General Information of This Antibody
Antibody ID
ANI0GYJQM
Antibody Name
Cetuximab
Brand Name
ERBITUX
Organization
Bristol-Myers Squibb; Merck & Co., Inc.
Indication
Colorectal cancer; Head and neck squamous cell carcinoma; Esophageal cancer
Approval Date
Feb. 2004
Synonyms
Fab C225; IMC-225; ABP-494; C225; C-225; CETUXIMAB CETUXIMAB BIOSIMILAR (ABP-494); CETUXIMAB (GENETICAL RECOMBINATION); CMAB009; CMAB-009; IMC-C225; MOAB C225
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Antibody Type
Monoclonal antibody (mAb)
Antibody Subtype
Chimeric IgG1-kappa
Antigen Name
Epidermal growth factor receptor (EGFR)
 Antigen Info 
ChEMBI ID
CHEMBL1201577
PDB ID
1yy8 , 1yy9 , 4gw1 , 4gw5 , 4kro , 4krp , 5esq , 5hpm , 5hyq , 5icx , 5icy , 5icz , 5id0 , 5id1
DrugBank ID
DB00002
Drug Central ID
4954
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence
QVQLKQSGPGLVQPSQSLSITCTVSGFSLTNYGVHWVRQSPGKGLEWLGVIWSGGNTDYN
TPFTSRLSINKDNSKSQVFFKMNSLQSNDTAIYYCARALTYYDYEFAYWGQGTLVTVSAA
STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSPKSCDKTHTCPPCPAPELL
GGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQ
YNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSR
DELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKS
RWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Heavy Chain Varible Domain
QVQLKQSGPGLVQPSQSLSITCTVSGFSLTNYGVHWVRQSPGKGLEWLGVIWSGGNTDYN
TPFTSRLSINKDNSKSQVFFKMNSLQSNDTAIYYCARALTYYDYEFAYWGQGTLVTVSA
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Heavy Chain Constant Domain 1
ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRV
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Heavy Chain Constant Domain 2
APELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTK
PREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAK
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Heavy Chain Constant Domain 3
GQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDS
DGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Heavy Chain Hinge Region
EPKSCDKTHTCPPCP
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Heavy Chain CDR 1
GFSLTNYG
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Heavy Chain CDR 2
IWSGGNT
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Heavy Chain CDR 3
ARALTYYDYEFAY
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Light Chain Sequence
DILLTQSPVILSVSPGERVSFSCRASQSIGTNIHWYQQRTNGSPRLLIKYASESISGIPS
RFSGSGSGTDFTLSINSVESEDIADYYCQQNNNWPTTFGAGTKLELKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGA
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Light Chain Varible Domain
DILLTQSPVILSVSPGERVSFSCRASQSIGTNIHWYQQRTNGSPRLLIKYASESISGIPS
RFSGSGSGTDFTLSINSVESEDIADYYCQQNNNWPTTFGAGTKLELK
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Light Chain Constant Domain
RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD
SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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Light Chain CDR 1
QSIGTN
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Light Chain CDR 2
YAS
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Light Chain CDR 3
QQNNNWPTT
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Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
Cet-TPL [Investigative]
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 72.17% (Day 13) Positive EGFR expression (EGFR +++/++)
Method Description
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model Lung adenocarcinoma PDX model (PDX: PDX1)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 91.89% (Day 15) Positive EGFR expression (EGFR +++/++)
Method Description
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model Lung adenocarcinoma PDX model (PDX: PDX1)
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) ≈ 12.39% (Day 15) Negative EGFR expression (EGFR -)
Method Description
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model H520 CDX model
In Vitro Model Lung squamous cell carcinoma NCI-H520 cells CVCL_1566
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 64.00% (Day 18) Positive EGFR expression (EGFR +++/++)
Method Description
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model A549 CDX model
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 93.80% (Day 24) Positive EGFR expression (EGFR +++/++)
Method Description
When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model SCC6 CDX model
In Vitro Model Squamous cell carcinoma UM-SCC-6 cells CVCL_7773
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
6.25 ug/mL - 12.5 ug/mL
Positive EGFR expression (EGFR +++/++)
Method Description
For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
In Vitro Model Squamous cell carcinoma UM-SCC-6 cells CVCL_7773
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
12.50 ug/mL
Positive EGFR expression (EGFR +++/++)
Method Description
For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
12.50 ug/mL
Positive EGFR expression (EGFR +++/++)
Method Description
For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
In Vitro Model Lung large cell carcinoma NCI-H1299 cells CVCL_0060
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100.00 ug/mL Negative EGFR expression (EGFR -)
Method Description
For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
In Vitro Model Lung squamous cell carcinoma NCI-H520 cells CVCL_1566
EGFR ADC-22 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00% (Day 40) Negative EGFR expression (EGFR -)
Method Description
After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 NCI-H2228 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model NCI-H2228 CDX model
In Vitro Model Lung adenocarcinoma NCI-H2228 cells CVCL_1543
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.65% (Day 40) Positive EGFR expression (EGFR +++/++)
Method Description
