高质量ADC药物靶点蛋白

高质量ADC药物靶点蛋白抗体药结合验证（ELISA/SPR/BLI）

纯度经SEC-HPLC验证高批间一致性 一站式多种属选择01ADC靶点蛋白产品产品优势

02资质证书

02ADC靶点蛋白应用案例

03明星产品推荐

04产品验证数据

04热门靶点支持多种属交叉活性验证

07高质量ADC药物靶点蛋白ADC药物靶点概述FDA批准的ADC药物北京义翘神州科技股份有限公司高质量ADC药物靶点01选择合适的靶点是ADC药物成功开发的第一步。理想的靶点应是肿瘤特异性的，在正常组织细胞中少量表达；靶点与相应抗体结合后应通过内吞作用内化，以促进ADC药物进入肿瘤细胞，并通过适当的细胞内转运途径释放细胞毒性药物；此外，靶点应相对稳定，不易发生突变，这样可以降低ADC耐药性的产生。FDA批准的ADC药物自2000年FDA批准首个ADC药物Mylotarg®（Gemtuzumab

Ozogamicin）以来，截至2024年6月，全球共有13种ADC药物获批用于治疗骨髓瘤、淋巴瘤、白血病、乳腺癌和头颈癌等多种癌症。目前获批ADC药物的靶点通常是在癌细胞过表达的蛋白，如血液系统肿瘤靶点

CD19、CD22、CD33、BCMA和CD79b，以及实体瘤靶点HER-2、TROP-2和Nectin-4。此外，还有100多个ADC候选药物处于临床试验的不同阶段。ADC药物靶点概述抗体偶联药物（ADCs）是一类将细胞毒性药物与单克隆抗体通过连接子偶联形成的抗肿瘤药物，它结合了细胞毒性药物的高效杀伤力和单克隆抗体的高度特异性靶向能力，在癌症治疗方面，拥有巨大的潜力。药物名称靶点细胞毒药物连接子适应症上市时间/公司Gemtuzumab

Ozogamicin(Mylotarg®)CD33N-acetyl-γ-calicheamicinHydrazoneAcute

myeloidleukemia2000,

2017;

PfizerBrentuximab

Vedotin(Adcetris®)CD30MMAEmc-VC-PABCHodgkin

lymphoma,systemic

anaplasticlarge-celllymphoma-celllymphoma2011;

SeagenTrastuzumab

Emtansine(Kadcyla®)HER-2DM1SMCCBreast

cancer2013;

RocheInotuzumab

Ozogamicin(Besponsa®)CD22N-acetyl-γ-calicheamicinHydrazoneB-cell

precursoracute

lymphoblasticleukemia2017;

PfizerMoxetumomab

pasudotox(Lumoxiti®)CD22mc-VC-PABCPE38Hairy

cell

leukemia2018;

AstraZenecaPolatuzumab

Vedotin(Polivy®)CD79bMMAEmc-VC-PABCDiffuse

large

B-celllymphoma2019;

RocheEnfortumab

Vedotin(Padcev®)Nectin-4MMAEmc-VC-PABCUrothelial

cancer2019;

SeagenTrastuzumab

Deruxtecan(Enhertu®)HER-2DXdtetrapeptideBreast

cancer2019;

Daiichi

SankyoSacituzumab

Govitecan(Trodelvy®)Trop-2SN38CL2ABreast

cancer,urothelial

cancer2020;

ImmunomedicsBelantamab

Mafodotin(Blenrep®)BCMAMMAFmcMultiple

myeloma2020,

Withdrawal

in2022;

GSKLoncastuximab

Tesirine(Zynlonta®)CD-19PBD

dimerdipeptideLarge

B-celllymphoma2021;

ADCTherapeuticsTisotumab

Vedotin(Tivdak®)TissuefactorMMAEmc-VC-PABCCervical

Cancer2021;

Genmab/SeagenMirvetuximab

Soravtansine(Elahere®)FRαDM4sulfo-SPDBOvarian

cancer2022;

