Linker Information
General Information of This Linker
| Linker ID |
LIN0BATVU
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| Linker Name |
P5 (OEt)-VC-PAB
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C29H39N6O7P
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| Isosmiles |
CC([C@H](NC(C1=CC=C(NP(C#C)(OCC)=O)C=C1)=O)C(N[C@@H](CCCNC(N)=O)C(NC2=CC=C(CO)C=C2)=O)=O)C
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| InChI |
InChI=1S/C29H39N6O7P/c1-5-42-43(41,6-2)35-23-15-11-21(12-16-23)26(37)34-25(19(3)4)28(39)33-24(8-7-17-31-29(30)40)27(38)32-22-13-9-20(18-36)10-14-22/h2,9-16,19,24-25,36H,5,7-8,17-18H2,1,3-4H3,(H,32,38)(H,33,39)(H,34,37)(H,35,41)(H3,30,31,40)/t24-,25-,43?/m0/s1
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| InChIKey |
BGASOHGAFJETKP-WOCPEKKISA-N
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| Pharmaceutical Properties |
Molecule Weight
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614.64
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Polar area
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200.98
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Complexity
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1285.302169
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xlogp Value
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2.7375
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Heavy Count
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43
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Rot Bonds
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16
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Hbond acc
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7
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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
37828728 ADC 1 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
251 ng/mL
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Positive HER2 expression (HER2+++/++) | ||
| Method Description |
To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | > 3000 ng/mL | Negative HER2 expression (HER2-) | ||
| Method Description |
To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).
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| In Vitro Model | Lung adenocarcinoma | HCC-78 cells | CVCL_2061 | ||
References