Ravoxertinib hydrochloride

盐酸雷沃替尼

Ravoxertinib hydrochloride

R656619-1ml

1ml

10mM in DMSO

干燥,-80℃储存

超低温冰袋运输

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 )

Ravoxertinib hydrochloride（GDC-0994 盐酸盐）是一种口服生物活性抑制剂，对 ERK 激酶活性具有选择性，对 ERK1 和 ERK2 的 IC 50 分别为 6.1 nM 和 3.1 nM。

2070009-58-2(DMSO)

C21H19Cl2FN6O2

477.32 g/mol

CN1C(=CC=N1)NC2=NC=CC(=N2)C3=CC(=O)N(C=C3)C(CO)C4=CC(=C(C=C4)Cl)F.Cl