Linker Information

Linker Name

triglycyl peptide linker CX

Linker Type

Flexible reactive (amino) linker

Antibody-Linker Relation

General Information of This Linker

Each Antibody-drug Conjugate Related to This Linker

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

M9346A-CX-DM1 [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)	≈ 87.77% (Day 23)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	M9436A-CX-DM1 (200 ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of KB cells with HER2 expression with high expression.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.30% (Day 23)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	M9436A-CX-DM1 (100 ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of KB cells with HER2 expression with high expression.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

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)	0.07 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FR-Expressing KB Cells in the absence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FOLR1-Expressing KB Cells in the presence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

References

Ref 1	A Case Study Comparing Heterogeneous Lysine- and Site-Specific Cysteine-Conjugated Maytansinoid Antibody-Drug Conjugates (ADCs) Illustrates the Benefits of Lysine Conjugation. Mol Pharm. 2019 Sep 3;16(9):3926-3937. doi: 10.1021/acs.molpharmaceut.9b00529. Epub 2019 Jul 31.