General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0VSAIC
ADC Name
Anti-FGFR2/4 mAb-12422 SMCC-DM1
Synonyms
Anti-FGFR2/4-mAb-12422-SMCC-DM1
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Organization
Novartis AG
Drug Status
Investigative
Indication
In total 3 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Colorectal cancer [ICD11:2B91]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
Drug-to-Antibody Ratio
4
Antibody Name
Anti-FGFR2/4 mAb 12422
 Antibody Info 
Antigen Name
Fibroblast growth factor receptor 2 (FGFR2); Fibroblast growth factor receptor 4 (FGFR4)
 Antigen Info 
Payload Name
Mertansine DM1
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
 Linker Info 
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 30.85
%
CVCL_1581
Cecum adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 35.79
%
CVCL_1581
Cecum adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 80.52
%
CVCL_0076
Gastric adenocarcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
< 3
nM
CVCL_0076
Gastric adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
< 3
nM
CVCL_0371
Down syndrome
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 30.85% (Day 22) Positive FGFR2 expression (FGFR2+++/++)
Method Description
The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 5 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.

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In Vivo Model NCI-H716 CDX model
In Vitro Model Cecum adenocarcinoma NCI-H716 cells CVCL_1581
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 35.79% (Day 22) Positive FGFR2 expression (FGFR2+++/++)
Method Description
The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 15 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.

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In Vivo Model NCI-H716 CDX model
In Vitro Model Cecum adenocarcinoma NCI-H716 cells CVCL_1581
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.52% (Day 33) Positive FGFR2 expression (FGFR2+++/++)
Method Description
The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.

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In Vivo Model SNU-16 CDX model
In Vitro Model Gastric adenocarcinoma SNU-16 cells CVCL_0076
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) < 3.00 nM Positive FGFR2 expression (FGFR2+++/++)
Method Description
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.

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In Vitro Model Gastric adenocarcinoma SNU-16 cells CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) < 3.00 nM Positive FGFR2 expression (FGFR2+++/++)
Method Description
Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.

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In Vitro Model Down syndrome KATO III cells CVCL_0371
References
Ref 1 Antibody drug conjugates.

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