Payload Information

General Information of This Payload

Payload ID	PAY0FUTGK
Name	ADC-C3 Payload
Synonyms	ADC-C3 Payload Click to Show/Hide
Structure
Structure	3D MOL		2D MOL
Formula	C29H30FN3O6S2
Isosmiles	CC[C@@](C(C=C1C2=NC3=C4C([C@@H](NC(C(C)(C)CO)=O)CCC4=C(C)C(F)=C3)=C2CN51)=C(C5=O)CO6)(O)C6=O.[S].[S]
InChI	InChI=1S/C29H30FN3O6.2S/c1-5-29(38)17-8-21-24-15(10-33(21)25(35)16(17)11-39-27(29)37)23-19(32-26(36)28(3,4)12-34)7-6-14-13(2)18(30)9-20(31-24)22(14)23;;/h8-9,19,34,38H,5-7,10-12H2,1-4H3,(H,32,36);;/t19-,29-;;/m0../s1
InChIKey	GIAYJYNDOVJSIW-PJKQHZEASA-N
Pharmaceutical Properties	Molecule Weight	599.706	Polar area	130.75
	Complexity	1631.464712	xlogp Value	3.94552
	Heavy Count	41	Rot Bonds	4
	Hbond acc	8	Hbond Donor	3

Each Antibody-drug Conjugate Related to This Payload

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

BGA9962 [Investigative]

ADC Info

Discovered Using Patient-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 lnhibition value (TGl)	106%	Positive CEA expression (CEA+++/++)
Method Description	Human patient-derived gastric tumors were induced on the right flank by a subcutaneous injection. When tumor volume reached approximately 200 mm3 in size, mice were randomized into 5 groups with 8, 9, and 9 animals in vehicle, BGA7650, and BGA9962 groups on Day 0, respectively. After ensuring all cohorts hadapproximately equal average tumor volumes to start, animals were intravenously administered vehicle, BGA9962 (2 mg/kg) on treatment Day 1. Animal body weight and tumor volume were measured twice weekly. Click to Show/Hide
In Vivo Model	Human patient-derived gastric xenograft model
Experiment 2 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth lnhibition value (TGl)	107%	Positive CEA expression (CEA+++/++)
Method Description	Human patient-derived gastric tumors were induced on the right flank by a subcutaneous injection. When tumor volume reached approximately 200 mm3 in size, mice were randomized into 5 groups with 8, 9, and 9 animals in vehicle, BGA7650, and BGA9962 groups on Day 0, respectively. After ensuring all cohorts hadapproximately equal average tumor volumes to start, animals were intravenously administered vehicle, BGA9962 (6 mg/kg) on treatment Day 1. Animal body weight and tumor volume were measured twice weekly. Click to Show/Hide
In Vivo Model	Human patient-derived gastric xenograft model

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.17 nM	Positive CEA expression (CEA+++/++)
Method Description	NCI-H2122 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Lung adenocarcinoma	NCI-H2122 cells		CVCL_1531
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.39 nM	Positive CEA expression (CEA+++/++)
Method Description	MKN45 cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.83 nM	Positive CEA expression (CEA+++/++)
Method Description	Ls147T cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Colon adenocarcinoma	Ls147T cells		CVCL_1384
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	27 nM	Negative CEA expression (CEA-)
Method Description	MDA-MB-231 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

WO2024110905A1 ADC-C3 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.008 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	H1048 cells		CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.018 nM	High B7H3 expression (B7H3 +++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.291 nM	Positive B7H3 expression (B7H3+++/++)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Lung papillary adenocarcinoma	H441 cells		CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Negative B7H3 expression (B7H3-)
Method Description	Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

BGA8357 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.14 nM	Positive CEA expression (CEA+++/++)
Method Description	NCI-H2122 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Lung adenocarcinoma	NCI-H2122 cells		CVCL_1531
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.38 nM	Positive CEA expression (CEA+++/++)
Method Description	MKN45 cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.67 nM	Positive CEA expression (CEA+++/++)
Method Description	Ls147T cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Colon adenocarcinoma	Ls147T cells		CVCL_1384
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	26 nM	Negative CEA expression (CEA-)
Method Description	MDA-MB-231 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

BGA7413 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.16 nM	Positive CEA expression (CEA+++/++)
Method Description	NCI-H2122 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Lung adenocarcinoma	NCI-H2122 cells		CVCL_1531
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.46 nM	Positive CEA expression (CEA+++/++)
Method Description	MKN45 cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.88 nM	Positive CEA expression (CEA+++/++)
Method Description	Ls147T cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Colon adenocarcinoma	Ls147T cells		CVCL_1384
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	28 nM	Negative CEA expression (CEA-)
Method Description	MDA-MB-231 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

BGA0179 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.16 nM	Positive CEA expression (CEA+++/++)
Method Description	NCI-H2122 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Lung adenocarcinoma	NCI-H2122 cells		CVCL_1531
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.3 nM	Positive CEA expression (CEA+++/++)
Method Description	MKN45 cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.62 nM	Positive CEA expression (CEA+++/++)
Method Description	Ls147T cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Colon adenocarcinoma	Ls147T cells		CVCL_1384
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	24 nM	Negative CEA expression (CEA-)
Method Description	MDA-MB-231 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

BGA2490 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.19 nM	Positive CEA expression (CEA+++/++)
Method Description	NCI-H2122 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Lung adenocarcinoma	NCI-H2122 cells		CVCL_1531
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.44 nM	Positive CEA expression (CEA+++/++)
Method Description	MKN45 cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.76 nM	Positive CEA expression (CEA+++/++)
Method Description	Ls147T cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Colon adenocarcinoma	Ls147T cells		CVCL_1384
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	21 nM	Negative CEA expression (CEA-)
Method Description	MDA-MB-231 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

References

Ref 1	Anti-CEA antibody drug conjugates and methods of use
Ref 2	Antibody drug conjugates

Payload Information

Citation

Visitor Map

Correspondence

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

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

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