General Information of This Linker
Linker ID
LIN0OXUQL
Linker Name
Mc-Val-Ala-PABC
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C25H34N4O6
Isosmiles
C[C@@H](C(=O)NC1=CC=C(C=C1)CO)NC(=O)[C@H](C(C)C)NC(=O)CCCCCN2C(=O)C=CC2=O
PubChem CID
100029273
InChI
InChI=1S/C25H34N4O6/c1-16(2)23(28-20(31)7-5-4-6-14-29-21(32)12-13-22(29)33)25(35)26-17(3)24(34)27-19-10-8-18(15-30)9-11-19/h8-13,16-17,23,30H,4-7,14-15H2,1-3H3,(H,26,35)(H,27,34)(H,28,31)/t17-,23-/m0/s1
InChIKey
DAMSURYLURICHN-SBUREZEXSA-N
IUPAC Name
6-(2,5-dioxopyrrol-1-yl)-N-[(2S)-1-[[(2S)-1-[4-(hydroxymethyl)anilino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]hexanamide
Pharmaceutical Properties
Molecule Weight
486.6
Polar area
145
Complexity
786
xlogp Value
0.9
Heavy Count
35
Rot Bonds
13
Hbond acc
6
Hbond Donor
4
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Tamrintamab pamozirine [Phase 1 (Terminated)]
Identified from the Human Clinical Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Partial Response (PR)
1.72%
Patients Enrolled
Female patients (age 18 years) with EOC if they had evidence of progressive disease during or within 6 months of receiving a platinum regimen.
Administration Dosage
1 of 6 dose levels (0.025-0.40 mg/kg) every 3 weeks (Q3W), utilizing a standard 3+3 design (dose-limiting toxicity [DLT] period: 21 days).
Related Clinical Trial
NCT Number NCT02539719  Clinical Status Phase 1
Clinical Description
A phase 1a/1b dose escalation and expansion study of SC-003 as a single-agent and in combination with ABBV-181 in subjects with platinum-resistant/ refractory ovarian cancer.
Primary Endpoint
The MTD for the Q3W schedule was 0.30 mg/kg and the SC-003 doses selected for the dose-expansion phase of the study were 0.30 mg/kg and 0.20 mg/kg.
Other Endpoint
ORR=5.17% (N=3/58), 3 patients achieved PR. All responses were observed at 0.20-0.30mg/kg. Responses were not durable, with only 1 PR confirmed on the follow-up 16-week scan.
Cetuximab- (FGX16-11) [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 42.79% (Day 36) High EGFR expression (EGFR+++)
Method Description
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 1 mg/kg.
In Vivo Model Colon cancer CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 63.01% (Day 36) High EGFR expression (EGFR+++)
Method Description
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 5 mg/kg.
In Vivo Model Colon cancer CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 92.22% (Day 36) High EGFR expression (EGFR+++)
Method Description
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 10 mg/kg.
In Vivo Model Colon cancer CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.98% (Day 36) High EGFR expression (EGFR+++)
Method Description
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 20 mg/kg.
In Vivo Model Colon cancer CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Experiment 5 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 36) High EGFR expression (EGFR+++)
Method Description
The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 40 mg/kg.
In Vivo Model Colon cancer CDX model
In Vitro Model Colon adenocarcinoma SW48 cells CVCL_1724
Anti-HER2-D265C-30.2371 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.00 pM
Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.00 pM
Positive HER2 expression (HER2 +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
71.00 pM
Moderate HER2 expression (HER2++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Anti-PSMA-D265C-30.2371 [Investigative]
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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
14.00 pM
Positive PSMA expression (PSMA +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model Prostate carcinoma LNCaP cells CVCL_0395
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
71.00 pM
Positive PSMA expression (PSMA +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model Prostate carcinoma 22RV1 cells CVCL_1045
Anti-HER2-D265C-30.1699 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
17.00 pM
Positive HER2 expression (HER2 +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
18.00 pM
Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.11 nM
Moderate HER2 expression (HER2++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Anti-PSMA-D265C-30.1699 [Investigative]
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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
22.00 pM
Positive PSMA expression (PSMA +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model Prostate carcinoma LNCaP cells CVCL_0395
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.11 nM
Positive PSMA expression (PSMA +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model Prostate carcinoma 22RV1 cells CVCL_1045
Anti-HER2-D265C-30.2115 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
25.00 pM
Positive HER2 expression (HER2 +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
54.00 pM
Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.28 nM
Moderate HER2 expression (HER2++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Anti-HER2-D265C-30.2060 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
31.00 pM
Positive HER2 expression (HER2 +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
32.00 pM
Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.21 nM
Moderate HER2 expression (HER2++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Anti-PSMA-D265C-30.2060 [Investigative]
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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
32.00 pM
Positive PSMA expression (PSMA +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model Prostate carcinoma LNCaP cells CVCL_0395
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.19 nM
Positive PSMA expression (PSMA +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model Prostate carcinoma 22RV1 cells CVCL_1045
Anti-PSMA-D265C-30.2347 [Investigative]
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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
43.00 pM
Positive PSMA expression (PSMA +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model Prostate carcinoma LNCaP cells CVCL_0395
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.16 nM
Positive PSMA expression (PSMA +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model Prostate carcinoma 22RV1 cells CVCL_1045
Anti-HER2-D265C-30.2347 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
46.00 pM
Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
59.00 pM
Positive HER2 expression (HER2 +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.13 nM
Moderate HER2 expression (HER2++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Anti-PSMA-D265C-30.2115 [Investigative]
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 [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.27 nM
Positive PSMA expression (PSMA +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model Prostate carcinoma LNCaP cells CVCL_0395
Experiment 2 Reporting the Activity Date of This ADC [3]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.36 nM
Positive PSMA expression (PSMA +++/++)
Method Description
The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model Prostate carcinoma 22RV1 cells CVCL_1045
Mil40-5 [Investigative]
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 [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
14.50 nM
High HER2 expression (HER2+++)
Method Description
SKOV-3, BT474 HerDR, MDA-MB-231 and MCF-7 cells were cultured under various concentrations of Mil40, SN-38 and ADCs for 10days, 9days, 6days, and 6days, respectively. Cytotoxicity assays were established using the CellTiter-Go assay kit (CTG).
