Payload Information

General Information of This Payload
Payload ID
PAY0XPJRQ
Name
Mertansine DM1 plus IRDye700DX
Synonyms
Mertansine DM1 plus IRDye700DX
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Target(s) Microtubule (MT)
 Target Info 
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
T-DM1-IR700 [Investigative]
 ADC Info 
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 Inhibition value (TGI) ≈ 10.10% (Day 7) Negative HER2 expression (HER2 -)
Method Description
Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (without NIR light, 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
In Vivo Model MDA-MB-468GFP CDX model
In Vitro Model Breast adenocarcinoma MDA-MB-468GFP cells CVCL_DH83
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 36.40% (Day 7) Negative HER2 expression (HER2 -)
Method Description
Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (without NIR light, 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
In Vivo Model MDA-MB-468GFP CDX model
In Vitro Model Breast adenocarcinoma MDA-MB-468GFP cells CVCL_DH83
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 nM - 10 nM
Positive HER2 expression (HER2+++/++)
Method Description
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model Lung squamous cell carcinoma NCI-H2170 cells CVCL_1535
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 nM - 10 nM
Positive HER2 expression (HER2+++/++)
Method Description
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model Lung adenocarcinoma Calu-3 cells CVCL_0609
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 nM - 10 nM
Low HER2 expression (HER2+)
Method Description
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 nM - 10 nM
Positive HER2 expression (HER2+++/++)
Method Description
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.50 nM
Positive HER2 expression (HER2 +++/++)
Method Description
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model Breast adenocarcinoma 3T3/HER2-luc-GFP cells Mus musculus
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
100 nM
Negative HER2 expression (HER2 -)
Method Description
Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model Breast adenocarcinoma MDA-MB-468GFP cells CVCL_DH83
References
Ref 1 Near-infrared-induced drug release from antibody-drug double conjugates exerts a cytotoxic photo-bystander effect. Bioeng Transl Med. 2022 Aug 21;7(3):e10388. doi: 10.1002/btm2.10388. eCollection 2022 Sep.

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