General Information of This Linker
Linker ID
LIN0IBFYU
Linker Name
MDpr-PEG (12)gluc
Linker Type
Unclear
Antibody-Linker Relation
Cleavable
Structure
Formula
C33H46N6O15
Isosmiles
O[C@@H]([C@H](O)[C@@H](O)[C@H](OC1=CC=C(C=C1NC(CCNC([C@@H](NC([C@@H](N2C(C=CC2=O)=O)CN)=O)CCCCNC(CCOC)=O)=O)=O)CO)O3)[C@H]3C(O)=O
InChI
InChI=1S/C33H46N6O15/c1-52-13-10-22(41)35-11-3-2-4-18(38-31(49)20(15-34)39-24(43)7-8-25(39)44)30(48)36-12-9-23(42)37-19-14-17(16-40)5-6-21(19)53-33-28(47)26(45)27(46)29(54-33)32(50)51/h5-8,14,18,20,26-29,33,40,45-47H,2-4,9-13,15-16,34H2,1H3,(H,35,41)(H,36,48)(H,37,42)(H,38,49)(H,50,51)/t18-,20-,26-,27-,28+,29-,33+/m0/s1
InChIKey
YIMBHRSOVQKEJO-FSHDZEOVSA-N
Pharmaceutical Properties
Molecule Weight
766.758
Polar area
325.71
Complexity
1469.354991
xlogp Value
-4.0452
Heavy Count
54
Rot Bonds
21
Hbond acc
15
Hbond Donor
10
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
hL49-HALC-MDpr-PEG (12)-gluc-MMAE [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC65)
14.9 nM
Method Description
Tumor cells (A375) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Amelanotic melanoma A375 cells CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC64)
7.3 nM
Moderate MELTF expression (MELTF++)
Method Description
Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Melanoma A2058 cells CVCL_1059
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC64)
13.7 nM
Method Description
Tumor cells (IGR37) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Melanoma IGR37 cells CVCL_2075
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC58)
3.7 nM
Method Description
Tumor cells (Colo853) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma Colo853 cells CVCL_2003
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC51)
2.5 nM
Method Description
Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
2.8 nM
Method Description
Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
cL49-MDpr-PEG (12)-gluc-MMAE [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
2 nM
Method Description
Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
2 nM
Method Description
Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
2 nM
Method Description
Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
5 nM
Moderate MELTF expression (MELTF++)
Method Description
Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Melanoma A2058 cells CVCL_1059
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
Biolegend (#363101)-MDpr-PEG (12)-gluc-MMAE [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
2 nM
Method Description
Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
7 nM
Method Description
Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
100 nM
Method Description
Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
718 nM
Moderate MELTF expression (MELTF++)
Method Description
Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Melanoma A2058 cells CVCL_1059
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
mL49-MDpr-PEG (12)gluc-MMAE [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
3 nM
Method Description
Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
3 nM
Method Description
Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
5 nM
Method Description
Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
12 nM
Moderate MELTF expression (MELTF++)
Method Description
Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Melanoma A2058 cells CVCL_1059
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
R&D (#893416)-MDpr-PEG (12)-gluc-MMAE [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
4 nM
Method Description
Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
6 nM
Method Description
Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
55 nM
Method Description
Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
444 nM
Moderate MELTF expression (MELTF++)
Method Description
Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Melanoma A2058 cells CVCL_1059
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
mL235-MDpr-PEG (12)-gluc-MMAE [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
17 nM
Method Description
Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
114 nM
Method Description
Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
305 nM
Method Description
Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
780 nM
Moderate MELTF expression (MELTF++)
Method Description
Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Melanoma A2058 cells CVCL_1059
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
Santa Cruz (#271633)-MDpr-PEG (12)gluc-MMAE [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM Moderate MELTF expression (MELTF++)
Method Description
Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Melanoma A2058 cells CVCL_1059
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
hIgG-MDpr-PEG (12)-gluc-MMAE [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM Moderate MELTF expression (MELTF++)
Method Description
Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Melanoma A2058 cells CVCL_1059
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Malignant melanoma RPMI-7951 cells CVCL_1666
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 1000 nM
Method Description
Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model Cutaneous melanoma SK-MEL-5 cells CVCL_0527
References
Ref 1 Anti-CD228 antibodies and antibody-drug conjugates