anti-SN-38 antibody/Anti-SN-38 antibody）正在开发中，敬请期待！

验证数据：

测定产品	货号：CTB-H5222 Human Cathepsin B / CTSB Protein, His Tag (active enzyme)	货号：MM9-H5221 Human MMP-9 Protein, His Tag (active enzyme)
水解底物	荧光标记多肽底物 Z-LR-AMC	荧光标记多肽底物 Mca-PLGL-Dpa-AR-NH2
酶活（pmol/min/μg）
	> 2500	> 2500

PK分析相关抗体

ACROBiosystems可提供一系列高特异性、高灵敏度和高稳定性的抗MMAE抗体和抗独特型抗体，用于ADC药物临床前和临床免疫原性分析的阳性参照和药代动力学分析，可以节省客户制备抗体的时间，免费提供完整的方法学protocol。

验证数据：

抗MMAE抗体高特异性结合MMAE

The EC50 value of anti-MMAE antibody to MMAE-conjugated hRS7 (MMAE-ADC) was 0.12 μg/ml. The unconjugated hRS7 antibody was used as negative control

申请 Protocol

Immobilized Disitamab Vedotin (RC48) at 0.2 μg/mL (100 μL/well) can bind Mouse Anti-MMAE Antibody, Mouse IgG1 (Cat. No. MME-M5252) with a linear range of 0.1-2 ng/mL (QC tested).

申请 Protocol

特异性检测体内抗体药水平

: Detection of rituximab by antigen-capture ELISA (0.1% serum).

: Detection of rituximab by anti-idiotypic capture ELISA (0.1% serum).

: Detection of rituximab by anti-idiotypic bridging ELISA (10% serum).

检测方法	线性范围（µg/mL）	灵敏度（µg/mL）	优势	劣势
Antigen-capture ELISA	—	—	方法简单，通用性好	背景值高，无活性
Anti-idiotypic capture ELISA	0.156-10	0.156	解决了CD20获得难的问题，方法简单	背景高，只适用于美罗华biosimilar
Bridging ELISA by anti-idiotypic antibodies	0.012-0.78	0.012	解决了CD20获得难的问题，灵敏度好，背景低	只适用于美罗华biosimilar