EGFR-IN-57

Names

[ CAS No. ]:
2492382-37-1

[ Name ]:
EGFR-IN-57

Biological Activity

[Description]:

EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin
Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR
Signaling Pathways >> Cell Cycle/DNA Damage >> Casein Kinase
Signaling Pathways >> Stem Cell/Wnt >> Casein Kinase

[Target]

EGFR:0.054 μM (IC50)

VEGFR-2:0.087 μM (IC50)

CK2α:0.171 μM (IC50)

topoisomerase II beta:0.13 μM (IC50)

tubulin polymerization:3.16 μM (IC50)


[References]

[1]. Warda ET, et al. New series of isoxazole derivatives targeting EGFR-TK: Synthesis, molecular modeling and antitumor evaluation. Bioorg Med Chem. 2020 Nov 1;28(21):115674.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H15N3O2S

[ Molecular Weight ]:
385.44

Related Compounds