Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0YJVVL
ADC Name
RAA22/B09-AZ1508
Synonyms
RAA22/B09 AZ1508
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Organization
AstraZeneca PLC
Drug Status
Investigative
Indication
In total 2 Indication(s)
Lung cancer [ICD11:2C25]
Investigative
Pancreatic cancer [ICD11:2C10]
Investigative
Drug-to-Antibody Ratio
2
Structure
Antibody Name
RAA22/B09
  Antibody Info 
Antigen Name
Epidermal growth factor receptor (EGFR); Hepatocyte growth factor receptor (MET)
  Antigen Info 
Payload Name
RAA22/B09-AZ1508
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
RAA22/B09-AZ1508
  Linker Info 
Conjugate Type
Site-specific conjugation through reduced inter-chain cysteines.
Combination Type
AZ1508
General Information of The Activity Data Related to This ADC
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 39 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST1104B)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST742)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST1749)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST2495)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST935B)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST2081)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST751)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST374)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST2891)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST1092B)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST1976B)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST115)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST551)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST551C)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST1506)
Tumor Growth Inhibition value (TGI) 
≈ 0
%
Lung cancer PDX model (PDX: ST599)
Tumor Growth Inhibition value (TGI) 
≈ 0-10
%
Lung cancer PDX model (PDX: ST1885)
Tumor Growth Inhibition value (TGI) 
≈ 0-10
%
Lung cancer PDX model (PDX: ST1328)
Tumor Growth Inhibition value (TGI) 
≈ 1.8
%
Pancreatic PDX model (PDX: MEDI-PANC-08)
Tumor Growth Inhibition value (TGI) 
≈ 10
%
Lung cancer PDX model (PDX: ST379)
Tumor Growth Inhibition value (TGI) 
≈ 11.16
%
Pancreatic PDX model (PDX: MEDI-PANC-08)
Tumor Growth Inhibition value (TGI) 
≈ 20
%
Lung cancer PDX model (PDX: ST1035B)
Tumor Growth Inhibition value (TGI) 
≈ 20
%
Lung cancer PDX model (PDX: ST396)
Tumor Growth Inhibition value (TGI) 
≈ 20
%
Lung cancer PDX model (PDX: ST140)
Tumor Growth Inhibition value (TGI) 
≈ 20
%
Lung cancer PDX model (PDX: ST1989)
Tumor Growth Inhibition value (TGI) 
≈ 20
%
Lung cancer PDX model (PDX: ST1151)
Tumor Growth Inhibition value (TGI) 
≈ 30
%
Lung cancer PDX model (PDX: ST1092B)
Tumor Growth Inhibition value (TGI) 
≈ 40
%
Lung cancer PDX model (PDX: ST1271)
Tumor Growth Inhibition value (TGI) 
≈ 50
%
Lung cancer PDX model (PDX: ST1243)
Tumor Growth Inhibition value (TGI) 
≈ 50
%
Lung cancer PDX model (PDX: ST1684)
Tumor Growth Inhibition value (TGI) 
≈ 70
%
Lung cancer PDX model (PDX: ST2822B)
Tumor Growth Inhibition value (TGI) 
≈ 79.28
%
Pancreatic PDX model (PDX: MEDI-PANC-08)
Tumor Growth Inhibition value (TGI) 
≈ 80
%
Lung cancer PDX model (PDX: ST137)
Tumor Growth Inhibition value (TGI) 
≈ 80
%
Lung cancer PDX model (PDX: ST1437)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Lung cancer PDX model (PDX: ST1229)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Lung cancer PDX model (PDX: ST698B)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Lung cancer PDX model (PDX: ST1976C)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Lung cancer PDX model (PDX: ST1906)
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Lung cancer PDX model (PDX: ST2869)
Revealed Based on the Cell Line Data
Click To Hide/Show 24 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Maximum inhibition efficiency (MIE) 
10
%
NCI-H661 cells
Lung large cell carcinoma
Maximum inhibition efficiency (MIE) 
30
%
NCI-H358 cells
Minimally invasive lung adenocarcinoma
Maximum inhibition efficiency (MIE) 
36
%
A-549 cells
Lung adenocarcinoma
Maximum inhibition efficiency (MIE) 
46
%
NCI-H23 cells
Lung adenocarcinoma
Maximum inhibition efficiency (MIE) 
55
%
HCC827 cells
Lung adenocarcinoma
Maximum inhibition efficiency (MIE) 
58
%
A-427 cells
Lung carcinoma
Maximum inhibition efficiency (MIE) 
59
%
HCC827-GR-step cells
Lung adenocarcinoma
Maximum inhibition efficiency (MIE) 
62
%
NCI-H292 cells
Lung mucoepidermoid carcinoma
Maximum inhibition efficiency (MIE) 
65
%
NCI-H1975 cells
Lung adenocarcinoma
Maximum inhibition efficiency (MIE) 
67
%
NCI-H596 cells
Lung adenosquamous carcinoma
Maximum inhibition efficiency (MIE) 
81
%
NCI-H1792 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.13
nM
HCC827 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.17
nM
