Linker Information

General Information of This Linker
Linker ID
LIN0AAPCY
Linker Name
Stable cleavable peptide linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C21H32N4O9S
Isosmiles
C[C@H](NC(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)CCCSC1CC(=O)N(CCCC(=O)O)C1=O)C(=O)O
InChI
InChI=1S/C21H32N4O9S/c1-11(18(30)23-12(2)19(31)24-13(3)21(33)34)22-15(26)6-5-9-35-14-10-16(27)25(20(14)32)8-4-7-17(28)29/h11-14H,4-10H2,1-3H3,(H,22,26)(H,23,30)(H,24,31)(H,28,29)(H,33,34)/t11-,12+,13-,14?/m0/s1
InChIKey
USLOMACHKOSHSN-WJLOJVBCSA-N
Pharmaceutical Properties
Molecule Weight
516.573
Polar area
199.28
Complexity
516.1889996
xlogp Value
-0.9092
Heavy Count
35
Rot Bonds
15
Hbond acc
8
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
IMGN151 [Phase 1]
 ADC Info 
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
100.00%
High FOLR1 expression (FOLR1+++; IHC H-score=300)
Method Description
IMGN151 activity was characterized against cell lines and xenograft models with a wide range of FR expression and compared to IMGN853.
In Vivo Model KB CDX model
In Vitro Model Human papillomavirus-related endocervical adenocarcinoma KB cells CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
100.00%
Moderate FOLR1 expression (FOLR1++; IHC H-score=140)
Method Description
IMGN151 activity was characterized against cell lines and xenograft models with a wide range of FR expression and compared to IMGN853.
In Vivo Model IGROV-1 CDX model
In Vitro Model Ovarian endometrioid adenocarcinoma IGROV-1 cells CVCL_1304
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
100.00%
Moderate FOLR1 expression (FOLR1++; IHC H-score=100)
Method Description
IMGN151 activity was characterized against cell lines and xenograft models with a wide range of FR expression and compared to IMGN853.
In Vivo Model Ishikawa CDX model
In Vitro Model Endometrial adenocarcinoma Ishikawa cells CVCL_2529
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI)
100.00%
Low FOLR1 expression (FOLR1+; IHC H-score=30)
Method Description
IMGN151 activity was characterized against cell lines and xenograft models with a wide range of FR expression and compared to IMGN853.
In Vivo Model OV-90 CDX model
In Vitro Model Ovarian adenocarcinoma OV-90 cells CVCL_3768
References
Ref 1 IMGN151-A next generation folate receptor alpha targeting antibody drug conjugate active against tumors with low, medium and high receptor expression. Cancer Res (2020) 80 (16_Supplement): 2890.