After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 HCC827 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model HCC827 CDX model
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.50 nM±0.10 nM
Positive EGFR expression (EGFR +++/++)
Method Description
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 500 nM Negative EGFR expression (EGFR -)
Method Description
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model Lung adenocarcinoma NCI-H2228 cells CVCL_1543
EGFR ADC-21 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00% (Day 40) Negative EGFR expression (EGFR -)
Method Description
After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 NCI-H2228 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model NCI-H2228 CDX model
In Vitro Model Lung adenocarcinoma NCI-H2228 cells CVCL_1543
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.65% (Day 40) Positive EGFR expression (EGFR +++/++)
Method Description
After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 HCC827 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model HCC827 CDX model
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.50 nM±0.10 nM
Positive EGFR expression (EGFR +++/++)
Method Description
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 500 nM Negative EGFR expression (EGFR -)
Method Description
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model Lung adenocarcinoma NCI-H2228 cells CVCL_1543
CTX-MMAE [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 12 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 12.50% (Day 10 Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model MIA PaCa-2 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 15.63% (Day 20) Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 45.63% (Day 20) Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 4 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 54.17% (Day 10) Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model MIA PaCa-2 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Experiment 5 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87.50% (Day 20) Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 6 Reporting the Activity Date of This ADC [3]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 10) Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model MIA PaCa-2 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Experiment 7 Reporting the Activity Date of This ADC [3]
Efficacy Data Median survival time (MST)
14 Day
Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model MIA PaCa-2 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Experiment 8 Reporting the Activity Date of This ADC [3]
Efficacy Data Median survival time (MST)
23 Day
Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 9 Reporting the Activity Date of This ADC [3]
Efficacy Data Median survival time (MST)
24 Day
Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model MIA PaCa-2 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Experiment 10 Reporting the Activity Date of This ADC [3]
Efficacy Data Median survival time (MST)
30 Day
Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 11 Reporting the Activity Date of This ADC [3]
Efficacy Data Median survival time (MST)
60 Day
Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model MIA PaCa-2 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Experiment 12 Reporting the Activity Date of This ADC [3]
Efficacy Data Median survival time (MST)
61 Day
Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
39.00 pM
Positive EGFR expression (EGFR +++/++)
Method Description
MIA PaCa-2 and PANC-1 cells were seeded at 1000 and 1500 per well, respectively, in a 96-well plate and left to adhere overnight. Cells were treated with a 5-fold dilution series of CTX-MMAE or CTX ranging from 0.000256 to 500 nM for 96 h.
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.38 nM
Positive EGFR expression (EGFR +++/++)
Method Description
MIA PaCa-2 and PANC-1 cells were seeded at 1000 and 1500 per well, respectively, in a 96-well plate and left to adhere overnight. Cells were treated with a 5-fold dilution series of CTX-MMAE or CTX ranging from 0.000256 to 500 nM for 96 h.
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Cetuximab- (FGX16-11) [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 42.79% (Day 36) High EGFR expression (EGFR+++)
Method Description
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 1 mg/kg.
In Vivo Model Colon cancer CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 63.01% (Day 36) High EGFR expression (EGFR+++)
Method Description
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 5 mg/kg.
In Vivo Model Colon cancer CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 92.22% (Day 36) High EGFR expression (EGFR+++)
Method Description
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 10 mg/kg.
In Vivo Model Colon cancer CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.98% (Day 36) High EGFR expression (EGFR+++)
Method Description
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 20 mg/kg.
In Vivo Model Colon cancer CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 5 Reporting the Activity Date of This ADC [4]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 36) High EGFR expression (EGFR+++)
Method Description
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 40 mg/kg.
In Vivo Model Colon cancer CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
EGFR-MMAU ADC [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 84.20% (Day 33) Positive EGFR expression (EGFR+++/++)
Method Description
MMAU ADCs (3 mg/kg, intravenously four times at seven day intervals) induces efficient tumor cell killing in cell line-derived models of HSC-2 cells with EGFR expression with high expression.