HCC827-GR-step cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.2
nM
NCI-H1792 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.26
nM
NCI-H1975 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.27
nM
NCI-H292 cells
Lung mucoepidermoid carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.67
nM
A-549 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.68
nM
NCI-H1975 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
2.77
nM
NCI-H1975 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
3.02
nM
NCI-H358 cells
Minimally invasive lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
3.24
nM
NCI-H596 cells
Lung adenosquamous carcinoma
Half Maximal Inhibitory Concentration (IC50) 
8.1
nM
NCI-H23 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
40.22
nM
A-427 cells
Lung carcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 66.67
nM
NCI-H661 cells
Lung large cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 39 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1104B)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST742)
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1749)
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST2495)
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST935B)
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST2081)
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST751)
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST374)
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST2891)
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1092B)
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1976B)
Experiment 12 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST115)
Experiment 13 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST551)
Experiment 14 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST551C)
Experiment 15 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1506)
Experiment 16 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST599)
Experiment 17 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0%-10%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1885)
Experiment 18 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0%-10%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1328)
Experiment 19 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 1.80% (Day 32)
Method Description
To assist in the selection of the appropriate EGFR affinity combination for the EGFR-CMET bispecific ADC, high and low affinity EGFR-CMET bispecific ADCs (1 mg/kg.) were compared in an in vivo eficacy study usingthe MEDI-PANC-08 pancreatic PDX model.
In Vivo Model Pancreatic PDX model (PDX: MEDI-PANC-08)
Experiment 20 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 10.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST379)
Experiment 21 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 11.16% (Day 32)
Method Description
To assist in the selection of the appropriate EGFR affinity combination for the EGFR-CMET bispecific ADC, high and low affinity EGFR-CMET bispecific ADCs (2 mg/kg.) were compared in an in vivo eficacy study usingthe MEDI-PANC-08 pancreatic PDX model.
In Vivo Model Pancreatic PDX model (PDX: MEDI-PANC-08)
Experiment 22 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 20.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1035B)
Experiment 23 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 20.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST396)
Experiment 24 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 20.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST140)
Experiment 25 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 20.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1989)
Experiment 26 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 20.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1151)
Experiment 27 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 30.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1092B)
Experiment 28 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 40.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1271)
Experiment 29 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 50.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1243)
Experiment 30 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 50.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1684)
Experiment 31 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 70.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST2822B)
Experiment 32 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 79.28% (Day 32)
Method Description
To assist in the selection of the appropriate EGFR affinity combination for the EGFR-CMET bispecific ADC, high and low affinity EGFR-CMET bispecific ADCs (3 mg/kg.) were compared in an in vivo eficacy study usingthe MEDI-PANC-08 pancreatic PDX model.
