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Ravoxertinib

Chemical Structure : Ravoxertinib

CAS No.: 1453848-26-4

Ravoxertinib (GDC-0994, GDC0994)

Catalog No.: PC-22330Not For Human Use, Lab Use Only.

Ravoxertinib (GDC-0994) is potent, selective and orally active ERK kinase inhibitor with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.

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

Biological Activity

Ravoxertinib (GDC-0994) is potent, selective and orally active ERK kinase inhibitor with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
Ravoxertinib (GDC-0994) displays at least 50-fold selectivity against the Invitrogen Selectscreen panel containing 279 kinases.
Ravoxertinib (GDC-0994) potently inhibits ERK dependent p90RSK serine 380 phosphorylation in PMA-stimulated HepG2 cells with IC50 of 12 nM.
Ravoxertinib (GDC-0994) decreases the viability of lung adenocarcinoma cell lines (A549, HCC827, HCC4006).
Ravoxertinib (GDC-0994) (15, 30, or 100 mg/kg, PO, QD) inhibits tumor growth in the HCT116 mouse xenograft model.

Physicochemical Properties

M.Wt 440.86
Formula C21H18ClFN6O2
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)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one

References

1. Blake JF, et al. J Med Chem. 2016 Jun 23;59(12):5650-60.

2. Varga A, Soria JC, et al. Clin Cancer Res. 2020 Mar 15;26(6):1229-1236.

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