Ravoxertinib hydrochloride

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

Product information

CAS Number: 2070009-58-2

Molecular Weight: 477.32

Formula: C21H19Cl2FN6O2

Synonym:

GDC-0994 hydrochloride

Chemical Name: 1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-{2-[(1-methyl-1H-pyrazol-5-yl)amino]pyrimidin-4-yl}-1, 2-dihydropyridin-2-one hydrochloride

Smiles: Cl.CN1N=CC=C1NC1=NC(=CC=N1)C1C=CN([C@H](CO)C2=CC(F)=C(Cl)C=C2)C(=O)C=1

InChiKey: RMNVBUVHPAETTJ-GMUIIQOCSA-N

InChi: InChI=1S/C21H18ClFN6O2.ClH/c1-28-19(5-8-25-28)27-21-24-7-4-17(26-21)13-6-9-29(20(31)11-13)18(12-30)14-2-3-15(22)16(23)10-14;/h2-11,18,30H,12H2,1H3,(H,24,26,27);1H/t18-;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (209.50 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Ravoxertinib also inhibits p90RSK with IC50 of 12 nM. Ravoxertinib is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively. Ravoxertinib (GDC0994; 50 nM, 0.5 µM, and 5 µM; 48 hours) decreases the viability of lung adenocarcinoma cell lines (A549, HCC827, HCC4006).

In Vivo:

In CD-1 mice, a 10 mg/kg oral dose of Ravoxertinib is sufficient to achieve the desired target coverage for at least 8 h. Daily, oral dosing of Ravoxertinib results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice.

References:

1. Kirk Robarge, et al. Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development. Proceedings: AACR Annual Meeting 2014; April 5-9, 2014.
2. MICHAEL LAI. Opportunity for Pharmaceutical Intervention in Lung Cancer: Selective Inhibition of JAK1/2 to Eliminate EMT-Derived Mesenchymal Cells.

Products are for research use only. Not for human use.