Linker Information

General Information of This Linker
Linker ID
LIN0KBZCU
Linker Name
Mc-Phe-Lys-PABC
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
CBR96-Phe-Lys-MMAE [Investigative]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
41.21% (Day 30)
Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description
1 mg conjugate/kg/inj.
In Vivo Model Karpas 299 ALCL cell line xenograft model
In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
88.67% (Day 40)
Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description
3 mg conjugate/kg/inj.
In Vivo Model L2987 cell line xenograft model
In Vitro Model Lung adenocarcinoma L2987 cells CVCL_H586
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
91.60% (Day 40)
Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description
3 mg conjugate/kg/inj.
In Vivo Model L2987 cell line xenograft model
In Vitro Model Lung adenocarcinoma L2987 cells CVCL_H586
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 [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.00 ng/mL
Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =2,111)
Method Description
The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.

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In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
13.00 ng/mL
Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =3,500)
Method Description
The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
18.00 ng/mL
Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =755)
Method Description
The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.

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In Vitro Model Breast carcinoma H3396 cells CVCL_D348
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
80.00 ng/mL
Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =922)
Method Description
The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.

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In Vitro Model Amelanotic melanoma MDA-MB-435 cells CVCL_0417
Experiment 5 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
80.00 ng/mL
Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =600)
Method Description
The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.

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In Vitro Model Colon carcinoma RCA cells CVCL_R735
Experiment 6 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
80.00 ng/mL
Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =645)
Method Description
The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Protease-activated drug development. Theranostics. 2012;2(2):156-78.
Ref 2 An antibody-drug conjugate that targets tissue factor exhibits potent therapeutic activity against a broad range of solid tumors. Cancer Res. 2014 Feb 15;74(4):1214-26.

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