Linker Information

General Information of This Linker
Linker ID
LIN0PFRAP
Linker Name
S35 linker
Linker Type
Uncleavable linker
Antibody-Linker Relation
Uncleavable
Structure
Formula
C26H28N4O7
Isosmiles
O=C(O)CCOCCOCCN(N=N1)C(C2=CC=CC=C2N(C(CCC(O)=O)=O)C3)=C1C4=C3C=CC=C4
InChI
InChI=1S/C26H28N4O7/c31-22(9-10-23(32)33)29-17-18-5-1-2-6-19(18)25-26(20-7-3-4-8-21(20)29)30(28-27-25)12-14-37-16-15-36-13-11-24(34)35/h1-8H,9-17H2,(H,32,33)(H,34,35)
InChIKey
TYAUEYJMFBRMPA-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
508.531
Polar area
144.08
Complexity
1230.429169
xlogp Value
2.8314
Heavy Count
37
Rot Bonds
12
Hbond acc
8
Hbond Donor
2
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
39424599 ADC-S35A [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
4.25 nM
Positive FR expression (FR+++/++)
Method Description
IGROV1 (FRalpha+) and A431 (FRalpha-) cells were sub-cultured and seeded at 10,000 cells/well in complete growth medium in 96 well tissue culture plates, incubated at 37°C, 5% CO2 overnight (16 hours). Test reagents were serial diluted 1:3 in 2 mL deep-well dilution plates, starting at 200 nM (10 dilutions total). Diluted samples (100 uL) were added to the cell plates (starting concentration of test samples at 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 5 days. Medium was then discarded. The plates were washed once with 200 uL DPBS, stained with 50 uL of 0.2% Crystal Violet solution at room temperature for 15 min, and then washed extensively with tap water. Plates were air-dried, and Crystal Violet was dissolved with 200 uL of 1% SDS solution. Plates were read at 570 nm. Data was analyzed using GraphPad Prism 6.

   Click to Show/Hide
In Vitro Model Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma IGROV1 cells CVCL_1304
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 100 nM Negative FR expression (FR-)
Method Description
IGROV1 (FRalpha+) and A431 (FRalpha-) cells were sub-cultured and seeded at 10,000 cells/well in complete growth medium in 96 well tissue culture plates, incubated at 37°C, 5% CO2 overnight (16 hours). Test reagents were serial diluted 1:3 in 2 mL deep-well dilution plates, starting at 200 nM (10 dilutions total). Diluted samples (100 uL) were added to the cell plates (starting concentration of test samples at 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 5 days. Medium was then discarded. The plates were washed once with 200 uL DPBS, stained with 50 uL of 0.2% Crystal Violet solution at room temperature for 15 min, and then washed extensively with tap water. Plates were air-dried, and Crystal Violet was dissolved with 200 uL of 1% SDS solution. Plates were read at 570 nm. Data was analyzed using GraphPad Prism 6.

   Click to Show/Hide
In Vitro Model Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma IGROV1 cells CVCL_1304
References
Ref 1 A Novel Concept for Cleavable Linkers Applicable to Conjugation Chemistry - Design, Synthesis and Characterization