AZD0364 | ERK1/2 inhibitor | Probechem Biochemicals

Chemical Structure : AZD0364

CAS No.: 2097416-76-5

AZD0364 (Tizaterkib, AZD-0364)

Catalog No.: PC-63271Not For Human Use, Lab Use Only.

Tizaterkib (AZD0364) is a potent, selective, ATP competitive, orally active ERK1/2 inhibitor with IC50 of 0.66 nM in ERK2 biochemical assay, binds similarly to ERK1 and ERK2 with Ki of 3.9 and 3.8 nM.

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Biological Activity

Tizaterkib (AZD0364) is a potent, selective, ATP competitive, orally active ERK1/2 inhibitor with IC50 of 0.66 nM in ERK2 biochemical assay, binds similarly to ERK1 and ERK2 with Ki of 3.9 and 3.8 nM.

AZD0364 inhibits p90RSK phosphorylation with an IC50 of 5.74 nM in an A375 melanoma cell line containing a BRAFV600E mutation.

AZD0364 potently inhibits ERK1/2 phosphorylation with IC50 of 1.73 nM, which is more potent than the reported ERK1/2 competitors, SCH772984, GDC-0994, and BVD-523 (ulixertinib).

AZD0364 is highly selective for ERK1/2 in a broader panel of 353 human kinases, with activity against only nine other kinases in this panel: MEK1, COT, BRAF, MEK2, c-RAF, ERK7, CDK2, CDK5, and ARK5.

AZD0364 directly modulates RAS/MAPK pathway signaling, demonstrates in vivo antitumor activity in KRAS- and BRAF-mutant cancer cell line xenograft models.

Physicochemical Properties

M.Wt	494.507
Formula	C24H24F2N8O2
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	(6R)-7-(3,4-Difluorobenzyl)-6-(methoxymethyl)-2-{5-methyl-2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl}-6,7-dihydroimidazo[1,2-a]pyrazin-8(5H)-one

References

1. Flemington V, et al. Mol Cancer Ther. 2021 Feb;20(2):238-249.
2. Ward RA, et al. J Med Chem. 2019 Dec 26;62(24):11004-11018.

AZD0364 (Tizaterkib, AZD-0364)

Biological Activity

Physicochemical Properties

References

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