Antibody Information

General Information of This Antibody
Antibody ID
ANI0ZQCVJ
Antibody Name
Trastuzumab-Flexmab
Synonyms
Trastuzumab (Light chain F118C C214V; heavy chain L124C C220V C228V)
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Antibody Type
Monoclonal antibody (mAb)
Antibody Subtype
Human IgG1-kappa
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence
EVQLVESGGGLVQPGGSLRLSCAASGENIKDTYIHWVRQAPGKGLEWVARIYPTNGYTRY
ADSVKGRFTISADTSKNTAYLOMNSLRAEDTAVYYCSRWGGDGFYAMDYWGOGTLVTVSS
ASTKGPSVFPCAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSVDKTHTCPPVPAPELLGG
PSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYN
STYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPOVYTLPPSREE
MTKNOVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRW
QQGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Light Chain Sequence
DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAWYQQKPGKAPKLLIYSASFLYSGVPS
RFSGSRSGTDFTLTISSLQPEDFATYYCQQHYTTPPTFGQGTKVEIKRTVAAPSVFICPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEV
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The Activity Data of This Antibody
Antibody Activity Information 1 [1]
Dissociation Constant (Kd)
2.15
nM
Antibody Function Binding kinetics of trastuzumab-Flexmab and trastuzumab to recombinant HER2.
Antibody Antigen Binding Assay Kinetic measurements were carried out using BIAcore T100 biosensor. The equilibrium dissociation constants, Kd, were calculated as the ratio of the two rate constants, koff/kon.
Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
Trastuzumab-Flexmab-SG3710 [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 82.20% (Day 50) Low HER2 expression (HER2+)
Method Description
The in vivo efficacy of trastuzumab-Flexmab-SG3710 was investigated after single-dose injections (0.30 mg/kg) in female athymic mice bearing NCI-N87 HER2-positive subcutaneous xenografts. NCI-N87 cells (5 x106) in 50% Matrigel were inoculated subcutaneously into 46 week-old female athymic nude mice. Five mice per group were dosed intravenously five days after their tumors reached a volume of 200 mm3.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 92.20% (Day 50) Low HER2 expression (HER2+)
Method Description
The in vivo efficacy of trastuzumab-Flexmab-SG3710 was investigated after single-dose injections (0.6 mg/kg) in female athymic mice bearing NCI-N87 HER2-positive subcutaneous xenografts. NCI-N87 cells (5 x106) in 50% Matrigel were inoculated subcutaneously into 46 week-old female athymic nude mice. Five mice per group were dosed intravenously five days after their tumors reached a volume of 200 mm3.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 92.80% (Day 40) Low HER2 expression (HER2+)
Method Description
The in vivo efficacy of trastuzumab-Flexmab-SG3710 and trastuzumab-C239i-SG3249 ADCs was investigated after single-dose injections (1 mg/kg) in female athymic mice bearing NCI-N87 HER2-positive subcutaneous xenografts,and tumor growth was monitored for 85 days. NCI-N87 cells (5 x106) in 50% Matrigel were inoculated subcutaneously into 46 week-old female athymic nude mice. Five mice per group were dosed intravenously five days after their tumors reached a volume of 200 mm3.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
35.50 pM
Low HER2 expression (HER2+)
Method Description
The cytotoxic effect of Trastuzumab-Flexmab-SG3710 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing breast and gastric cancers. The potency of trastuzumab-Flexmab-SG3710 was assessed on the SKBR-3 cell line after five days of incubation.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
References
Ref 1 Design and characterization of homogenous antibody-drug conjugates with a drug-to-antibody ratio of one prepared using an engineered antibody and a dual-maleimide pyrrolobenzodiazepine dimer. MAbs. 2019 Apr;11(3):500-515.

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