In Vivo Model HSC-2 CDX model
In Vitro Model Oral cavity squamous cell carcinoma HSC-2 cells CVCL_1287
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.30% (Day 33) Positive EGFR expression (EGFR+++/++)
Method Description
MMAU ADCs (10 mg/kg, intravenously four times at seven day intervals) induces efficient tumor cell killing in cell line-derived models of HSC-2 cells with EGFR expression with high expression.
In Vivo Model HSC-2 CDX model
In Vitro Model Oral cavity squamous cell carcinoma HSC-2 cells CVCL_1287
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
25.00 pM
Low EGFR expression (EGFR+)
Method Description
Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model Non-small cell lung carcinoma NCI-H522 cells CVCL_1567
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
30.00 pM
High EGFR expression (EGFR+++)
Method Description
Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
ITcetuximab [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85.00% (Day 16) Positive EGFR expression (EGFR +++/++)
Method Description
Mice were injected intraperitoneally with 3 mg/kg of ITcetuximab, and 2days later,2 h after the administration of NPe6 (5 mg/kg) via the tail vein, the tumors were irradiated with a 664 nm laser at a dose of 30 J/cm2 from the diode laser unit.
In Vivo Model A549 CDX model
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.36 nM
High EGFR expression (EGFR +++)
Method Description
Cancer cell lines were incubated with compounds for 72 h. IC50 was evaluated from the sigmoid curve obtained using the curvefitting tool of the ImageJ software.
In Vitro Model Skin squamous cell carcinoma A-431 cells CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.77 nM
Positive EGFR expression (EGFR +++/++)
Method Description
Cancer cell lines were incubated with compounds for 72 h. IC50 was evaluated from the sigmoid curve obtained using the curvefitting tool of the ImageJ software.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC [6]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 nM Low EGFR expression (EGFR +)
Method Description
Cancer cell lines were incubated with compounds for 72 h. IC50 was evaluated from the sigmoid curve obtained using the curvefitting tool of the ImageJ software.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Hu-Alpha-EGFR-172 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [7]
Efficacy Data Tumor Growth Inhibition value (TGI)
90.30% (Day 18)
High EGFR expression (EGFR+++)
Method Description
To test the effect of STING ADCs in vivo, we used a mouse tumor model in which the C57BL/6J mice were implanted subcutaneously with B16F10 melanoma cells stably expressing human EGFR (B16-EGFR). After the tumors grew to ~100 mm 3 , STING ADCs were administered to the mice through intraperitoneal injection three times (200 g each time on day 5, 8, and 11 after tumor cell inoculation).

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In Vivo Model Melanoma CDX model
In Vitro Model Mouse melanoma B16-F10 cells CVCL_0159
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 [7]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 uM Negative EGFR expression (EGFR-)
Method Description
Serial dilutions of IMSA172 or its conjugates with the indicated antibodies (ADCs) were incubated with THP1-ISG-Luc or this cell line stably expressing human EGFR (THP1-ISG-luc-EGFR; B and D) for 16 h, and the interferon response was measured by luciferase assay.
In Vitro Model Acute monocytic leukemia THP1-Lucia ISG cells CVCL_X587
Cetuximab-vc-MMAE [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [8]
Efficacy Data Inhibition rate (50 nM)
92.00%
High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description
Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC [8]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.10 nM
High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description
Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC [8]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.00 nM
Method Description
Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Normal NHEK-iPSCs #1 cells CVCL_A4HY
Experiment 4 Reporting the Activity Date of This ADC [8]
Efficacy Data 80% Effective Dose (ED80)
0.70 nM
High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description
Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Cetuximab-Comound (Ia) [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.66 pM
Positive EGFR expression (EGFR+++/++)
Method Description
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model Biphasic synovial sarcoma Aska-SS cells CVCL_6C43
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.57 pM
Positive EGFR expression (EGFR+++/++)
Method Description
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model Monophasic synovial sarcoma HS-SY-2 cells CVCL_8719
Cetux Cys-vc-MMAE [Investigative]
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 [10]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 nM
High EGFR expression (EGFR+++/++)
Method Description
Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR. After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model Glioblastoma U-87MG cells CVCL_0022
MAb-DMBA-SIL-MMAE [Investigative]
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 [11]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 nM
Method Description
Cytotoxicity of non-irradiated or X-ray-irradiated (8 Gy) mAb-DMBA-SIL-MMAE conjugate in comparison to free MMAE in anaplastic thyroid cancer.