ImmunoGen北京义翘神州科技股份有限公司02高质量ADC药物靶点蛋白产品覆盖90+热门ADC药物靶点结合活性经抗体药验证HEK293表达，重组蛋白更接近天然构象多种属，支持种属交叉验证多标签覆盖资质证书高纯度：经SDS

&

SEC-HPLC验证高生物活性：细胞活性和抗体结合活性（ELISA、SPR/BLI）高稳定性，高批间一致性严格的质量控制体系：ISO

9001/ISO

13485/GMP质量体系认证提供Biotin定点标记蛋白（AVI

tag）产品优势ADC靶点蛋白产品义翘神州已开发出一系列ADC药物靶点蛋白产品，包含热门药物靶点如HER-2、TROP-2、Nectin-4、EGFR、CD19、BCMA，以及新兴靶点如EphA3、GFRA1、CLEC7A等。这些靶点蛋白产品均经过抗体结合活性验证，并且具备多种属、多标签选择的特点，全面支持ADC药物研发。2024年值得关注的生长因子供应商CNAS认证FDA

DMF备案ISO

9001:2015认证ISO

13485:2016认证GMP认证北京义翘神州科技股份有限公司高质量ADC药物靶点03Products

used:Human

c-MET/HGFR

Protein

(Cat#:

10692-H08H)新型抗肿瘤药物FDCs（Fab

drug

conjugates）的结合活性检测（ELISA）The

structure

of

IMMU-132

(a).

Specificity

of

hRS7

for

human

Trop-2

(yellow

curves)

and

murine

Trop-2

(red

curves)

(b).The

binding

of

IMMU-132

to

Trop-2

was

analyzed

by

surface

plasmon

resonance

(BIACORE)

(c).Source:

/10.3390/ph13090245;

/10.1021/acs.bioconjchem.5b00223anti-TROP2

Trodelvy®

(sacituzumab

govitecan

or

IMMU-132)HS-HS--sH-SH-SHHS--SH

-sNOOOHO

OOO

NNN

HNHH

O

O

N

O

Lys

N7

O

Omaleimide

Hshort

PEG

forsolubilitycleavablecarbonateOO

NOSN-387.6ADC靶点蛋白应用案例ADC药物IMMU-132的交叉反应和结合活性检测（ELISA

&

SPR）Products

used:Human

Trop-2

Protein

(Cat#:

10428-H08H);Mouse

Trop-2

Protein

(Cat#:

50922-M08H)(a)4320.00010.0010.010.11101001000Absorbance

at

450

nm10Concentration,

nMBinding

affinity

determination

via

ELISA

of

the

anti-cMET

Fab/IgG

and

their

corresponding

drug

conjugates.Source:

/10.1080/14712598.2023.2292633α-cMET

Fabα-cMET

lgGα-cMET

FDC-Duo5_P1α-cMET

FDC-Duo5_P2α-cMET

ADC-Duo5_P1EC50

(nM)α-cMet

Fab0.28α-cMET

FDC-Duo5-P10.47α-cMET

FDC-Duo5-P20.43α-cMet

lgG0.17α-cMET

ADC-Duo5-P10.23(c)6005004003002001000-100RU-25

-5

15

35

55

75

95

115

135

155

sResp.Diff.IMMU-132

(pH

7.4)TimeStart

StopSample

SampleInjection

Injection700

400nM400nM400nM400nM(b)OD450nm2.22.01.81.61.41.21.00.80.60.40.20.0-0.2-2

-1

0

1

2

3

4

5[hR

S7]

(ng/mL)hR

S7

on

Human

Trop-2

Coated

Plate

hR

S7

on

Murine

Trop-2

Coated

Plate北京义翘神州科技股份有限公司04高质量ADC药物靶点明星产品推荐产品验证数据抗体药结合验证无标签蛋白供应高批间一致性No

Tag

(Cat#:

