Linker Information

Linker Information

Prof. Feng ZHU (zhufeng@zju.edu.cn)

Prof. Xiaowu DONG (dongxw@zju.edu.cn)

Prof. Luo FANG (fangluo@zjcc.org.cn)

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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

CTX-MMAE [Investigative]

ADC Info

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 12 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 12.50% (Day 10	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 15.63% (Day 20)	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.63% (Day 20)	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 54.17% (Day 10)	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.50% (Day 20)	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 6 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 10)	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 7 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Median survival time (MST)	14 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 8 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Median survival time (MST)	23 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 9 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Median survival time (MST)	24 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 10 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Median survival time (MST)	30 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 11 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Median survival time (MST)	60 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 12 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Median survival time (MST)	61 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480

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)	39.00 pM	Positive EGFR expression (EGFR +++/++)
Method Description	MIA PaCa-2 and PANC-1 cells were seeded at 1000 and 1500 per well, respectively, in a 96-well plate and left to adhere overnight. Cells were treated with a 5-fold dilution series of CTX-MMAE or CTX ranging from 0.000256 to 500 nM for 96 h.
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.38 nM	Positive EGFR expression (EGFR +++/++)
Method Description	MIA PaCa-2 and PANC-1 cells were seeded at 1000 and 1500 per well, respectively, in a 96-well plate and left to adhere overnight. Cells were treated with a 5-fold dilution series of CTX-MMAE or CTX ranging from 0.000256 to 500 nM for 96 h.
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428

References

Ref 1	Two engineered site-specific antibody-drug conjugates, HLmD4 and HLvM4, have potent therapeutic activity in two DLL4-positive tumour xenograft models. Am J Cancer Res. 2020 Aug 1;10(8):2387-2408. eCollection 2020.

Linker Name

PD-Val-Cit-PABC

Linker Type

Flexible dual-reactive (thiol) linker

Antibody-Linker Relation