General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0NJJCX
ADC Name
Hu005-44-MMAE
Synonyms
Hu005-44-MMAE
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Organization
Hefei Institutes of Physical Science
Drug Status
Investigative
Drug-to-Antibody Ratio
4.12
Structure
Antibody Name
Hu005-44
 Antibody Info 
Antigen Name
Inactive tyrosine-protein kinase transmembrane receptor ROR1 (ROR1)
 Antigen Info 
Payload Name
Monomethyl auristatin E
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Mc-Val-Cit-PABC
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
Vedotin
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth lnhibition value (TGl) 
22.14
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
45.08
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
64.97
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
93.69
%
Undisclosed Undisclosed
Revealed Based on the Cell Line Data
Click To Hide/Show 11 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
1.58
nM
CVCL_0479
Ovarian mixed germ cell tumor
Half Maximal inhibitory Concentration (lC50) 
2.95
nM
CVCL_1562
Lung small cell carcinoma
Half Maximal inhibitory Concentration (lC50) 
3.84
nM
CVCL_1247
Breast ductal carcinoma
Half Maximal inhibitory Concentration (lC50) 
5.16
nM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
9.11
nM
CVCL_0626
Colon adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
10.32
nM
CVCL_0062
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
11.57
nM
CVCL_1129
Colon carcinoma
Half Maximal inhibitory Concentration (lC50) 
16.85
nM
CVCL_0320
Colon adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
19.99
nM
CVCL_2063
Lung adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
> 100
nM
CVCL_0033
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
> 100
nM
CVCL_0031
Invasive breast carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) 22.14% High ROR1 expression (ROR1 +++)
Method Description
Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (PA-1) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model NCI-N87 xenograft model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) 45.08% High ROR1 expression (ROR1 +++)
Method Description
Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (MDA-MB-231) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.

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In Vivo Model MDA-MB-231 xenograft model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) 64.97% High ROR1 expression (ROR1 +++)
Method Description
Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (PA-1) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model NCI-N87 xenograft model
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) 93.69% High ROR1 expression (ROR1 +++)
Method Description
Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (MDA-MB-231) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model MDA-MB-231 xenograft model
Revealed Based on the Cell Line Data
Click To Hide/Show 11 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 1.58 nM High ROR1 expression (ROR1 +++)
Method Description
A total of 250-1500cells (PA-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.

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In Vitro Model Ovarian mixed germ cell tumor PA-1 cells CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 2.95 nM High ROR1 expression (ROR1 +++)
Method Description
A total of 250-1500cells (NCI-H446) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.

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In Vitro Model Lung small cell carcinoma NCI-H446 cells CVCL_1562
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 3.84 nM High ROR1 expression (ROR1 +++)
Method Description
A total of 250-1500cells (HCC1187) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.

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In Vitro Model Breast ductal carcinoma HCC1187 cells CVCL_1247
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 5.16 nM High ROR1 expression (ROR1 +++)
Method Description
A total of 250-1500cells (NCI-N87) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 9.11 nM High ROR1 expression (ROR1 +++)
Method Description
A total of 250-1500cells (SK-CO-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.

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In Vitro Model Colon adenocarcinoma SKCO1 cells CVCL_0626
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 10.32 nM High ROR1 expression (ROR1 +++)
Method Description
A total of 250-1500cells (MDA-MB-231) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.

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In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 11.57 nM Moderate ROR1 expression (ROR1++)
Method Description
A total of 250-1500cells (COLO-678) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.

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In Vitro Model Colon carcinoma COLO-678 cells CVCL_1129
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 16.85 nM High ROR1 expression (ROR1 +++)
Method Description
A total of 250-1500cells (HT-29) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.

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In Vitro Model Colon adenocarcinoma HT-29 cells CVCL_0320
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 19.99 nM High ROR1 expression (ROR1 +++)
Method Description
A total of 250-1500cells (HCC827) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.

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In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Positive ROR1 expression (ROR1+++/++)
Method Description
A total of 250-1500cells (SK-BR-3) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Low ROR1 expression (ROR1+)
Method Description
A total of 250-1500cells (MCF-7) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Antibodies specifically binding ROR1, their drug conjugates, preparation methods and uses