In Vivo Model Pancreatic PDX model (PDX: MEDI-PANC-08)
Experiment 33 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST137)
Experiment 34 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1437)
Experiment 35 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1229)
Experiment 36 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST698B)
Experiment 37 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1976C)
Experiment 38 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST1906)
Experiment 39 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00%
Method Description
When tumors reached the appropriate Tumor Volume lnitiation (TVl) range (125-250 mm3), animalswere randomized into treatment and control groups and intravenous (lV) dosing was initiated (Day 0). lnitial dosing began on Day 0; animals in allgroups were dosed l.V. by weight (0.01 ml per gram; 10 ml/kg). Drug treated animals were dosed every 7days for a total of 4 doses.

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In Vivo Model Lung cancer PDX model (PDX: ST2869)
Revealed Based on the Cell Line Data
Click To Hide/Show 24 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 10.00% Negative EGFR expression (EGFR ++); Negative MET expression (MET -)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung large cell carcinoma NCI-H661 cells CVCL_1577
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 30.00% Moderate EGFR expression (EGFR ++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Minimally invasive lung adenocarcinoma NCI-H358 cells CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 36.00% Moderate EGFR expression (EGFR ++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 46.00% Low EGFR expression (EGFR ++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenocarcinoma NCI-H23 cells CVCL_1547
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 55.00% High EGFR expression (EGFR +++); High MET expression (MET +++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 58.00% Moderate EGFR expression (EGFR ++); Low MET expression (MET +)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung carcinoma A-427 cells CVCL_1055
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 59.00% High EGFR expression (EGFR +++); High MET expression (MET +++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenocarcinoma HCC827-GR-step cells CVCL_S705
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 62.00% Moderate EGFR expression (EGFR ++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 65.00% Moderate EGFR expression (EGFR ++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 67.00% High EGFR expression (EGFR +++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenosquamous carcinoma NCI-H596 cells CVCL_1571
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 81.00% Moderate EGFR expression (EGFR ++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenocarcinoma NCI-H1792 cells CVCL_1495
Experiment 12 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.13 nM High EGFR expression (EGFR +++); High MET expression (MET +++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 13 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.17 nM High EGFR expression (EGFR +++); High MET expression (MET +++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenocarcinoma HCC827-GR-step cells CVCL_S705
Experiment 14 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.20 nM Moderate EGFR expression (EGFR ++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenocarcinoma NCI-H1792 cells CVCL_1495
Experiment 15 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.26 nM Moderate EGFR expression (EGFR ++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 16 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.27 nM Moderate EGFR expression (EGFR ++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 17 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.67 nM Moderate EGFR expression (EGFR ++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 18 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.68 nM Moderate EGFR expression (EGFR ++); Moderate MET expression (MET ++);
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay. In the representative experiment, pre-treatment of NCI-H1975 cells with MET IgG RAA22.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 19 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 2.77 nM Moderate EGFR expression (EGFR ++); Moderate MET expression (MET ++);
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay. In the representative experiment, pre-treatment of NCI-H1975 cells with MET IgG B09.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 20 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 3.02 nM Moderate EGFR expression (EGFR ++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Minimally invasive lung adenocarcinoma NCI-H358 cells CVCL_1559
Experiment 21 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 3.24 nM High EGFR expression (EGFR +++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenosquamous carcinoma NCI-H596 cells CVCL_1571
Experiment 22 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 8.10 nM Low EGFR expression (EGFR ++); Moderate MET expression (MET ++)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung adenocarcinoma NCI-H23 cells CVCL_1547
Experiment 23 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 40.22 nM Moderate EGFR expression (EGFR ++); Low MET expression (MET +)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung carcinoma A-427 cells CVCL_1055
Experiment 24 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 66.67 nM Negative EGFR expression (EGFR ++); Negative MET expression (MET -)
Method Description
The in vitro potency of EGFR/CMET bispecific ADC's was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model Lung large cell carcinoma NCI-H661 cells CVCL_1577
References
Ref 1 Antibody molecules and conjugates; 2023-05-19.

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