Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0GYXZG
|
|||||
|---|---|---|---|---|---|---|
| ADC Name |
Mehozumab-DM1
|
|||||
| Synonyms |
Mehozumab-DM1
Click to Show/Hide
|
|||||
| 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
| 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
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| 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.
Click to Show/Hide
|
||||
| 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.
Click to Show/Hide
|
||||
| In Vivo Model | CRISPR-Mediated Cynomolgus Monkey Liver Cancer Model | ||||
Revealed Based on the Cell Line Data
| 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).
Click to Show/Hide
|
||||
| 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).
Click to Show/Hide
|
||||
| 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).
Click to Show/Hide
|
||||
| In Vitro Model | Adult hepatocellular carcinoma | Huh-7 cells | CVCL_0336 | ||
References
