Linker Information
General Information of This Linker
| Linker ID |
LIN0VKJHT
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| Linker Name |
Mm-C6-PEG4-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 |
C37H59N5O12
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| Isosmiles |
COC(/C=C\C(NCCCCCC(NCCOCCOCCOCCOCCC(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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| PubChem CID | ||||||
| InChI |
InChI=1S/C37H59N5O12/c1-27(2)35(37(49)40-28(3)36(48)41-30-11-9-29(26-43)10-12-30)42-33(46)15-18-51-20-22-53-24-25-54-23-21-52-19-17-39-31(44)8-6-5-7-16-38-32(45)13-14-34(47)50-4/h9-14,27-28,35,43H,5-8,15-26H2,1-4H3,(H,38,45)(H,39,44)(H,40,49)(H,41,48)(H,42,46)/b14-13-/t28-,35-/m0/s1
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| InChIKey |
WYJXNWFRRUAKIS-TXUOPLLDSA-N
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| Pharmaceutical Properties |
Molecule Weight
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765.902
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Polar area
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228.95
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Complexity
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1229.08542
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xlogp Value
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0.7414
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Heavy Count
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54
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Rot Bonds
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30
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Hbond acc
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12
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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-A [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) |
0.069 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 0.064 to 0.075 nmol/L. 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) |
98.357 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 | ||