Linker Information

General Information of This Linker
Linker ID
LIN0YLYYC
Linker Name
NH2-PEG3-Val-Cit-PABC
Antibody-Linker Relation
Cleavable
Structure
Formula
C26H44N6O8
Isosmiles
CC(C)[C@H](NC(=O)COCCOCCOCCN)C(=O)N[C@@H](CCCNC(N)=O)C(=O)Nc1ccc(CO)cc1
InChI
InChI=1S/C26H44N6O8/c1-18(2)23(32-22(34)17-40-15-14-39-13-12-38-11-9-27)25(36)31-21(4-3-10-29-26(28)37)24(35)30-20-7-5-19(16-33)6-8-20/h5-8,18,21,23,33H,3-4,9-17,27H2,1-2H3,(H,30,35)(H,31,36)(H,32,34)(H3,28,29,37)/t21-,23-/m0/s1
InChIKey
FSVRVIFMHZBDGT-GMAHTHKFSA-N
Pharmaceutical Properties
Molecule Weight
568.672
Polar area
216.36
Complexity
568.3220624
xlogp Value
-0.8
Heavy Count
40
Rot Bonds
21
Hbond acc
9
Hbond Donor
7
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
DP-303c [Phase 3]
 ADC Info 
Identified from the Human Clinical Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Related Clinical Trial
NCT Number NCT05334810  Clinical Status Phase 2
Clinical Description
A multi-center, open-lable, single-arm phase 2 study to evaluate the efficacy and safety of DP303c in patients with HER2-positive unresectable locally advanced, relapsed, or metastatic breast cancer.
Experiment 2 Reporting the Activity Date of This ADC [2]
Related Clinical Trial
NCT Number NCT04828616  Clinical Status Phase 2
Clinical Description
An open-label, multicentre, phase 2 study of DP303c injection in patients with HER2-expressing advanced ovarian cancer.
Experiment 3 Reporting the Activity Date of This ADC [3]
Related Clinical Trial
NCT Number NCT04826107  Clinical Status Phase 2
Clinical Description
An open-label, multicentre, phase 2 study of DP303c injection in patients with unresectable locally advanced, recurrent or metastatic gastric cancer with HER2 expression.
Experiment 4 Reporting the Activity Date of This ADC [4]
Related Clinical Trial
NCT Number NCT04146610  Clinical Status Phase 1
Clinical Description
A phase 1a, multicenter, open and dose-increasing study of DP303c to evaluate the safety , pharmacokinetics, immunogenicity and antitumor activity of subjects with HER2-positive advanced solid tumors.
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 34 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 7.60% (Day 32) Moderate HER2 expression (HER2++)
Method Description
DP001 (10 mg/kg).
In Vivo Model JIMT -1 cell line xenograft model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 16.20% (Day 32) Moderate HER2 expression (HER2++)
Method Description
T-DM1 (10 mg/kg).
In Vivo Model JIMT -1 cell line xenograft model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 28.47% (Day 18) High HER2 expression (HER2+++/++)
Method Description
DP001 (10 mg/kg).
In Vivo Model SK-OV-3 cell line xenograft model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 33.60% (Day 25) High HER2 expression (HER2+++/++)
Method Description
DP001 (10 mg/kg).
In Vivo Model NCI-N87 xenograft model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 39.00% (Day 32) Moderate HER2 expression (HER2++)
Method Description
DP303c (0.3 mg/kg).
In Vivo Model JIMT -1 cell line xenograft model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 45.26% (Day 18) High HER2 expression (HER2+++/++)
Method Description
DP303c (1 mg/kg).
In Vivo Model SK-OV-3 cell line xenograft model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 54.40% (Day 32) Moderate HER2 expression (HER2++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 0.1 mg/kg.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 8 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 82.10% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 1 mg/kg.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 9 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 83.94% (Day 18) High HER2 expression (HER2+++/++)
Method Description
DP303c (3 mg/kg).
In Vivo Model SK-OV-3 cell line xenograft model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 10 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.48% (Day 21) High HER2 expression (HER2+++/++)
Method Description
DP001 (15 mg/kg).
In Vivo Model HCC1954 cell line xenograft model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 11 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 91.60% (Day 25) High HER2 expression (HER2+++/++)
Method Description
T-DM1 (10 mg/kg).
In Vivo Model NCI-N87 xenograft model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 12 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.00% (Day 25) High HER2 expression (HER2+++/++)
Method Description
DP303c (10 mg/kg).
In Vivo Model NCI-N87 xenograft model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 13 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.00% (Day 25) High HER2 expression (HER2+++/++)
Method Description
DP303c (2.5 mg/kg).
In Vivo Model NCI-N87 xenograft model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 14 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.00% (Day 25) High HER2 expression (HER2+++/++)
Method Description
DP303c (5 mg/kg).
In Vivo Model NCI-N87 xenograft model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 15 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.10% (Day 18) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 16 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.16% (Day 18) High HER2 expression (HER2+++/++)
Method Description
T-DM1 (10 mg/kg).
In Vivo Model SK-OV-3 cell line xenograft model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 17 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.30% (Day 21) High HER2 expression (HER2+++/++)
Method Description
T-DM1 (15 mg/kg).
In Vivo Model HCC1954 cell line xenograft model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 18 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.00% (Day 21) High HER2 expression (HER2+++/++)
Method Description
DP303c (10 mg/kg).
In Vivo Model HCC1954 cell line xenograft model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 19 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.00% (Day 21) High HER2 expression (HER2+++/++)
Method Description
DP303c (15 mg/kg).
In Vivo Model HCC1954 cell line xenograft model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 20 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.00% (Day 21) High HER2 expression (HER2+++/++)
Method Description
DP303c (3 mg/kg).
In Vivo Model HCC1954 cell line xenograft model
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 21 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.10% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 22 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.50% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 2.5 mg/kg.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 23 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.50% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 24 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.80% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 5 mg/kg.

