| Bioactivity | Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Kiapp of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts[1][2][3]. | ||||||||||||
| Invitro | 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[3]. Mirdametinib (100 nmol/L; for 4 days) induces apoptosis in K2 cells (top) or TPC-1 cells[3]. 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[3]. 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)[3]. | ||||||||||||
| Name | Mirdametinib | ||||||||||||
| CAS | 391210-10-9 | ||||||||||||
| Formula | C16H14F3IN2O4 | ||||||||||||
| Molar Mass | 482.19 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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