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AZD-9291 mesylate

Chemical Structure : AZD-9291 mesylate

CAS No.: 1421373-66-1

AZD-9291 mesylate (Osimertinib mesylate, Mereletinib mesylate, AZD9291 mesylate)

Catalog No.: PC-44707Not For Human Use, Lab Use Only.

Osimertinib mesylate (AZD-9291) is a potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively. Osimertinib shows weak activity against wt EGFR (IC50=184 nM).

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Biological Activity

Osimertinib mesylate (AZD-9291) is a potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively.
Osimertinib shows weak activity against wt EGFR (IC50=184 nM).
Osimertinib inhibits signaling pathways and cellular growth in both EGFRm(+) and EGFRm(+)/T790M(+) mutant cell lines in vitro.
Osimertinib exhibits tumor regression in EGFR-mutant tumor xenograft and transgenic models; orally active.

Physicochemical Properties

M.Wt 595.713
Formula C29H37N7O5S
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

DMSO

Chemical Name/SMILES

2-Propenamide, N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-, methanesulfonate (1:1)

References

1. Finlay MR, et al. J Med Chem. 2014 Oct 23;57(20):8249-67.

2. Cross DA, et al. Cancer Discov. 2014 Sep;4(9):1046-61.

3. Eberlein CA, et al. Cancer Res. 2015 Jun 15;75(12):2489-500.

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