General Information of This Linker
Linker ID
LIN0NUGJD
Linker Name
Open-chain glycine maleimide
Linker Type
Flexible reactive (thiol) linker
Antibody-Linker Relation
Uncleavable
Structure
Formula
C6H7NO5
Isosmiles
O=C(O)/C=C\C(=O)NCC(=O)O
InChI
InChI=1S/C6H7NO5/c8-4(1-2-5(9)10)7-3-6(11)12/h1-2H,3H2,(H,7,8)(H,9,10)(H,11,12)/b2-1-
InChIKey
JKCBZBFTTXFZGH-UPHRSURJSA-N
Pharmaceutical Properties
Molecule Weight
173.124
Polar area
103.7
Complexity
12
xlogp Value
-1.172
Heavy Count
12
Rot Bonds
4
Hbond acc
3
Hbond Donor
3
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
C4.4A-EC4 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 60.70% (Day 80) High LYPD3 expression (LYPD3+++)
Method Description
The in vivo antitumor efficacy and tolerability of the selected NAMPTi-ADCs were evaluated in the cell line-derived MDA-MB-453 human breast cancer xenograft models. Treatment with the C4.4a-EC4 (10 mg/kg,iv,Q7Dx7).
In Vivo Model Breast cancer CDX model
In Vitro Model Breast cancer Breast cancer cells Homo sapiens
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 [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.30 nM
High CD276 expression (CD276+++)
Method Description
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.

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In Vitro Model Lung adenocarcinoma A549-C4.4a cells CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
58.00 nM
High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.

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In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 uM High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.

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In Vitro Model Childhood acute monocytic leukemia THP-1 cells CVCL_0006
HER2-EC4 DAR7.8 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 88.10% (Day 80) High LYPD3 expression (LYPD3+++)
Method Description
The in vivo antitumor efficacy and tolerability of the selected NAMPTi-ADCs were evaluated in the cell line-derived MDA-MB-453 human breast cancer xenograft models. Treatment with the HER2-EC4 (10 mg/kg,iv,Q7Dx7).
In Vivo Model Breast caner CDX model
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
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 [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.30 pM
High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.

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In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
300.00 nM
High CD276 expression (CD276+++)
Method Description
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.

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In Vitro Model Lung adenocarcinoma A549-C4.4a cells CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 uM High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.

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In Vitro Model Childhood acute monocytic leukemia THP-1 cells CVCL_0006
Anti-B7H3 APDC 3f [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 90.04% (Day 30) Positive B7H3 expression (B7H3 +++/++)
Method Description
Both APDCs (10 mg/kg) have been administered to B7H3-positive U251-glioma-tumor-bearing mice; 24hours after treatment, tumors and organs were collected.
In Vivo Model U251 CDX model
In Vitro Model Astrocytoma U-251MG cells CVCL_0021
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 50) Positive B7H3 expression (B7H3 +++/++)
Method Description
In the B7H3-positive, slowly growing head and neck squamous cell carcinoma model SCC4, APDC 3 g at a dose of 10 mg/kg given 3 times in a weekly schedule which favorably compared to cisplatin and radiation therapy.
In Vivo Model SCC4 CDX model
In Vitro Model Tongue squamous cell carcinoma SCC-4 cells CVCL_1684
Anti-B7H3 APDC 3g [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.08% (Day 30) Positive B7H3 expression (B7H3 +++/++)
Method Description
Both APDCs (10 mg/kg) have been administered to B7H3-positive U251-glioma-tumor-bearing mice; 24hours after treatment, tumors and organs were collected.
In Vivo Model U251 CDX model
In Vitro Model Astrocytoma U-251MG cells CVCL_0021
B7H3-EC4 [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 [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) < 0.00 nM High CD276 expression (CD276+++)
Method Description
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.

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In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 300.00 nM High LYPD3 expression (LYPD3+++)
Method Description
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.

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In Vitro Model Lung adenocarcinoma A549-C4.4a cells CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 uM High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.

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In Vitro Model Childhood acute monocytic leukemia THP-1 cells CVCL_0006
HER2-EC4 DAR2.7 [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 [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
High CD276 expression (CD276+++)
Method Description
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.

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In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
300.00 nM
High LYPD3 expression (LYPD3+++)
Method Description
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.

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In Vitro Model Lung adenocarcinoma A549-C4.4a cells CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 uM High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description
The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.

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In Vitro Model Childhood acute monocytic leukemia THP-1 cells CVCL_0006
TWEAKR ADC 3a [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 [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Colon adenocarcinoma LoVo cells CVCL_0399
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.30 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.90 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
TWEAKR ADC 3g [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 [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.30 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Colon adenocarcinoma LoVo cells CVCL_0399
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.20 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.30 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
TWEAKR ADC 3f [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 [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.30 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Colon adenocarcinoma LoVo cells CVCL_0399
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.70 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.90 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
TWEAKR ADC 3e [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 [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.30 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Colon adenocarcinoma LoVo cells CVCL_0399
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.90 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.20 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
TWEAKR ADC 3c [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 [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.30 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Colon adenocarcinoma LoVo cells CVCL_0399
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.80 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.10 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
TWEAKR ADC 3b [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 [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.60 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.60 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Colon adenocarcinoma LoVo cells CVCL_0399
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.10 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
TWEAKR ADC 3d [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 [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
600 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Lung mucoepidermoid carcinoma NCI-H292 cells CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
600 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
600 nM
Positive TNFRSF12A expression (TNFRSF12A +++/++)
Method Description
Cytotoxicity of ADCs, SMOL KSP inhibitors, and payload metabolite were determined in TWEAKR-positive cancer cell lines 72 h after treatment with the Promega CellTiter Glo (CTG) cell viability assay according to manufacturers instructions.
In Vitro Model Colon adenocarcinoma LoVo cells CVCL_0399
References
Ref 1 A Novel NAMPT Inhibitor-Based Antibody-Drug Conjugate Payload Class for Cancer Therapy. Bioconjug Chem. 2022 Jun 15;33(6):1210-1221.
Ref 2 Antibody-Prodrug Conjugates with KSP Inhibitors and Legumain-Mediated Metabolite Formation. Chemistry. 2019 Jun 21;25(35):8208-8213. doi: 10.1002/chem.201900441. Epub 2019 Apr 15.

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