Table 2. Truncated Tail SAR.

^aB-Raf^V600E enzymatic activity. Values are means of at least two experiments; individual values are within 2-fold of the reported mean value.

^bInhibition of pERK in SKMEL28 cells. Values are means of at least two experiments; individual values are within 2-fold of the reported mean value.

^cInhibition of SKMEL28 cell proliferation. IC₅₀ values are means of at least experiments; individual values are within 3-fold of the reported mean value.

^dIntravenous clearance reported in units of milliliters per minute per kilogram. Oral dose-normalized AUC (DNAUC) reported as nanograms hours per milliliter per milligram per kilogram (n = 3).

^eData from four-compound cassette dosing. Pharmacokinetic values based on cassette dosing were found to be within 2-fold of those of discretely dosed experiments.

^fNot tested.

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

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