General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0CZVJA
ADC Name
BR112024020733A2ADC1
Synonyms
ADC1
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Organization
LIGACHEM BIOSCIENCES INC.
Drug Status
Investigative
Drug-to-Antibody Ratio
2
Structure
Antibody Name
2G10-5
 Antibody Info 
Antigen Name
Tumor-associated calcium signal transducer 2 (TACSTD2)
 Antigen Info 
Payload Name
Monomethyl auristatin E
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
BR112024020733A2 ADC1 Linker
 Linker Info 
Conjugate Type
Cysteine-maleimide conjugation
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 7 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
half-maximal cytotoxicity Concentration (CC50) 
0.582
nM
CVCL_1603
Gastric tubular adenocarcinoma
half-maximal cytotoxicity Concentration (CC50) 
1.412
nM
CVCL_1846
Pancreatic adenocarcinoma
half-maximal cytotoxicity Concentration (CC50) 
3.538
nM
CVCL_0609
Lung adenocarcinoma
half-maximal cytotoxicity Concentration (CC50) 
4.043
nM
CVCL_A8EZ
Colon cancer
half-maximal cytotoxicity Concentration (CC50) 
4.639
nM
CVCL_0186
Pancreatic ductal adenocarcinoma
half-maximal cytotoxicity Concentration (CC50) 
6.104
nM
CVCL_0419
Breast adenocarcinoma
half-maximal cytotoxicity Concentration (CC50) 
18.06
nM
CVCL_0237
Pancreatic ductal adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data half-maximal cytotoxicity Concentration (CC50) 0.582 nM High TROP2 expression (TROP2 +++)
Method Description
Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data half-maximal cytotoxicity Concentration (CC50) 1.412 nM High TROP2 expression (TROP2 +++)
Method Description
Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.

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In Vitro Model Pancreatic adenocarcinoma Patu8988s cells CVCL_1846
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data half-maximal cytotoxicity Concentration (CC50) 3.538 nM High TROP2 expression (TROP2 +++)
Method Description
Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.

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In Vitro Model Lung adenocarcinoma Calu-3 cells CVCL_0609
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data half-maximal cytotoxicity Concentration (CC50) 4.043 nM High TROP2 expression (TROP2 +++)
Method Description
Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.

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In Vitro Model Colon cancer HT29 cells CVCL_A8EZ
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data half-maximal cytotoxicity Concentration (CC50) 4.639 nM High TROP2 expression (TROP2 +++)
Method Description
Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.

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In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data half-maximal cytotoxicity Concentration (CC50) 6.104 nM High TROP2 expression (TROP2 +++)
Method Description
Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.

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In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data half-maximal cytotoxicity Concentration (CC50) 18.06 nM High TROP2 expression (TROP2 +++)
Method Description
Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.

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In Vitro Model Pancreatic ductal adenocarcinoma Capan-1 cells CVCL_0237
References
Ref 1 Conjugate antibody-drug comprising human trop2 antibody and use of the same