Antibody Information
General Information of This Antibody
Antibody ID | ANI0GYJQM |
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Antibody Name | Cetuximab |
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Brand Name | ERBITUX |
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Organization | Bristol-Myers Squibb; Merck & Co., Inc. |
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Indication | Colorectal cancer; Head and neck squamous cell carcinoma; Esophageal cancer |
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Approval Date | Feb. 2004 |
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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) |
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Antibody Subtype | Chimeric IgG1-kappa |
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Antigen Name | Epidermal growth factor receptor (EGFR) |
Antigen Info | ||||
ChEMBI ID | ||||||
PDB ID | ||||||
DrugBank ID | ||||||
Drug Central ID | ||||||
Click to Show/Hide the Sequence Information of This Antibody | ||||||
Heavy Chain Sequence |
QVQLKQSGPGLVQPSQSLSITCTVSGFSLTNYGVHWVRQSPGKGLEWLGVIWSGGNTDYN
TPFTSRLSINKDNSKSQVFFKMNSLQSNDTAIYYCARALTYYDYEFAYWGQGTLVTVSAA STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSPKSCDKTHTCPPCPAPELL GGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQ YNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSR DELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKS RWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK Click to Show/Hide
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Heavy Chain Varible Domain |
QVQLKQSGPGLVQPSQSLSITCTVSGFSLTNYGVHWVRQSPGKGLEWLGVIWSGGNTDYN
TPFTSRLSINKDNSKSQVFFKMNSLQSNDTAIYYCARALTYYDYEFAYWGQGTLVTVSA Click to Show/Hide
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Heavy Chain Constant Domain 1 |
ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRV Click to Show/Hide
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Heavy Chain Constant Domain 2 |
APELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTK
PREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAK Click to Show/Hide
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Heavy Chain Constant Domain 3 |
GQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDS
DGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK Click to Show/Hide
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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 Click to Show/Hide
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Light Chain Varible Domain |
DILLTQSPVILSVSPGERVSFSCRASQSIGTNIHWYQQRTNGSPRLLIKYASESISGIPS
RFSGSGSGTDFTLSINSVESEDIADYYCQQNNNWPTTFGAGTKLELK Click to Show/Hide
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Light Chain Constant Domain |
RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD
SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC Click to Show/Hide
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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
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.
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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.
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In Vivo Model | Lung adenocarcinoma PDX model (PDX: PDX1) |
Discovered Using Cell Line-derived Xenograft Model
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.
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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.
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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.
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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
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
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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.
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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
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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.
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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
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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.
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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.
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In Vitro Model | Lung squamous cell carcinoma | NCI-H520 cells | CVCL_1566 |
EGFR ADC-22 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
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.
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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.
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In Vivo Model | HCC827 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | HCC827 cells | CVCL_2063 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.50 nM±0.10 nM
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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.
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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.
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In Vitro Model | Lung adenocarcinoma | NCI-H2228 cells | CVCL_1543 |
EGFR ADC-21 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
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.
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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.
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In Vivo Model | HCC827 CDX model | ||||
In Vitro Model | Lung adenocarcinoma | HCC827 cells | CVCL_2063 |
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.50 nM±0.10 nM
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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.
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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.
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In Vitro Model | Lung adenocarcinoma | NCI-H2228 cells | CVCL_1543 |
CTX-MMAE [Investigative]
Discovered Using Cell Line-derived Xenograft Model
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).
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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).
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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).
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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).
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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).
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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).
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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
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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).
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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
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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).
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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
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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).
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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
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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).
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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
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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).
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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
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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).
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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
Experiment 1 Reporting the Activity Date of This ADC | [3] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
39.00 pM
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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.
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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
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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.
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In Vitro Model | Pancreatic ductal adenocarcinoma | MIA PaCa-2 cells | CVCL_0428 |
Cetuximab- (FGX16-11) [Investigative]
Discovered Using Cell Line-derived Xenograft Model
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.
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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.
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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.
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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.
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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.
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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
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.
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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.
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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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
Experiment 1 Reporting the Activity Date of This ADC | [20] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
29.21 ng/mL
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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.
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In Vitro Model | Esophageal squamous cell carcinoma | KYSE-520 cells | CVCL_1355 |
References
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