PF-07284890 (ARRY-461) is an orally bioavailable, brain penetrant, potent, small molecule BRAF V600 mutants inhibitor, inhibits BRAF and CRAF with IC50 of 5.8 and 4.1 nM, respectively.PF-07284890 inhibits the clinically relevant kinase domain BRAF V600 mutants (V600E and V600K) with IC50 of 24-25 nM.PF-07284890 potently inhibits phosphorylation of ERK, a downstream marker of BRAF inhibition, and potently inhibits proliferation of BRAF V600E/K mutant melanoma cell lines (IC50=18-38 nM).PF-07284890 inhibits phosphorylation of ERK in A375 BRAF V600E tumors, achieving maximal target inhibitions at a dose of 10 mg/kg.PF-07284890 (10-30 mg/kg BID) caused significant and durable tumor regressions in the intracranial A375-luc BRAF V600E melanoma xenograft model.

Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.