Linker Information
General Information of This Linker
| Linker ID |
LIN0XRRVP
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| Linker Name |
A PSar-modified branched-link agent
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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 |
C39H58N8O10
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| Isosmiles |
C[C@H](NC([C@@H](NC([C@@H](NC(CCCCCN1C(C=CC1=O)=O)=O)CCCCNC(CN(C(CN(C(C)=O)C)=O)C)=O)=O)C(C)C)=O)C(NC2=CC=C(CO)C=C2)=O
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| InChI |
InChI=1S/C39H58N8O10/c1-25(2)36(39(57)41-26(3)37(55)42-29-16-14-28(24-48)15-17-29)44-38(56)30(43-31(50)13-8-7-11-21-47-33(52)18-19-34(47)53)12-9-10-20-40-32(51)22-46(6)35(54)23-45(5)27(4)49/h14-19,25-26,30,36,48H,7-13,20-24H2,1-6H3,(H,40,51)(H,41,57)(H,42,55)(H,43,50)(H,44,56)/t26-,30-,36-/m0/s1
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| InChIKey |
YDUKUPGEZYVLOQ-UJEQNXJUSA-N
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| Pharmaceutical Properties |
Molecule Weight
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798.939
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Polar area
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243.73
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Complexity
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1543.428701
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xlogp Value
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-0.0437
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Heavy Count
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57
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Rot Bonds
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24
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Hbond acc
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10
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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
40285886 7300-LP3004 [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) |
186.6 nM
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| Method Description |
SHP-77 cells were grown in RPMI-1640 medium supplemented with 10% FBS and 1 ug/mL puromycin at 37 °C in a 5% CO2 incubator. SHP-77 cells were dissociated using TrypLETM Express Enzyme (Thermo Fisher Scientific, Waltham, MA, USA) and, after counting, the cells were resuspended in RPMI-1640 medium supplemented with 10% FBS at a density of 3 × 104 cells/mL. The cells were plated in 96-well plates and incubated at 37 °C for 24 h. ADCs and payloads were diluted separately and added to the 96-well cell culture plates containing cells, followed by incubation in a 5% CO2 incubator for 5 days. A multifunctional microplate reader was used, and the absorbance was measured at 450 nm with a reference wavelength of 630 nm. The IC50 values were calculated using GraphPad Prism 10.1.2 software.
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| In Vitro Model | Small cell lung carcinoma | SHP-77 cells | CVCL_1693 | ||
References