In Vitro Model Invasive breast carcinoma BT474 HerDR cells CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
157.60 nM
High HER2 expression (HER2+++)
Method Description
SKOV-3, BT474 HerDR, MDA-MB-231 and MCF-7 cells were cultured under various concentrations of Mil40, SN-38 and ADCs for 10days, 9days, 6days, and 6days, respectively. Cytotoxicity assays were established using the CellTiter-Go assay kit (CTG).
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 1000.00 nM Negative HER2 expression (HER2-)
Method Description
SKOV-3, BT474 HerDR, MDA-MB-231 and MCF-7 cells were cultured under various concentrations of Mil40, SN-38 and ADCs for 10days, 9days, 6days, and 6days, respectively. Cytotoxicity assays were established using the CellTiter-Go assay kit (CTG).
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC [4]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 1000.00 nM Negative HER2 expression (HER2-)
Method Description
SKOV-3, BT474 HerDR, MDA-MB-231 and MCF-7 cells were cultured under various concentrations of Mil40, SN-38 and ADCs for 10days, 9days, 6days, and 6days, respectively. Cytotoxicity assays were established using the CellTiter-Go assay kit (CTG).
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
PD-L1 ADC 1 [Investigative]
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 [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
265.30 nM
High PD-L1 expression (PD-L1+++)
Method Description
The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model Lung squamous cell carcinoma SK-MES-1 cells CVCL_0630
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 663.08 nM High PD-L1 expression (PD-L1+++)
Method Description
The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model Lung squamous cell carcinoma Calu-1 cells CVCL_0608
Experiment 3 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 663.08 nM High PD-L1 expression (PD-L1+++)
Method Description
The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 663.08 nM Negative PD-L1 expression (PD-L1-)
Method Description
The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model Pancreatic ductal adenocarcinoma AsPC-1 cells CVCL_0152
PD-L1 ADC 3 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Effective Concentration (EC50)
9.75 nM
High PD-L1 expression (PD-L1+++)
Method Description
The in vitro cytotoxicity of ADC 3 was quickly evaluated in three PD-L1-positive cell lines, ie, MDA-MB-231, PC 9, and A431, and one PD-L1-negative cell line, ie, Romas.
In Vitro Model Lung adenocarcinoma PC-9 cells CVCL_B260
Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Effective Concentration (EC50)
10.33 nM
High PD-L1 expression (PD-L1+++)
Method Description
The in vitro cytotoxicity of ADC 3 was quickly evaluated in three PD-L1-positive cell lines, ie, MDA-MB-231, PC 9, and A431, and one PD-L1-negative cell line, ie, Romas.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC [5]
Efficacy Data Half Maximal Effective Concentration (EC50)
11.94 nM
High PD-L1 expression (PD-L1+++)
Method Description
The in vitro cytotoxicity of ADC 3 was quickly evaluated in three PD-L1-positive cell lines, ie, MDA-MB-231, PC 9, and A431, and one PD-L1-negative cell line, ie, Romas.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
References
Ref 1 Tamrintamab pamozirine (SC-003) in patients with platinum-resistant/refractory ovarian cancer: Findings of a phase 1 study. Gynecol Oncol. 2020 Sep;158(3):640-645.
Ref 2 DNA sequence-selective G-A cross-linking ADC payloads for use in solid tumour therapies. Commun Biol. 2022 Jul 29;5(1):741.
Ref 3 Amatoxin antibody-drug conjugates and uses thereof; 2020-10-29.
Ref 4 Synthesis and evaluation of highly releasable and structurally stable antibody-SN-38-conjugates. Drug Deliv. 2021 Dec;28(1):2603-2617.
Ref 5 Development of bifunctional anti-PD-L1 antibody MMAE conjugate with cytotoxicity and immunostimulation. Bioorg Chem. 2021 Nov;116:105366.