Payload Information
General Information of This Payload
| Payload ID | PAY0FJMEW |
|||||
|---|---|---|---|---|---|---|
| Name | NAMPT inhibitor 5 |
|||||
| Synonyms |
NAMPT inhibitor 5
Click to Show/Hide
|
|||||
| Target(s) | Nicotinamide phosphoribosyltransferase (NAMPT) | |||||
| Structure |
|
|||||
| Formula | C24H30N6O2 |
|||||
| Isosmiles | CC1CC(=O)N(CCCCCN)N=C1c1ccc(NC(=O)N2Cc3ccncc3C2)cc1 |
|||||
| InChI |
InChI=1S/C24H30N6O2/c1-17-13-22(31)30(12-4-2-3-10-25)28-23(17)18-5-7-21(8-6-18)27-24(32)29-15-19-9-11-26-14-20(19)16-29/h5-9,11,14,17H,2-4,10,12-13,15-16,25H2,1H3,(H,27,32)
|
|||||
| InChIKey |
UGLKHXHKWSTIFS-UHFFFAOYSA-N
|
|||||
| Pharmaceutical Properties | Molecule Weight |
434.544 |
Polar area |
103.92 |
||
Complexity |
32 |
xlogp Value |
3.3308 |
|||
Heavy Count |
32 |
Rot Bonds |
7 |
|||
Hbond acc |
5 |
Hbond Donor |
2 |
|||
The activity data of This Payload
| Standard Type | Value | Units | Cell line | Disease Model | Cell line ID | Reference |
|---|---|---|---|---|---|---|
| Half Maximal Inhibitory Concentration (IC50) | 0.023 | nM |
THP-1 cells
|
Childhood acute monocytic leukemia
|
[1] | |
| Half Maximal Inhibitory Concentration (IC50) | <0.03 | nM |
MDA-MB-453 cells
|
Breast adenocarcinoma
|
[1] | |
| Half Maximal Inhibitory Concentration (IC50) | 97 | nM |
A549-C4.4a cells
|
Lung adenocarcinoma
|
[1] |
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
C4.4A-EC4 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| 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
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Lung adenocarcinoma | A549-C4.4a cells | CVCL_0023 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [2] | ||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Childhood acute monocytic leukemia | THP-1 cells | CVCL_0006 | ||
HER2-EC4 DAR7.8 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| 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
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Lung adenocarcinoma | A549-C4.4a cells | CVCL_0023 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [2] | ||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Childhood acute monocytic leukemia | THP-1 cells | CVCL_0006 | ||
B7H3-EC4 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Lung adenocarcinoma | A549-C4.4a cells | CVCL_0023 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [2] | ||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Childhood acute monocytic leukemia | THP-1 cells | CVCL_0006 | ||
HER2-EC4 DAR2.7 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Lung adenocarcinoma | A549-C4.4a cells | CVCL_0023 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [2] | ||||
| 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.
Click to Show/Hide
|
||||
| In Vitro Model | Childhood acute monocytic leukemia | THP-1 cells | CVCL_0006 | ||
References
If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.