General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0GYXZG
ADC Name
Mehozumab-DM1
Synonyms
Mehozumab-DM1
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Organization
Department of Cell Biology, National Translational Science Center for Molecular Medicine, Fourth Military Medical University.
Drug Status
Investigative
Drug-to-Antibody Ratio
5.8
Structure
Antibody Name
undisclosed
Antigen Name
Basigin (BSG)
 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 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth lnhibition value (TGl) 
87.39
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
91.11
%
Undisclosed Undisclosed
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
35.97
nM
CVCL_6832
Adult hepatocellular carcinoma
Half Maximal inhibitory Concentration (lC50) 
83.07
nM
CVCL_E3I0
Adult hepatocellular carcinoma
Half Maximal inhibitory Concentration (lC50) 
367.1
nM
CVCL_0336
Adult hepatocellular carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
87.39%
Method Description
When the tumor diameter reached 1.00 cm, qualified cynomolgus monkey liver cancer models were selected and randomly divided into an ADC intravenous injection 0.2 mg kg-1 group (n = 3), an ADC intravenous injection 1.0 mg kg-1 group (n = 3), and a physiological saline control group (n = 2). The ADC was administered once a week for 8 weeks. Tumor volumes were observed by ultrasound scans, and Figure 3C shows representative photos of ultrasound scans before and after the 8-week ADC treatment,0.2 mg/kg.

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In Vivo Model CRISPR-Mediated Cynomolgus Monkey Liver Cancer Model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl)
91.11%
Method Description
When the tumor diameter reached 1.00 cm, qualified cynomolgus monkey liver cancer models were selected and randomly divided into an ADC intravenous injection 0.2 mg kg-1 group (n = 3), an ADC intravenous injection 1.0 mg kg-1 group (n = 3), and a physiological saline control group (n = 2). The ADC was administered once a week for 8 weeks. Tumor volumes were observed by ultrasound scans, and Figure 3C shows representative photos of ultrasound scans before and after the 8-week ADC treatment,1 mg/kg.

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In Vivo Model CRISPR-Mediated Cynomolgus Monkey Liver Cancer Model
Revealed Based on the Cell Line Data
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Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 35.97 nM High CD147 expression (CD147 +++)
Method Description
Human HCC cell lines HCC-LM3, MHCC97-H, and Huh-7 were seeded in 96-well plates (3000 cells per well). After the cells had adhered to the walls, different concentration gradients of Mehozumab-DM1 diluent, Mehozumab diluent, and IgG were added, and the cells were cultured in a 37 °C incubator under 5% CO2 for 72 h. ThenCCK8 (cat#: C005; Topscience Biology) was used to determine cell viability. Per the manufacturer's instructions, 10 uL of CCK8 reagent was added to each well followed by incubation for 1 h. The absorbance was measured at 450 nm, and used to calculate the corresponding IC50 value using GraphPad Prism v8.0 software (GraphPad Software Inc., San Diego, CA).

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In Vitro Model Adult hepatocellular carcinoma HCC-LM3 cells CVCL_6832
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 83.07 nM High CD147 expression (CD147 +++)
Method Description
Human HCC cell lines HCC-LM3, MHCC97-H, and Huh-7 were seeded in 96-well plates (3000 cells per well). After the cells had adhered to the walls, different concentration gradients of Mehozumab-DM1 diluent, Mehozumab diluent, and IgG were added, and the cells were cultured in a 37 °C incubator under 5% CO2 for 72 h. ThenCCK8 (cat#: C005; Topscience Biology) was used to determine cell viability. Per the manufacturer's instructions, 10 uL of CCK8 reagent was added to each well followed by incubation for 1 h. The absorbance was measured at 450 nm, and used to calculate the corresponding IC50 value using GraphPad Prism v8.0 software (GraphPad Software Inc., San Diego, CA).

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In Vitro Model Adult hepatocellular carcinoma MHCC97-H cells CVCL_E3I0
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 367.1 nM Moderate CD147 expression (CD147++)
Method Description
Human HCC cell lines HCC-LM3, MHCC97-H, and Huh-7 were seeded in 96-well plates (3000 cells per well). After the cells had adhered to the walls, different concentration gradients of Mehozumab-DM1 diluent, Mehozumab diluent, and IgG were added, and the cells were cultured in a 37 °C incubator under 5% CO2 for 72 h. ThenCCK8 (cat#: C005; Topscience Biology) was used to determine cell viability. Per the manufacturer's instructions, 10 uL of CCK8 reagent was added to each well followed by incubation for 1 h. The absorbance was measured at 450 nm, and used to calculate the corresponding IC50 value using GraphPad Prism v8.0 software (GraphPad Software Inc., San Diego, CA).

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In Vitro Model Adult hepatocellular carcinoma Huh-7 cells CVCL_0336
References
Ref 1 An Anti-CD147 Antibody-Drug Conjugate Mehozumab-DM1 is Efficacious Against Hepatocellular Carcinoma in Cynomolgus Monkey