PD0325901

A selective, non ATP-competitive MEK inhibitor with IC50 of 0.33 nM; markedly inhibits ERK phosphorylation and growth of both BRAF mutant and wild-type melanoma cell lines with IC50 in the nanomolar range; significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo; orally active.Brain Cancer Phase 2 Clinical (In Vitro) :Mirdametinib (PD325901; 0.0064, 0.032, 0.16, 0.8, 4, 20, 100 nM; for 2 days) inhibits the growth of Papillary thyroid carcinomas (PTC) cell lines (TPC-1 cells and K2 cells) with GC50 of 11 nM and 6.3 nM, respectively.Mirdametinib (100 nmol/L; for 4 days) induces apoptosis in K2 cells (top) or TPC-1 cells.Mirdametinib (0.1, 1, 10, 100, 1000 nM; for 1 hour) suppresses the expression of p-ERK1/2 in K2 cells (top) or TPC-1 cells.Mirdametinib prevents the growth of melanoma cell lines. Mirdametinib significantly prevents the the growth of PTC cells harboring a BRAF mutation at very low concentration (10 nM) . (In Vivo) :Mirdametinib (25 mg/kg, p.o.) inhibits phosphorylation of ERK by more than 50% at 24 hours post-dosing. Mirdametinib (25 mg/kg/day; po) produces a 70% incidence of complete tumor responses (C26 model) .Mirdametinib (20-25 mg/kg/day; oral gavage; for 3 weeks (5 consecutive days/week) ) suppresses tumor growth completely in mice inoculated with PTC cells carrying a BRAF mutation (K2) and significantly decreased tumor growth in mice inoculated with PTC cells carrying the RET/PTC1 rearrangement (TPC-1) in athymic Ncr-nu/nu mice at ages 6 to 8 weeks.

391210-10-9

PD 0325901 | PD325901 | PD-0325901

>98% (HPLC)

DMSO: ≥ 56 mg/mL

O=C (NOC[C@H] (O) CO) C1=CC=C (F) C (F) =C1NC2=CC=C (I) C=C2F

C16H14F3IN2O4

482.1931

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.