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AZ5104

Chemical Structure : AZ5104

CAS No.: 1421373-98-9

AZ5104 (AZ 5104, AZ-5104)

Catalog No.: PC-63158Not For Human Use, Lab Use Only.

AZ 5104 is the active metabolite of AZD 9291 (Osimertinib), which is an irreversible inhibitor of EGFR-sensitizing and T790M resistance mutations (IC50=15-17 nM) that spares the wild-type form of the receptor (IC50=480 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AZ 5104 is the active metabolite of AZD 9291 (Osimertinib), which is an irreversible inhibitor of EGFR-sensitizing and T790M resistance mutations (IC50=15-17 nM) that spares the wild-type form of the receptor (IC50=480 nM).
AZ5104 inhibits cellular growth in Ex20Ins mutant cell lines in vitro and demonstrate sustained tumor growth inhibition of EGFR-mutant tumor xenograft harboring the most prevalent Ex20Ins in vivo.

Physicochemical Properties

M.Wt 485.592
Formula C27H31N7O2
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

N-[2-[[2-(dimethylamino)ethyl]methylamino]-5-[[4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-4-methoxyphenyl]-2-propenamide

References

1. Yates JW, et al. Mol Cancer Ther. 2016 Oct;15(10):2378-2387.

2. Hanker AB, et al. Cancer Discov. 2017 Jun;7(6):575-585.

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