Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0LCPTG
ADC Name
CN119371541A 99961.1-MMAE
Synonyms
99961.1-MMAE
   Click to Show/Hide
Organization
Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd.
Drug Status
Investigative
Drug-to-Antibody Ratio
3.8
Antibody Name
99961.1
  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
ADC-specific functional property(2027 Update)
Bystander Killing Effect
Click To Hide/Show 1 ADC-specific functional property Data
Bystander Killing Effect Description Reference
no Undisclosed
[1]
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 15 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth lnhibition value (TGl) 
11.08
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
15.9
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
34.6
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
37.81
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
59.22
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
64.31
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
67.66
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
89.35
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
91.74
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
95.77
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
96.6
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
97.86
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
98.21
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
99.2
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
100
%
Undisclosed Undisclosed
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 Effective Concentration (EC50) 
21.22
nM
CVCL_0419
Breast adenocarcinoma
Half Maximal Effective Concentration (EC50) 
44.56
nM
CVCL_1865
Mantle cell lymphoma
Half Maximal Effective Concentration (EC50) 
80.79
nM
CVCL_0320
Colon adenocarcinoma
Half Maximal Effective Concentration (EC50) 
82.09
nM
CVCL_0320
Colon adenocarcinoma
Half Maximal Effective Concentration (EC50) 
102.8
nM
CVCL_1508
Lung adenocarcinoma
Half Maximal Effective Concentration (EC50) 
250.7
nM
CVCL_0023
Lung adenocarcinoma
Half Maximal Effective Concentration (EC50) 
295.6
nM
CVCL_0023
Lung adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 15 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
11.08%
Method Description
Cell line-derived xenograft models were established in nude mice by subcutaneous injection of 1x106 (HT-29) tumor cells, and treatment with 0.4mg/kg 99961.1-MMAE (BIW&#424) was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model HT-29 xenograft model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
15.90%
Method Description
Cell line-derived xenograft models were established in nude mice by subcutaneous injection of 1x106 (HT-29) tumor cells, and treatment with 2mg/kg 99961.1-MMAE (BIW&#424) was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model HT-29 xenograft model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
34.60%
Method Description
Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x107 (Jeko-1) tumor cells,and treatment with 2.5 (D15)/3.5 (D29)mpk 99961.1-MMAE (Q2W&#422)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 41.
In Vivo Model Jeko-1 xenograft model
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
37.81%
Method Description
Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (A549) tumor cells,and treatment with 10mpk (mg/kg)99961.1-MMAE (BIW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 48.
In Vivo Model A549 xenograft model
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
59.22%
Method Description
Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x107 (Jeko-1) tumor cells,and treatment with 2.5mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 41.
In Vivo Model Jeko-1 xenograft model
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
64.31%
Method Description
Cell line-derived xenograft models were established in female nude mice (NOD),by subcutaneous injection of 1x107 (MDA-MB-468) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (single dose)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model MDA-MB-468 xenograft model
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
67.66%
Method Description
Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (MDA-MB-231) tumor cells,and treatment with 5mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model MDA-MB-231 xenograft model
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
89.35%
Method Description
Cell line-derived xenograft models were established in nude mice by subcutaneous injection of 1x106 (HT-29) tumor cells, and treatment with 10mg/kg 99961.1-MMAE (BIW&#424) was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model HT-29 xenograft model
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
91.74%
Method Description
Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x107 (Jeko-1) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (single dose)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 41.
In Vivo Model Jeko-1 xenograft model
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
95.77%
Method Description
Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x107 (Jeko-1) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 41.
In Vivo Model Jeko-1 xenograft model
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
96.60%
Method Description
Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (MDA-MB-231) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model MDA-MB-231 xenograft model
Experiment 12 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
97.86%
Method Description
Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (NCI-N87) tumor cells,and treatment with 5mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model NCI-N87 xenograft model
Experiment 13 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
98.21%
Method Description
Cell line-derived xenograft models were established in female nude mice (NOD),by subcutaneous injection of 1x107 (MDA-MB-468) tumor cells,and treatment with 5mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model MDA-MB-468 xenograft model
Experiment 14 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
99.20%
Method Description
Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (NCI-N87) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model NCI-N87 xenograft model
Experiment 15 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
100%
Method Description
Cell line-derived xenograft models were established in female nude mice (NOD),by subcutaneous injection of 1x107 (MDA-MB-468) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model MDA-MB-468 xenograft model
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 Effective Concentration (EC50) 21.22 nM High ROR1 expression (ROR1 +++)
Method Description
MDA-MB-468 cell line was plated at 2×105cell/mL, 90uL/well,12 hours later, ADCs (500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, 0.05nM) were added and incubated for 72h,then 10uL CCK8 (Bimake,B34304)was added to each well and a microplate reader was used for detection OD492.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
44.56 nM
Method Description
Jeko-1 cell line was plated at 1×105cell/mL, 90uL/well,12 hours later, ADCs (500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, 0.05nM) were added and incubated for 72h,then 10uL CCK8 (Bimake,B34304)was added to each well and a microplate reader was used for detection OD492.
In Vitro Model Mantle cell lymphoma JeKo-1 cells CVCL_1865
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
80.79 nM
Method Description
HT-29 cell line (1×104cell/mL,100uL/well) , the ADCs (2000, 500, 250, 125, 62.5, 31.25, 15.625, 7.813, 1.953nM) were added 12 hours later, and incubated for 96h, then 40uL/well MTS (Promega,G3580) was added to each well and a microplate reader was used for detection OD492.
In Vitro Model Colon adenocarcinoma HT-29 cells CVCL_0320
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
82.09 nM
Method Description
HT-29 cell line (1×104cell/mL,100uL/well) , the ADCs (2000, 500, 250, 125, 62.5, 31.25, 15.625, 7.813, 1.953nM) were added 12 hours later, and incubated for 96h, then 40uL/well MTS (Promega,G3580) was added to each well and a microplate reader was used for detection OD492.
In Vitro Model Colon adenocarcinoma HT-29 cells CVCL_0320
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50)
102.8 nM
Method Description
NCI-H1944 cell line was plated at 1.2×105cell/mL, 90uL/well,12 hours later, ADCs (500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, 0.05nM) were added and incubated for 72h,then 10uL CCK8 (Bimake,B34304)was added to each well and a microplate reader was used for detection OD492.
In Vitro Model Lung adenocarcinoma NCI-H1944 cells CVCL_1508
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 250.7 nM Moderate ROR1 expression (ROR1++)
Method Description
A549 at 1×104cell/mL,100uL/well, 12 hours later,ADCs (2000, 500, 250, 125, 62.5, 31.25, 15.625, 7.813, 1.953nM) were added and incubated for 72h, then 40uL/well MTS (Promega,G3580) was added to each well and a microplate reader was used for detection OD492.
In Vitro Model Lung adenocarcinoma A549 cells CVCL_0023
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 295.6 nM Moderate ROR1 expression (ROR1++)
Method Description
A549 at 1×104cell/mL,100uL/well, 12 hours later,ADCs (2000, 500, 250, 125, 62.5, 31.25, 15.625, 7.813, 1.953nM) were added and incubated for 72h, then 40uL/well MTS (Promega,G3580) was added to each well and a microplate reader was used for detection OD492.
In Vitro Model Lung adenocarcinoma A549 cells CVCL_0023
References
Ref 1 Binding molecules targeting ROR1 and uses thereof