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WSD0922

Names

[ CAS No. ]:
2226552-64-1

[ Name ]:
WSD0922

Biological Activity

[Description]:

WSD-0922 is a potent, selective, orally active, and BBB penetrable EGFR/EGFRVIII inhibitor. WSD-0922 is against EGFRm+ (EGFRvIII/Del19/L858R) with an IC50 of <10 nM. WSD0922 shows good safety profile and preclinical anti-tumor efficacy[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

IC50: EGFRm+ (EGFRvIII/Del19/L858R)[1]


[In Vivo]

WSD0922 treatment results in tumor regression on cetuximab resistant PDX model of HNSCC. WSD0922 demonstrates remarkable tumor regression in 3 PDX models (platinum sensitive/insensitive/EGFRm+). WSD0922 is well tolerated in GLP tox at dose ~10x clinical equivalent dose.[1]

[References]

[1]. Wei Zhong, et al. Abstract 1326: WSD0922: A BBB penetrable EGFR/EGFRVIII inhibitor for the treatment of GBM and metastatic CNS tumor. Experimental and Molecular Therapeutics.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H21F3N4O2

[ Molecular Weight ]:
442.43

Related Compounds