10004-HCCH)HisTag

(Cat#:

10004-H08H)160140120100806040200-20Neutralization,

%50ED

=0.3-1.5

µg/mL1

10HumanERBB2Conc.(µg/mL)Measured

by

its

ability

to

block

anti-ErbB2mediated

inhibition

of

BT474

humanbreast

ductal

carcinomacell

proliferation.0.50.40.30.20.1Response

(nm)0.00Loaded

Anti-Erbb2

Antibody

(Pertuzumab)

on

ProABiosensor,

can

bind

human

Her2/ERBB2

protein

withan

affinity

constant

of

0.382

nM

as

determined

in

BLIassay

(Sartorius

Octet

RED384)

(Routinely

tested).1E-3

0.01

0.1

1

10

100Anti-HER2/ERBB2

Antibody

Conc.

(ng/mL)Three

independent

lots

of

humanERBB2

protein

have

identical

bioactivity.0123His

Tag,

Biotinylated(Cat#:

10004-H08H-B)Lot

14

Lot

2Lot

3Abs.(OD450nm-Blank)货号靶点种属表达宿主SEC-HPLC纯度活性10904-H08HCD73/NT5EHumanHEK293

Cells≥

95%ELISA,

BLI10620-H08HBCMAHumanHEK293

Cells≥

95%ELISA,BLI,

FACS10818-H08HCD38HumanHEK293

Cells≥

95%ELISA,

SPR10774-H08HCD40/TNFRSF5HumanHEK293

Cells≥

95%ELISA,

BLI12283-H08HCD47HumanHEK293

Cells≥

95%ELISA,

SPR,

BLI10692-H08Hc-MET/HGFRHumanHEK293

Cells≥

90%ELISA11159-H08HCTLA-4HumanHEK293

Cells≥

95%ELISA,

SPR,

BLI10694-H08HEpCAM/TROP1HumanHEK293

Cells≥

90%Cellular

Activity13926-H08HEphA2HumanHEK293

Cells≥

90%ELISA10464-H07HFAPHumanHEK293

Cells≥

90%Enzymatic

Activity10164-H08HIGF1RHumanHEK293

Cells>

90%

(SDS-PAGE)ELISA,

SPR,

BLI15786-H08HLRRC15HumanHEK293

Cells>

95%

(SDS-PAGE)ELISA13128-H08H1MesothelinHumanHEK293

Cells≥

95%

(SDS)ELISA,

BLI19771-H08HNectin-4HumanHEK293

Cells>

95%ELISA,

BLI15877-H07HPSMA/FOLH1HumanHEK293

Cells>

95%

(SDS-PAGE)ELISA11020-H07HTFR1/CD71HumanHEK293

Cells>

90%ELISA10428-H08HTROP-2HumanHEK293

Cells>

96%

(SDS-PAGE)ELISA,

BLI注：H：人；M：小鼠；R：大鼠；C：犬；Rh：恒河猴；Cy：食蟹猴。HOT

HumanHer2/ERBB2

Protein130 260

390

520

650

780Time

(s)mFc

Tag10004-H05HhFc

Tag90020-K02HhFc

Tag50714-M02HHis

Tag90295-C08HhFc

TagH

10004-H02HHis

Tag90020-K08HRhHis

TagM

50714-M08HHis

&

AVI

Tag90295-C49H-BCyHis

Tag80079-R08HhFc

Tag80079-R02HHis

Tag70024-D08HRC不同种属HER2蛋白，可供选择！北京义翘神州科技股份有限公司高质量ADC药物靶点05hFc

Tag(Cat#:

10001-H02H)HisTag(Cat#:

10001-H08H)His

&

AVI

Tag,

Biotinylated(Cat#:

29662-H27H-B)Purity

>

95

%

as

determined

bySEC-HPLC.Abs.

