Linker Information
General Information of This Linker
| Linker ID |
LIN0VGFLP
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| Linker Name |
Fmoc-Val-Cit-PAB-PNP
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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 |
C38H59N11O13S2
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| Isosmiles |
CC([C@H](NC(COCCOCCOCCN(N=N1)C=C1CNC([C@@H]2CN(S(C=C)(=O)=O)CCN2S(C=C)(=O)=O)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC3=CC=C(C=C3)CO)=O)=O)C
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| InChI |
InChI=1S/C38H59N11O13S2/c1-5-63(56,57)48-14-15-49(64(58,59)6-2)32(24-48)36(53)41-22-30-23-47(46-45-30)16-17-60-18-19-61-20-21-62-26-33(51)44-34(27(3)4)37(54)43-31(8-7-13-40-38(39)55)35(52)42-29-11-9-28(25-50)10-12-29/h5-6,9-12,23,27,31-32,34,50H,1-2,7-8,13-22,24-26H2,3-4H3,(H,41,53)(H,42,52)(H,43,54)(H,44,51)(H3,39,40,55)/t31-,32-,34-/m0/s1
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| InChIKey |
VXDSPVWUSAQOCY-HSRBSRBISA-N
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| Pharmaceutical Properties |
Molecule Weight
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942.088
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Polar area
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324.91
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Complexity
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2006.447147
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xlogp Value
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-1.918
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Heavy Count
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64
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Rot Bonds
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29
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Hbond acc
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16
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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
37235999 ADC 401-4 [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) |
13.18 nM
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High B7-H3 expression (B7-H3 +++) | ||
| Method Description |
Cancer cell lines U87, U251, U87/B7-H3 KO cells (3000 cells per well) at logarithmic growth stage were seeded in 96-well plates and allowed to adhere overnight at 37 °C in a humidified incubator of 5% CO2. After that, ADCs, 401 and MMAE were diluted at a certain concentration gradient and added to cell plates in triplicate, the cells were treated at 37 °C with 5% CO2 for 72 h. In addition, the complete medium without cells served as the blank and the cells cultured in medium alone served as vehicle control.
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| In Vitro Model | Glioblastoma | U87 cells | CVCL_0022 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
35.48 nM
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High B7-H3 expression (B7-H3 +++) | ||
| Method Description |
Cancer cell lines U87, U251, U87/B7-H3 KO cells (3000 cells per well) at logarithmic growth stage were seeded in 96-well plates and allowed to adhere overnight at 37 °C in a humidified incubator of 5% CO2. After that, ADCs, 401 and MMAE were diluted at a certain concentration gradient and added to cell plates in triplicate, the cells were treated at 37 °C with 5% CO2 for 72 h. In addition, the complete medium without cells served as the blank and the cells cultured in medium alone served as vehicle control.
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| In Vitro Model | Astrocytoma | U251 cells | CVCL_0021 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
239.88 nM
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High B7-H3 expression (B7-H3 +++) | ||
| Method Description |
Cancer cell lines U87, U251, U87/B7-H3 KO cells (3000 cells per well) at logarithmic growth stage were seeded in 96-well plates and allowed to adhere overnight at 37 °C in a humidified incubator of 5% CO2. After that, ADCs, 401 and MMAE were diluted at a certain concentration gradient and added to cell plates in triplicate, the cells were treated at 37 °C with 5% CO2 for 72 h. In addition, the complete medium without cells served as the blank and the cells cultured in medium alone served as vehicle control.
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| In Vitro Model | Glioblastoma | U87 cells (B7-H3 KO) | CVCL_0022 | ||
References