General Information of This Linker
Linker ID
LIN0SXPBU
Linker Name
BG based linker
Linker Type
Bioorthogonal reaction linker
Antibody-Linker Relation
Uncleavable
Structure
Formula
C18H38O10
Isosmiles
OCCOCCOCCOCCOCCOCCOCCOCCOCCO
InChI
InChI=1S/C18H38O10/c19-1-3-21-5-7-23-9-11-25-13-15-27-17-18-28-16-14-26-12-10-24-8-6-22-4-2-20/h19-20H,1-18H2
InChIKey
YZUUTMGDONTGTN-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
414.492
Polar area
114.3
Complexity
414.2464974
xlogp Value
-0.8962
Heavy Count
28
Rot Bonds
25
Hbond acc
10
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
BDC-1001 [Phase 2 (Terminated)]
Identified from the Human Clinical Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Patients Enrolled
Patients with advanced metastatic HER2-expressing (IHC2/3+) or amplified solid tumors. Patients had received a median of 4 prior therapies.
Administration Dosage
4 dose levels (0.15-5.00 mg/kg) every 3 weeks.
Related Clinical Trial
NCT Number NCT04278144  Clinical Status Phase 1/2
Clinical Description
Phase 1/2 study of BDC-1001 as a single agent and in combination with nivolumab in patients with advanced HER2-expressing solid tumors.
1711 (scFv)-SNAP-AuriF [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 [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.52 uM
High EGFR expression (EGFR+++)
Method Description
XTT viability assay was used to assess cytotoxicity following a 72 h incubation with 1711 (scFv)-SNAP-AuriF on MDA-MB-468.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
References
Ref 1 Preliminary results from a phase 1/2 study of BDC-1001, a novel HER2 targeting TLR7/8 immune-stimulating antibody conjugate (ISAC), in patients (pts) with advanced HER2-expressing solid tumors. J Clin Oncol. 2021 39:15_suppl, 2549-2549.
Ref 2 Click Chemistry-Generated Auristatin F-Linker-Benzylguanine for a SNAP-Tag-Based Recombinant Antibody-Drug Conjugate Demonstrating Selective Cytotoxicity toward EGFR-Overexpressing Tumor Cells. ACS Omega. 2023 Jan 17;8(4):4026-4037. doi: 10.1021/acsomega.2c06844. eCollection 2023 Jan 31.