(OD450nm-Blank)5432100.01

0.1

1

10

100Human

EGFRConc.(ng/mL)50ED

=2-8ng/mLImmobilized

human

TGFA

/

TGF-alphaprotein

at

2

µg/ml

(100

µl/well)

can

bindhuman

EGFR

/

HER1

/

ErbB1(Cat#:

10001-H02H).Captured

Cetuximab(IgG1)on

proAChipcanbind

human

EGFR

protein

with

an

affinityconstant

of

1.07

nM

as

determined

in

an

SPRassay

(Biacore

T200)

(Routinely

tested).-1-5

000RU

454035302520151050Response100

200

300

400Time

(s)5

10

15

20

25

minmAU1101009080706050403020100VLP,

Nanodisc,

Detergent三大平台无标签蛋白供应高活性经BLI/ELISA验证VLP,

No

Tag（Cat#:

30025-HNAH）VLP,

fluorescent（Cat#:

30025-HNAH1）Nanodisc,

His

&

Strep

Tag（Cat#:

30025-H64H-NA）Immobilized

human

Claudin18.2-VLP

(FullLength)

protein

(Cat:

30025-HNAH)

at

5

µg/mL(100µL/well)canbindanti-humanclaudin18.2

antibody,

human

IgG1.Immobilized

human

Claudin18.2-VLP

(Full Loaded

anti-human

Claudin-18.2

antibody,Length)

protein,

fluorescent

(Cat: human

IgG1

on

ProA

Biosensor,

can

bind30025-HNAH1)

at5

µg/mL(100

µL/well)can recombinant

human

Claudin-18.2-Nanodiscbind

anti-human

claudin18.2

antibody, protein

with

an

affinity

constant

of

3.43

nMhuman

IgG1. as

determined

in

BLI

assay

(Sartorius

OctetRED384)

(Routinely

tested).抗体药结合验证EGF结合验证产品被多次引用HOT

Human

EGFR

ProteinHOT

Human

Full-length

Claudin

18.2

Protein注：H：人；R：大鼠；Ra：兔；P:猪;M：小鼠；C：犬；Rh：恒河猴；Cy：食蟹猴；F：猫Human

CLDN18.2-Detergent

(Full

Length)

Protein

(His

&

Strep

Tag)

(Cat#:

30025-H64H-DD)

is

coming

soon!EGFRvIII,AVI

&Histag29662-H27H-BhFc

Tag90317-K02HHis

Tag80100-R08HHis

Tag70026-D08BEGFRvIII,

His

tagH

29662-H08HHis

Tag90317-K08HRhHis

Tag51091-M08HHis

Tag90285-C08HMCyRCHis

TagRa

65172-T08HHis

TagF

62011-U08B不同种属EGFR蛋白，可供选择！54321OD450-BlankEC

=5-20ng/mL50OD450-Blank-0.50.01

0.1

1

10

100

1000

0.01

10

100

1000Anti-claudin

18.2

antibody

Conc.(ng/mL)

Anti-claudin

18.2

antibody

Conc.(ng/mL)4.0 EC

=53.9

ng/mL3.53.02.52.01.51.00.50.80.60.40.20

0.0

0.0

Respone(nm)0

60

120180

240

300Time(s)50北京义翘神州科技股份有限公司06高质量ADC药物靶点EphA3

Protein经HPLC验证多种属配体结合验证抗体药结合验证经HPLC验证多种属Human,His

Tag（Cat#:

15786-H08H）Mouse,

His

&

AVI

Tag（Cat#:

5A4998-M49H-B）Cynomolgus,

His

Tag（Cat#:

91010-C08H）Immobilized

Anti-LRRC15

Antibody

at

2µg/mL

(100

µL/well)

can

bind

recombi-nant

Cynomolgus

LRRC15

Protein.Immobilized

Anti-LRRC15

Antibody(Samrotamab)

at

2

µg/mL

(100µL/well)can

bind

recombinant

human

LRRC15protein.Immobilized

Anti-LRRC15

Antibody

at

2

µg/mL(100

µL/well)

can

bind

recombinant

mouseLRRC15

Protein.Human,His

Tag（Cat#:

11459-H08H）Mouse,

His

Tag（Cat#:

51122-M08H）Rat,

His

Tag（Cat#:

80465-R08H）Immobilized

rat

EphA3

protein

at

2

µg/ml(100

µl/well)

canbind

ratEphrin-A5/

EFNA5

protein

(FcTag)(Cat:

80105-R02H).Measured

by

its

binding

ability

in

afunctional

ELISA.

