Biaffin

Newsletter

kinases protein kinase inhibitors signaling activators kinase substrates antibodies bioluminescence assays
PD 325901, 5 mg  

PD 325901, 5 mg

N-((2R)-2,3-Dihyroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-benzamide

Synonyms: PD0325901, PD325901, PD-325901
highly potent and specific non-ATP competitive inhibitor of MEK1 /MEK2

More details

PKI-PD325-005

Availability: within 3 days

145,00 €

Background: PD0325901 is a highly potent and specific non-ATP competitive inhibitor of MEK1 /MEK2 (Ki of 1 nM). Compared to other known MEK inhibitors (such as its parent compound CI-1040/PD184352) PD0325901 has improved pharmacologic and pharmaceutical properties, higher bioavailability, increased metabolic stability and is currently in phase 1/2 clinical development. Upon treatment of human melanoma cell lines with PD0135902 suppressed ERK phosphorylation, growth inhibition as well as a proapoptotic, and antiangiogenic activity was determined. An oral administration of PD0325901 in mice inoculated with papillary thyroid carcinoma cells results in a significantly reduced tumor growth.

Chemical formula: C16H14F3IN2O4
Molecular Weight: 482.19 g/mol
Purity: ≥ 99 %
Solubility: soluble in DMSO at 12 mg/ml
CAS number: 391210-10-9

Product specific literature references:

Ciuffreda L, Del Bufalo D, Desideri M, Di Sanza C, Stoppacciaro A, Ricciardi MR, Chiaretti S, Tavolaro S, Benassi B, Bellacosa A, Foà R, Tafuri A, Cognetti F, Anichini A, Zupi G, Milella M. (2009) "Growth-inhibitory and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations." Neoplasia. 11(8):720-31.

Thompson N, Lyons J. (2005) "Recent progress in targeting the Raf/MEK/ERK pathway with inhibitors in cancer drug discovery." Curr Opin Pharmacol. 5(4):350-6.

Brown AP, Carlson TC, Loi CM, Graziano MJ. (2007) "Pharmacodynamic and toxicokinetic evaluation of the novel MEK inhibitor, PD0325901, in the rat following oral and intravenous administration." Cancer Chemother Pharmacol. 59(5):671-9.

Henderson YC, Chen Y, Frederick MJ, Lai SY, Clayman GL. (2010) "MEK inhibitor PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo.” Mol Cancer Ther.;9(7):1968-76.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.