In Vitro Model Thyroid gland anaplastic carcinoma 8505C cells CVCL_1054
WO2017089895A1 ADC66 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.11 nM
Moderate EGFR expression (EGFR++)
Method Description
The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.30 nM Low EGFR expression (EGFR+)
Method Description
The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC66 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.11 nM
Moderate EGFR expression (EGFR++)
Method Description
The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.30 nM Negative EGFR expression (EGFR-)
Method Description
The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC65 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.17 nM
Moderate EGFR expression (EGFR++)
Method Description
The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.30 nM Low EGFR expression (EGFR+)
Method Description
The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC65 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.17 nM
Moderate EGFR expression (EGFR++)
Method Description
The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.30 nM Negative EGFR expression (EGFR-)
Method Description
The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
C-IgG-Val-Cit-MMAE [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [14]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.44±0.03 nM
High EGFR expression (EGFR+++/++)
Method Description
The inhibitory activity of C-IgG-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC [14]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100.00 nM Negative EGFR expression (EGFR-)
Method Description
The inhibitory activity of C-IgG-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC [19]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.40 nM
Low FOLR1 expression (FOLR1+)
Method Description
The inhibitory activity of C-IgG-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
WO2017089895A1 ADC64 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.47 nM
Moderate EGFR expression (EGFR++)
Method Description
The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.30 nM
High EGFR expression (EGFR+++)
Method Description
The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC [12]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.30 nM Low EGFR expression (EGFR+)
Method Description
The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC64 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.47 nM
Moderate EGFR expression (EGFR++)
Method Description
The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.30 nM
High EGFR expression (EGFR+++)
Method Description
The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC [13]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.30 nM Negative EGFR expression (EGFR-)
Method Description
The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
EGFR ADC-23 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.80 nM±0.10 nM
Positive EGFR expression (EGFR +++/++)
Method Description
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 500 nM Negative EGFR expression (EGFR -)
Method Description
ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model Lung adenocarcinoma NCI-H2228 cells CVCL_1543
Cet-DM1 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [15]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.85 nM
High EGFR expression (EGFR+++/++)
Method Description
HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model HCC1954/TDR CDX model (CDX: C#10)
In Vitro Model Breast ductal carcinoma HCC1954 T-DM1R (T-DM1 resistance) cells CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC [15]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.85 nM
High EGFR expression (EGFR+++/++)
Method Description
HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model HCC1954/TDR CDX model (CDX: C#19)
In Vitro Model Breast ductal carcinoma HCC1954 T-DM1R (T-DM1 resistance) cells CVCL_1259
Experiment 3 Reporting the Activity Date of This ADC [15]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.41 nM
High EGFR expression (EGFR+++/++)
Method Description
HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 4 Reporting the Activity Date of This ADC [15]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.52 nM
High EGFR expression (EGFR+++/++)
Method Description
HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model HCC1954/TDR CDX model (CDX: C#20)
In Vitro Model Breast ductal carcinoma HCC1954 T-DM1R (T-DM1 resistance) cells CVCL_1259
Experiment 5 Reporting the Activity Date of This ADC [15]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.68 nM
High EGFR expression (EGFR+++/++)
Method Description
HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model HCC1954/TDR CDX model (CDX: C#29)
In Vitro Model Breast ductal carcinoma HCC1954 T-DM1R (T-DM1 resistance) cells CVCL_1259
WO2022078260A1 ADC-9 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.11 nM
Positive HER2 expression (EPHA2+++/++)
Method Description
Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.02 nM
Positive HER2 expression (EPHA2+++/++)
Method Description
Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
WO2022078260A1 ADC-10 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.15 nM
Positive HER2 expression (EPHA2+++/++)
Method Description
Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.54 nM
Positive HER2 expression (EPHA2+++/++)
Method Description
Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Quinoin cetuximab immunoconjugate [Investigative]
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 [17]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
27.70 nM
Positive EGFR expression (EGFR +++/++)
Method Description
Cells were treated with different concentrations of drugs for 72 h. The viability was determined using the MTT assay.