Immobilized

humanEPHA3-His

at

10

µg/ml

(100

µl/well)

canbind

human

EphrinA5-Fc(Cat:

10192-H02H).Measured

by

its

binding

ability

in

a

functionalELISA.

Immobilized

mouse

EPHA3-His

at

10

µg/mL(100

µL/well)

can

bind

mouse

EFNA5-Fc

(Cat:

50597-M02H).LRRC15

ProteinHOTAbs.

(OD450nm-Blank)5432100.01

0.1

1

10 100

1000

1000Human

LRRC15

Conc.(ng/mL)EC50=

3-9

ng/mL43210Abs.

(OD450nm-Blank)0.01

0.1

1

10Mouse

LRRC15Conc.(ng/mL)100EC50=

0.6-1.8

ng/mLCynomolgus

LRRC15

Conc.(ng/mL)4321Abs.

(OD450nm-Blank)00.01

0.1

1

10100EC50=

1.2-3.6

ng/mL1.00.80.60.40.2Abs.

(OD450nm-Blank)50EC

=

6.2-14.6

ng/mLHuman

EphA3

Conc.

(ng/mL)

Mouse

EphA3

Conc.(ng/mL) Rat

EphA3

Conc.

(ng/mL)4321Abs.

(OD450nm-Blank)0

00.1

1

10

100

1000

10000

0.1

1

10

100

1000

1000050EC

=

4.9-11.4

ng/mL4321Abs.

(OD450nm-Blank)00.0

1

10

100100050EC

=

0.6-1.8

ng/mL北京义翘神州科技股份有限公司高质量ADC药物靶点07GFR

Alpha-1/GFRA1

Protein经HPLC验证细胞活性验证多种属Human,His

Tag(Cat#:

10330-H08H)Mouse,

His

Tag(Cat#:

50171-M08H)Rat,

His

Tag(Cat#:

80021-R02H)Immobilized

rat

His-GDNF

(78-211)(Cat#:

80050-R07B)

at

10

µg/ml

(100

µl/well)

can

bind

rat

GFRA1-Fc.543210Abs.

(OD450nm-Blank)1

10

100 1000

10000Human

GFR

Alpha-1/GFRA1

Conc.

(ng/mL)50EC

=

15-48

ng/mLImmobilized

human

GDNF

protein(Cat#:10561-HNCH)

at

2

µg/mL

(100

µL/well)

can

bind

human

GFRA1

/

GFRα1

/GDNFRA

protein.Immobilized

mouse

GFRA1

/

GFR

alpha-1

Protein

at

2

µg/mL

(100

µL/well)

can

bind

biotinylated

rat

GDNF

protein.1

10

100

10004.03.53.02.52.01.51.00.50.0-0.50.1Abs.

(OD450nm-Blank)MouseGFR

Alpha-1/GFRA1Conc.

(ng/mL)50EC

=20-60

ng/mL1

10

100

1000

10000-0.50.1Abs.

(OD450nm-Blank)Rat

GFR

Alpha-1/GFRA1

Conc.

(ng/mL)3.5

503.02.52.01.51.00.50.0EC

=

20-46.6ng/mL热门靶点支持多种属交叉活性验证靶点多种属结合活性细胞活性SEC-HPLC纯度B7-H3YesYesTestingYesB7-H4YesYesTestingYesBCAMYesTestingYesYesBCMAYesYesYesYesCD155/PVRYesYesTestingYesCD19YesYesTestingYesCD2