Linker Information
General Information of This Linker
| Linker ID |
LIN0LVHFD
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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 |
C50H84N6O17
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| Isosmiles |
COCCOCCOCCOCCOCCOCCOCCOCCC(NCCCC[C@H](NC(CCCCCNC(/C=C\C(OC)=O)=O)=O)C(NC(C(C)C)C(NC(C(NC1=CC=C(CO)C=C1)=O)C)=O)=O)=O
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| InChI |
InChI=1S/C50H84N6O17/c1-38(2)47(50(64)53-39(3)48(62)54-41-15-13-40(37-57)14-16-41)56-49(63)42(55-45(60)12-7-6-9-20-51-43(58)17-18-46(61)66-5)11-8-10-21-52-44(59)19-22-67-25-26-69-29-30-71-33-34-73-36-35-72-32-31-70-28-27-68-24-23-65-4/h13-18,38-39,42,47,57H,6-12,19-37H2,1-5H3,(H,51,58)(H,52,59)(H,53,64)(H,54,62)(H,55,60)(H,56,63)/b18-17-/t39?,42-,47?/m0/s1
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| InChIKey |
PEAZNNYNHDTJCP-LQLSIPHVSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1041.247
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Polar area
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294.97
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Complexity
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1619.544006
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xlogp Value
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1.0927
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Heavy Count
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73
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Rot Bonds
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46
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Hbond acc
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17
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Hbond Donor
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7
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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-C [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) |
0.064 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) |
30.219 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 | ||