General Information of This Linker
Linker ID
LIN0PVIFI
Linker Name
T800
Antibody-Linker Relation
Cleavable
Structure
Formula
C27H37N5O6
Isosmiles
CN[C]c1cc(NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)CCCCCN2C(=O)C=CC2=O)C(C)C)ccc1CO
InChI
InChI=1S/C27H37N5O6/c1-17(2)25(31-22(34)8-6-5-7-13-32-23(35)11-12-24(32)36)27(38)29-18(3)26(37)30-21-10-9-19(16-33)20(14-21)15-28-4/h9-12,14,17-18,25,28,33H,5-8,13,16H2,1-4H3,(H,29,38)(H,30,37)(H,31,34)/t18-,25-/m0/s1
InChIKey
LWMKNYXUYFYLFC-BVZFJXPGSA-N
Pharmaceutical Properties
Molecule Weight
527.622
Polar area
156.94
Complexity
527.2743839
xlogp Value
0.85459
Heavy Count
38
Rot Bonds
15
Hbond acc
7
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
AMT-562 [Phase 1]
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 71.80% (Day 28) Low HER3 expression (HER3+)
Method Description
AMT-562 (10 mg/kg, day 1) induces efficient tumor cell killing in cell line-derived models of Pancreatic cancer cell with HER3 expression with high expression.
In Vivo Model Pancreatic cancer PDX model (PDX: PDX-200930)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 40) Low HER3 expression (HER3+)
Method Description
AMT-562 (10 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of Pancreatic cancer cell with HER3 expression with high expression.
In Vivo Model Squamous cell carcinoma PDX model (PDX: PDX-361318)
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 49) Low HER3 expression (HER3+)
Method Description
AMT-562 (10 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of Pancreatic cancer cell with HER3 expression with high expression.
In Vivo Model Pancreatic cancer PDX model (PDX: PDX-361319)
References
Ref 1 AMT-562, a novel HER3-targeting antibody drug conjugate, demonstrates a potential to broaden therapeutic opportunities for HER3-expressing tumors. Mol Cancer Ther. 2023 Jun 11:MCT-23-0198. doi: 10.1158/1535-7163.MCT-23-0198. Online ahead of print.