General Information of This Linker
Linker ID
LIN0XRRVP
Linker Name
A PSar-modified branched-link agent
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C39H58N8O10
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
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
InChIKey
YDUKUPGEZYVLOQ-UJEQNXJUSA-N
Pharmaceutical Properties
Molecule Weight
798.939
Polar area
243.73
Complexity
1543.428701
xlogp Value
-0.0437
Heavy Count
57
Rot Bonds
24
Hbond acc
10
Hbond Donor
6
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
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
186.6 nM
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
Ref 1 Design, Synthesis, and Evaluation of Camptothecin-Based Antibody-Drug Conjugates with High Hydrophilicity and Structural Stability