Payload Information

General Information of This Payload

Payload ID	PAY0KJLPP
Name	Maytansinoid DM1
Synonyms	Maytansinoid DM1 Click to Show/Hide
Target(s)	Microtubule (MT)	Target Info

The activity data of This Payload

Standard Type	Value	Units	Cell line	Disease Model	Cell line ID	Reference
Half Maximal Inhibitory Concentration (IC50)	0.43	nmol/L	BT-474 cells	Invasive breast carcinoma	CVCL_0179	[1]
Half Maximal Inhibitory Concentration (IC50)	9.1	nmol/L	SK-BR-3 cells	Breast adenocarcinoma	CVCL_0033	[1]
Half Maximal Inhibitory Concentration (IC50)	230.4	nM	BT-474 cells	Invasive breast carcinoma	CVCL_0179	[2]

Each Antibody-drug Conjugate Related to This Payload

Full Information of The Activity Data of The ADC(s) Related to This Payload

hu4DFabv8 (A121C)-BMPEO-DM1 [Investigative]

ADC Info

Obtained from the Model Organism Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.51% (Day 7)	High HER2 expression (HER2 +++)
Method Description	An allograft was propagated from the Fo5 mmty transgenic mouse which does not respond to.or responds poorly to HERCEPTIN therapy. Subjects were treated once with ADC (37.5 mg/kg); and placebo PBS buffer control (Vehicle) andmonitored over 3 weeks.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5

Revealed Based on the Cell Line Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 ug/mL	High HER2 expression (HER2+++)
Method Description	Exposing mammalian cells having HER2 receptors to ADC in a cell culture medium; culturing the cells for a period from about 6 hours to about 5 days; and measuring cell viability Cell-based in vitro assays were used to measure viability, cytotoxicity, and induction of apoptosis of the ADC of the invention.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

hu4DFabv8 (V110C)-BMPEO-DM1 [Investigative]

ADC Info

Obtained from the Model Organism Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.33% (Day 7)	High HER2 expression (HER2 +++)
Method Description	An allograft was propagated from the Fo5 mmty transgenic mouse which does not respond to.or responds poorly to HERCEPTIN therapy. Subjects were treated once with ADC (25 mg/kg); and placebo PBS buffer control (Vehicle) andmonitored over 3 weeks.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5

Revealed Based on the Cell Line Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 ug/mL	High HER2 expression (HER2+++)
Method Description	Exposing mammalian cells having HER2 receptors to ADC in a cell culture medium; culturing the cells for a period from about 6 hours to about 5 days; and measuring cell viability Cell-based in vitro assays were used to measure viability, cytotoxicity, and induction of apoptosis of the ADC of the invention.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Thio-Tr (A121C)-BMPEO-DM1 [Investigative]

ADC Info

Obtained from the Model Organism Data

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.69% (Day 7)	High HER2 expression (HER2 +++)
Method Description	An allograft was propagated from the Fo5 mmty transgenic mouse which does not respond to.or responds poorly to HERCEPTIN therapy. Subjects were treated once with ADC (10 mg/kg); and placebo PBS buffer control (Vehicle) andmonitored over 3 weeks.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 2 Reporting the Activity Date of This ADC				[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.92% (Day 7)	High HER2 expression (HER2 +++)
Method Description	An allograft was propagated from the Fo5 mmty transgenic mouse which does not respond to.or responds poorly to HERCEPTIN therapy. Subjects were treated once with ADC (21 mg/kg); and placebo PBS buffer control (Vehicle) andmonitored over 3 weeks.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5

References

Ref 1	Hypoxia Attenuates Trastuzumab Uptake and Trastuzumab-Emtansine (T-DM1) Cytotoxicity through Redistribution of Phosphorylated Caveolin-1. Mol Cancer Res. 2020 Apr;18(4):644-656.
Ref 2	Development of HER2-Specific Aptamer-Drug Conjugate for Breast Cancer Therapy. Int J Mol Sci. 2020 Dec 21;21(24):9764.
Ref 3	Cysteine engineered antibodies and conjugates.