Linker Information
General Information of This Linker
| Linker ID |
LIN0NTKSQ
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| Linker Name |
BVP-PEG-VC-PABC
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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 |
C41H65N11O14S2
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| Isosmiles |
C=CS(N(CCN1S(=O)(C=C)=O)C[C@H]1C(NCC2=CN(N=N2)CCOCCOCCOCCOCCC(N[C@@H](C(N[C@H](CCCNC(N)=O)C(NC3=CC=C(C=C3)CO)=O)=O)C(C)C)=O)=O)(=O)=O
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| InChI |
InChI=1S/C41H65N11O14S2/c1-5-67(59,60)51-15-16-52(68(61,62)6-2)35(28-51)39(56)44-26-33-27-50(49-48-33)17-19-64-21-23-66-25-24-65-22-20-63-18-13-36(54)47-37(30(3)4)40(57)46-34(8-7-14-43-41(42)58)38(55)45-32-11-9-31(29-53)10-12-32/h5-6,9-12,27,30,34-35,37,53H,1-2,7-8,13-26,28-29H2,3-4H3,(H,44,56)(H,45,55)(H,46,57)(H,47,54)(H3,42,43,58)/t34-,35+,37-/m1/s1
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| InChIKey |
UUHZXVAWOLRFPJ-QOTGTGQHSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1000.168
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Polar area
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334.14
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Complexity
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2075.809293
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xlogp Value
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-1.5113
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Heavy Count
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68
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Rot Bonds
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33
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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
SA-7-49 [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) |
28.28 nM
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High TROP2 expression (TROP2 +++) | ||
| Method Description |
Panc 08.13, Panc 10.05, A375 and HCT116 cells were seeded in 96-well plate at a density of 5000 cells per well. After overnight adherence at 37 °C in a humidified incubator with 5 % CO2, drugs were added to the cells in a specific concentration gradient. After incubated at 37 °C, 5 % CO2 for 72h, cell viability was detected using the Cell Counting Kit-8 kit (Shandong Sparkjade Biotechnology Co., Ltd.), and the absorbance optical density (OD) values at 450 nm were read by a microplate reader (SpectraMax i3, MD, USA). The cell viability rate was calculated according to the following equation: viability % = (ODadministration - ODblank)/ (ODcontrol - ODblank) × 100 %. Olaparib and Adavosertib were purchased from MedChemExpress. KU-60019, Rabusertib, ML323, Berzosertib, RI-1 and AZD7648 were purchased from Selleck.
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| In Vitro Model | Pancreatic ductal adenocarcinoma | Panc 10.05 cells | CVCL_1639 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
31.59 nM
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High TROP2 expression (TROP2 +++) | ||
| Method Description |
Panc 08.13, Panc 10.05, A375 and HCT116 cells were seeded in 96-well plate at a density of 5000 cells per well. After overnight adherence at 37 °C in a humidified incubator with 5 % CO2, drugs were added to the cells in a specific concentration gradient. After incubated at 37 °C, 5 % CO2 for 72h, cell viability was detected using the Cell Counting Kit-8 kit (Shandong Sparkjade Biotechnology Co., Ltd.), and the absorbance optical density (OD) values at 450 nm were read by a microplate reader (SpectraMax i3, MD, USA). The cell viability rate was calculated according to the following equation: viability % = (ODadministration - ODblank)/ (ODcontrol - ODblank) × 100 %. Olaparib and Adavosertib were purchased from MedChemExpress. KU-60019, Rabusertib, ML323, Berzosertib, RI-1 and AZD7648 were purchased from Selleck.
Click to Show/Hide
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| In Vitro Model | Pancreatic ductal adenocarcinoma | Panc 08.13 cells | CVCL_1638 | ||
References