   Click to Show/Hide
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 25 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.80% (Day 18) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 26 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.80% (Day 32) Moderate HER2 expression (HER2++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 1 mg/kg.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 27 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.50% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.

   Click to Show/Hide
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 28 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.54% (Day 18) High HER2 expression (HER2+++/++)
Method Description
DP303c (10 mg/kg).
In Vivo Model SK-OV-3 cell line xenograft model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 29 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 98.80% (Day 32) Moderate HER2 expression (HER2++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 30 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.10% (Day 25) High HER2 expression (HER2+++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 15 mg/kg.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 31 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.90% (Day 32) Moderate HER2 expression (HER2++)
Method Description
Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.

   Click to Show/Hide
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 32 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 32) Moderate HER2 expression (HER2++)
Method Description
DP303c (1 mg/kg).
In Vivo Model JIMT -1 cell line xenograft model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 33 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 32) Moderate HER2 expression (HER2++)
Method Description
DP303c (10 mg/kg).
In Vivo Model JIMT -1 cell line xenograft model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 34 Reporting the Activity Date of This ADC [5]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 32) Moderate HER2 expression (HER2++)
Method Description
DP303c (3 mg/kg).
In Vivo Model JIMT -1 cell line xenograft model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Revealed Based on the Cell Line Data
Click To Hide/Show 14 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.07 nM
Moderate HER2 expression (HER2++; HER2 MFI=157,231)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.07 nM
High HER2 expression (HER2+++)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 nM
High HER2 expression (HER2+++; HER2 MFI=987,353)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 nM
Negative HER2 expression (HER2-; HER2 MFI=256)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.15 nM
High HER2 expression (HER2+++)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 6 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.15 nM
High HER2 expression (HER2+++)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 7 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.22 nM
Negative HER2 expression (HER2-)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.22 nM
High HER2 expression (HER2+++)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 9 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.23 nM
High HER2 expression (HER2+++; HER2 MFI=804,573)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 10 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.23 nM
High HER2 expression (HER2+++; HER2 MFI=892,333)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 11 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.39 nM
High HER2 expression (HER2+++)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 12 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.39 nM
Moderate HER2 expression (HER2++)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 13 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 50.00 nM High HER2 expression (HER2+++; HER2 MFI=1,106,494)
Method Description
To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 14 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 1000.00 nM High HER2 expression (HER2+++; HER2 MFI=765,629)
Method Description
Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
References
Ref 1 A Multi-center, Open-lable, Single-arm Phase II Study to Evaluate the Efficacy and Safety of DP303c in Patients With HER2-positive Unresectable Locally Advanced, Relapsed, or Metastatic Breast Cancer, NCT05334810
Ref 2 An Open-label, Multicentre, Phase II Study of DP303c Injection in Patients With HER2-expressing Advanced Ovarian Cancer, NCT04828616
Ref 3 An Open-label, Multicentre, Phase II Study of DP303c Injection in Patients With Unresectable Locally Advanced, Recurrent or Metastatic Gastric Cancer With HER2 Expression, NCT04826107
Ref 4 A Phase Ia, Multicenter, Open and Dose-increasing Study of DP303c to Evaluate the Safety , Pharmacokinetics, Immunogenicity and Antitumor Activity of Subjects With HER2-Positive Advanced Solid Tumors, NCT04146610
Ref 5 An Innovative Site-Specific Anti-HER2 Antibody-Drug Conjugate with High Homogeneity and Improved Therapeutic Index. Onco Targets Ther. 2022 Apr 8;15:331-343.