Linker Information
General Information of This Linker
| Linker ID |
LIN0IVSCI
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| Linker Name |
Mm-C6-PEG8-Val-Ala-PAB
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| Linker Type |
Unclear
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C45H75N5O16
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| Isosmiles |
COC(/C=C\C(NCCCCCC(NCCOCCOCCOCCOCCOCCOCCOCCOCCC(N[C@@H](C(C)C)C(N[C@H](C(NC1=CC=C(CO)C=C1)=O)C)=O)=O)=O)=O)=O
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| InChI |
InChI=1S/C45H75N5O16/c1-35(2)43(45(57)48-36(3)44(56)49-38-11-9-37(34-51)10-12-38)50-41(54)15-18-59-20-22-61-24-26-63-28-30-65-32-33-66-31-29-64-27-25-62-23-21-60-19-17-47-39(52)8-6-5-7-16-46-40(53)13-14-42(55)58-4/h9-14,35-36,43,51H,5-8,15-34H2,1-4H3,(H,46,53)(H,47,52)(H,48,57)(H,49,56)(H,50,54)/b14-13-/t36-,43-/m0/s1
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| InChIKey |
VSMDIOPUGPBIRL-KFGXZAQSSA-N
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| Pharmaceutical Properties |
Molecule Weight
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942.114
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Polar area
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265.87
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Complexity
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1424.418002
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xlogp Value
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0.8078
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Heavy Count
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66
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Rot Bonds
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42
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Hbond acc
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16
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Hbond Donor
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6
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Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
EP3838893B1-ADC-B [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.075 nM
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
BT-474, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.
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| In Vitro Model | Invasive breast carcinoma | BT-474 cells | CVCL_0179 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
139.901 nM
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Negative HER2 expression (HER2-) | ||
| Method Description |
MCF-7, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 | ||