Antiproliferative agent-34

Antiproliferative agent-34 (Compound A14) is a multi-target kinase inhibitor, with an IC50 of 177 nM and 1567 nM for EGFR L858R/T790M and EGFR WT. Antiproliferative agent-34 also inhibits JAK2, ROS1, FLT3, FLT4, PDGFRα with IC50 of 30.93, 106.90, 108.00, 226.60, 42.53 nM. Antiproliferative agent-34 inhibits H1975 and HCC827 cells proliferation with IC50 values below 40 nM under normoxic condition, and the anti-proliferation potency achieves 4–6-fold improvement (IC50 values [1].

Product Specifications

CAS Number

[2910858-34-1]

UNSPSC

12352005

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/antiproliferative-agent-34.html

Solubility

10 mM in DMSO

Smiles

CN(C1=C2C=CC=C1)C=C2C3=NC(NC4=CC(OCCOCCN5C=CN=C5[N+]([O-])=O)=C(OC)C=C4)=NC=C3

Molecular Formula

C27H27N7O5

Molecular Weight

529.55

References & Citations

[1]Jia T, et al. Discovery of novel hypoxia-activated, nitroimidazole constructed multi-target kinase inhibitors on the basis of AZD9291 for the treatment of human lung cancer. Bioorg Med Chem. 2023 Aug 15;91:117384.