Linker Information
General Information of This Linker
| Linker ID |
LIN0CMSRQ
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
A polyethylene glycol-modified straight-link agent
|
|||||
| Linker Type |
Cathepsin-cleavable linker
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C41H65N5O15
|
|||||
| Isosmiles |
C[C@H](NC([C@@H](NC(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(CCN1C(C=CC1=O)=O)=O)=O)C(C)C)=O)C(NC2=CC=C(CO)C=C2)=O
|
|||||
| InChI |
InChI=1S/C41H65N5O15/c1-31(2)39(41(53)43-32(3)40(52)44-34-6-4-33(30-47)5-7-34)45-36(49)11-14-54-16-18-56-20-22-58-24-26-60-28-29-61-27-25-59-23-21-57-19-17-55-15-12-42-35(48)10-13-46-37(50)8-9-38(46)51/h4-9,31-32,39,47H,10-30H2,1-3H3,(H,42,48)(H,43,53)(H,44,52)(H,45,49)/t32-,39-/m0/s1
|
|||||
| InChIKey |
YJYDWLGCCNOUSJ-GSSDHLSPSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
867.991
|
Polar area
|
247.85
|
||
|
Complexity
|
1373.587817
|
xlogp Value
|
-0.2829
|
|||
|
Heavy Count
|
61
|
Rot Bonds
|
37
|
|||
|
Hbond acc
|
15
|
Hbond Donor
|
5
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
40285886 7300-LP1003 [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) |
32.17 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.
Click to Show/Hide
|
||||
| In Vitro Model | Small cell lung carcinoma | SHP-77 cells | CVCL_1693 | ||
References
