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ADC药物研发解决方案

ADC药物研发解决方案
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dexiconelektrik.com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。
ADC结构图
热门dexiconelektrik.com
ADC热门靶点蛋白
ADC靶点蛋白

dexiconelektrik.com特点

  1. 50 +ADC热门靶点蛋白全覆盖;
  2. 多种属,多标签;
  3. 高纯度经MALS验证;
  4. 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dexiconelektrik.com

  • ✔ 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
Cathepsin B等,ADC 多肽Linker裂解酶

dexiconelektrik.com特点

  1. dexiconelektrik.com类型丰富:MMPsCathepsin以及uPA系列
    蛋白dexiconelektrik.com;
  2. 采用HEK293表达,更接近蛋白天然构象;
  3. 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
抗MMAE抗体及抗独特型抗体,ADC PK分析相关抗体

dexiconelektrik.com特点

  1. dexiconelektrik.com丰富:抗MMAE抗体和多种抗独特型抗体
  2. 高特异性;
  3. 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dexiconelektrik.com

  • 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
ADC中SPB/BLI分子互作及ADA开发服务

SPR/BLI亲和力检测服务:

  1. 免费提供检测用蛋白
  2. 专业的技术团队
  3. 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
dexiconelektrik.com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 dexiconelektrik.com描述 订购/预购
Cathepsin Cathepsin B CTB-H5222 Human Cathepsin B / CTSB Protein, His Tag (active enzyme)

订购

PLAU PLAU PLU-H5229 Human PLAU / uPA Protein, His Tag

订购

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 dexiconelektrik.com描述 中和活性 Affinity KD, nM 应用
MME-M5252NEW 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
靶点蛋白验证数据
高纯度—MALS 验证
HER2 MALS测定结果

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
HER2 ELISA测定结果

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
PSMA ELISA测定结果

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
LIV-1 SPR测定结果

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
HER2 SPR测定结果

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
Nectin-4 BLI测定结果

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
ROR1 BLI测定结果

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MMPsCathepsin以及uPA蛋白dexiconelektrik.com。

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-MMAF antibody)正在开发中,敬请期待!
ADC作用机理
验证数据:
测定dexiconelektrik.com 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抗MMAE抗体抗独特型抗体,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
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
抗MMAE抗体高特异性结合MMAE ADC

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
抗Rituximab抗体特异性检测体内抗体药水平
Detection of rituximab by antigen-capture ELISA (0.1% serum).
抗Rituximab抗体特异性检测体内抗体药水平
Detection of rituximab by anti-idiotypic capture ELISA (0.1% serum).
抗Rituximab抗体特异性检测体内抗体药水平
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

相关阅读:

ADC药物PK验证,岂能缺少抗MMAE抗体

SPR/BLI亲和力检测以及抗独特性抗体开发服务
除上述dexiconelektrik.com外,依托强大专业的技术团队,ACROBiosystems同时也为客户提供高质量一体化的SPR&BLI分子互作检测服务以及多种抗独特型单/多克隆抗体、血药浓度定量检测试剂盒开发的一站式服务,协助客户加快ADC药物研发进程。
SPR&BLI分子互作检测服务
合作工业及科研用户百余家
检测用ADC靶点蛋白免费提供
抗体筛选、表征、一致性评价方法开发免费赠送
最快询单次日即可出具报告
助力多个抗体药物成功申报临床
ADC中SPB/BLI分子互作服务
抗独特型抗体开发服务
抗体筛选所需ACRO蛋白免费提供
响应快,项目组一对一服务,实时跟进实验进度
提供从抗原制备到检测试剂盒开发的一站式服务
保证交付灵敏度满足法规要求的PK/ADA检测试剂
ADC中抗独特型抗体(ADA)开发服务

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