PD0325901

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种选择性、非 ATP 竞争性 MEK 抑制剂，IC50 为 0.33 nM。

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.

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PD 0325901 | PD325901 | PD-0325901

MAPK/ERK Signaling

MEK

MEK

Cancer

Brain Cancer

391210-10-9

482.1931

C16H14F3IN2O4

>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

Benzamide, N-[(2R)-2,3-dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-

(-20℃)

With Ice Pack

≥ 2 years