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. 2013 Feb 7;4(3):358–362. doi: 10.1021/ml4000063

Table 1. Structure, in Vitro Data, and Pharmacokinetic Data for Compound 1 in Rat, Dog, and Monkey.

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B-RafV600E IC50 (nM) pERK IC50 (nM) SKMEL28 proliferation IC50 (nM) species intrinsic Clia Clb po DNAUCc % F
3.8 23 48 rat 9 9d 1748d 85
      dog 53 38e 42e 10
      monkey 8 39e 23e 5
a

Intrinsic clearance data from liver microsomes, reported in units of milliliters per minute per gram of liver.

b

Intravenous blood clearance reported in units of milliliters per minute per kilogram.

c

Oral dose-normalized AUC (DNAUC) reported as nanograms hour per milliliter per milligram per kilogram (n = 3).

d

Dosing vehicle: 1% DMSO, 10% solutol in saline or water, at pH 5.0.

e

Dosing vehicle: 1% DMSO, 30% PEG400 in saline or water, at pH 3.5–4.5.