General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0XEYCE
ADC Name
AXL02-MMAE
Synonyms
AXL02-MMAE
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Organization
Fudan University School of Pharmacy.; Shanghai Institute of Materia Medica, Chinese Academy of Sciences.
Drug Status
Investigative
Drug-to-Antibody Ratio
4
Structure
Antibody Name
AXL02
 Antibody Info 
Antigen Name
Tyrosine-protein kinase receptor UFO (AXL)
 Antigen Info 
Payload Name
Monomethyl auristatin E
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Undisclosed
Conjugate Type
DBCO-Azide Click Chemistry Conjugation
Combination Type
Vedotin
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 7 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
< 0.1
nM
CVCL_1375
Lung large cell carcinoma
Half Maximal inhibitory Concentration (lC50) 
< 0.1
nM
CVCL_0332
Invasive breast carcinoma of no special type
Half Maximal inhibitory Concentration (lC50) 
< 0.1
nM
CVCL_B260
Lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
< 0.1
nM
CVCL_0022
Glioblastoma
Half Maximal inhibitory Concentration (lC50) 
< 0.1
nM
CVCL_0062
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
< 0.1
nM
CVCL_0608
Lung squamous cell carcinoma
Half Maximal inhibitory Concentration (lC50) 
> 100
nM
CVCL_0418
Breast adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.1 nM High AXL expression (AXL +++)
Method Description
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.

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In Vitro Model Lung large cell carcinoma LCLC-103H cells CVCL_1375
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.1 nM High AXL expression (AXL +++)
Method Description
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.

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In Vitro Model Invasive breast carcinoma of no special type Hs578T cells CVCL_0332
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.1 nM High AXL expression (AXL +++)
Method Description
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.

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In Vitro Model Lung adenocarcinoma PC9 cells CVCL_B260
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.1 nM High AXL expression (AXL +++)
Method Description
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.

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In Vitro Model Glioblastoma U87 MG cells CVCL_0022
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.1 nM High AXL expression (AXL +++)
Method Description
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.

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In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) < 0.1 nM High AXL expression (AXL +++)
Method Description
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.

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In Vitro Model Lung squamous cell carcinoma Calu-1 cells CVCL_0608
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Low AXL expression (AXL+)
Method Description
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.

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In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
References
Ref 1 AXL antibody and AXL-ADC mediate antitumor efficacy via targeting AXL in tumor-intrinsic epithelial-mesenchymal transition and tumor-associated M2-like macrophage