Ravoxertinib hydrochloride - 10mM in DMSO , CAS No.2070009-58-2

CAS: 2070009-58-2 Cat. No.: R656619 Peso molecular: 477.32 PubChem CID: 92044395

GRADE & PURITY 10mM in DMSO

Storage

Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for ERK kinase activity with IC 50 of 6.1 nM and 3.1 nM for ERK1 and ERK2 , respectively.

In Vitro

Ravoxertinib also inhibits p90RSK with IC 50 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:ERK2 3.1 nM (IC 50 ) ERK1 6.1 nM (IC 50 ) p-RSK 12 nM (IC 50 )

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for ERK kinase activity with IC 50 of 6.1 nM and 3.1 nM for ERK1 and ERK2 , respectively.

Condiciones de almacenamiento de almacenamiento

Desiccated, Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Nombres e identificadores

• Isómeros SMILES: CN1C(=CC=N1)NC2=NC=CC(=N2)C3=CC(=O)N(C=C3)[C@H](CO)C4=CC(=C(C=C4)Cl)F.Cl
• PubChem CID: 92044395
• Peso molecular: 477.32