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AZ14133346

Chemical Structure : AZ14133346

CAS No.:

AZ14133346 (AZ 14133346, AZ-14133346)

Catalog No.: PC-22389Not For Human Use, Lab Use Only.

AZ14133346 is a potent and selective inhibitor of EGFR Ex20Ins with enzyme IC50 of <3 nM and cell IC50 of 85 nM, 14-fold selective over wild-type EGFR (cell IC50=1200 nM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

AZ14133346 is a potent and selective inhibitor of EGFR Ex20Ins with enzyme IC50 of <3 nM and cell IC50 of 85 nM, 14-fold selective over wild-type EGFR (cell IC50=1200 nM).
AZ14133346 is both a potent and efficacious inhibitor of EGFR Ex20Ins and has an improved in vivo margin to WT when compared to CLN-081.
AZ14133346 can achieve robust Ex20Ins-mediated pathway inhibition in H2073 Ex20Ins SVD (D770_N771InsSVD) xenograft models.

Physicochemical Properties

M.Wt 477.57
Formula C29H27N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S,E)-1-(3-(3-(3-(2-(5-Cyclopropyloxazol-2-yl)vinyl)phenyl)-4-(pyridin-4-yl)-1H-pyrazol-1-yl)pyrrolidin-1-yl)prop-2-en-1-one

References

1. Clare Thomson, et al. Journal of Medicinal Chemistry, May 21, 2024.

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