In Vitro Model Colon carcinoma GEO cells (Cetuximab-resistant) CVCL_0271
Cetuximab-Puromycin [Investigative]
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 [18]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
37.42 ug/mL
High EGFR expression (EGFR+++)
Method Description
Cells were seeded into 6-well plates, 500,000 cells/well. One day (24 hours) before treatment, MDA-MB-231 cells are being fasted from FBS. Cells are divided into five different doses of conjugate (5 ug/mL; 10 ug/mL; 20 ug/mL; 40 ug/mL; 80 ug/mL) and one untreated group. They were incubated for 48 hours.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
EGFR-ADC-07 (DAR8) [Investigative]
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 [20]
Efficacy Data Half Maximal Effective Concentration (EC50)
11.56 ng/mL
Positive EGFR expression (EGFR +++/++)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Esophageal squamous cell carcinoma KYSE-520 cells CVCL_1355
EGFR-ADC-07 (DAR4) [Investigative]
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 [20]
Efficacy Data Half Maximal Effective Concentration (EC50)
18.17 ng/mL
Positive EGFR expression (EGFR +++/++)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Esophageal squamous cell carcinoma KYSE-520 cells CVCL_1355
EGFR-ADC-32 (DAR4) [Investigative]
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 [20]
Efficacy Data Half Maximal Effective Concentration (EC50)
29.21 ng/mL
Positive EGFR expression (EGFR +++/++)
Method Description
Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model Esophageal squamous cell carcinoma KYSE-520 cells CVCL_1355
References
Ref 1 Cetuximab-Triptolide Conjugate Suppresses the Growth of EGFR-Overexpressing Lung Cancers through Targeting RNA Polymerase II. Mol Ther Oncolytics. 2020 Jul 6;18:304-316. doi: 10.1016/j.omto.2020.07.001. eCollection 2020 Sep 25.
Ref 2 Divinylsulfonamides enable the construction of homogeneous antibody-drug conjugates. Bioorg Med Chem. 2020 Dec 1;28(23):115793. doi: 10.1016/j.bmc.2020.115793. Epub 2020 Oct 6.
Ref 3 Two engineered site-specific antibody-drug conjugates, HLmD4 and HLvM4, have potent therapeutic activity in two DLL4-positive tumour xenograft models. Am J Cancer Res. 2020 Aug 1;10(8):2387-2408. eCollection 2020.
Ref 4 DNA sequence-selective G-A cross-linking ADC payloads for use in solid tumour therapies. Commun Biol. 2022 Jul 29;5(1):741.
Ref 5 Hydrophilic Auristatin Glycoside Payload Enables Improved Antibody-Drug Conjugate Efficacy and Biocompatibility. Antibodies (Basel). 2018 Mar 22;7(2):15. doi: 10.3390/antib7020015.
Ref 6 Development of a new minimally invasive phototherapy for lung cancer using antibody-toxin conjugate. Thorac Cancer. 2023 Mar;14(7):645-653. doi: 10.1111/1759-7714.14776. Epub 2023 Jan 19.
Ref 7 Tumor-targeted delivery of a STING agonist improvescancer immunotherapy. Proc Natl Acad Sci U S A. 2022 Dec 6;119(49):e2214278119.
Ref 8 Balancing Selectivity and Efficacy of Bispecific Epidermal Growth Factor Receptor (EGFR) c-MET Antibodies and Antibody-Drug Conjugates. J Biol Chem. 2016 Nov 25;291(48):25106-25119. doi: 10.1074/jbc.M116.753491. Epub 2016 Sep 30.
Ref 9 Neodegrader conjugates; 2021-10-07.
Ref 10 MAbs. 2023 Jan-Dec;15(1):2149057. doi: 10.1080/19420862.2022.2149057.
Ref 11 Radiation Cleaved Drug-Conjugate Linkers Enable Local Payload Release. Bioconjug Chem. 2022 Aug 17;33(8):1474-1484.
Ref 12 Antibody-drug conjugates comprising branched linkers and methods related thereto; 2017-06-01.
Ref 13 Conjugates comprising self-immolative groups and methods related thereto.
Ref 14 EGFR binding Fc domain-drug conjugates: stable and highly potent cytotoxic molecules mediate selective cell killing. Biol Chem. 2021 Sep 20;403(5-6):525-534.
Ref 15 An anti-EGFR antibody-drug conjugate overcomes resistance to HER2-targeted drugs. Cancer Lett. 2023 Feb 1;554:216024.
Ref 16 Camptothecin derivative and ligand-drug conjugate thereof; 2022-04-21.
Ref 17 A Novel EGFR Targeted Immunotoxin Based on Cetuximab and Type 1 RIP Quinoin Overcomes the Cetuximab Resistance in Colorectal Cancer Cells. Toxins (Basel). 2023 Jan 9;15(1):57. doi: 10.3390/toxins15010057.
Ref 18 Conjugation of Cetuximab - Puromycin and Its Target-Specific Effect on Triple Negative Breast Cancer Cell Lines. Asian Pac J Cancer Prev. 2022 May 1;23(5):1803-1812.
Ref 19 Discovery of STRO-002, a Novel Homogeneous ADC Targeting Folate Receptor Alpha, for the Treatment of Ovarian and Endometrial Cancers. Mol Cancer Ther. 2023 Feb 1;22(2):155-167.
Ref 20 Bioactive substance conjugate, preparation method therefor and use thereof; 2022-08-18.

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