PD 325901, Free Base **

产品名称：PD 325901, Free Base
产品货号：LC  P-9688
产品规格：100 MG
PD 325901 is an inhibitor of mitogen activated protein kinase kinase (MEK or MAPKK).  The potency, solubility and effectiveness of PD 325901 are greatly improved compared to PD 184352 (CI-1040).  Barrett, S.D., et al.  "The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901."  Bioorg. Med. Chem. Lett. 18:  6501-6504 (2008).
PD 325901 potently inhibited the growth of melanoma cells, with and without BRAF mutation.  It also had an antiangiogenic activity.  Ciuffreda, L., et al.  "Growth-inhibitory and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations."  Neoplasia 11:  720-731 (2009).
The sensitivity of RAS mutant cancers to MEK inhibitors depends on the activity of the phosphatidylinositol 3-kinase (PI3K) pathway.  Wee, S., et al.  "PI3K pathway activation mediates resistance to MEK inhibitors in KRAS mutant cancers."  Cancer Res. 69:  4286-4293 (2009).
The antiproliferative effect on cancer cells of PD 325901 can be determined by a sensitive imaging biomarker, 3'-deoxy-3'-[18F]fluorothymidine-positron emission tomography ([18F]FLT-PET).  Leyton, J.,  "Noninvasive imaging of cell proliferation following mitogenic extracellular kinase inhibition by PD0325901."  Mol. Cancer Ther. 7:  3112-3121 (2008).
PD 325901 potently inhibited the proliferation of thyroid cancer cells with an IC50 of 0.06-0.78 µM.  It also has synergistic inhibitory effects when combined with phosphatidylinositol 3-kinase (PI3K) or NF-κB pathway inhibitors in most thyroid cancer cell lines.  Liu, D. and Xing, M.  "Potent inhibition of thyroid cancer cells by the MEK inhibitor PD0325901 and its potentiation by suppression of the PI3K and NF-kappaB pathways."  Thyroid 18:  853-864 (2008).
Blockade of MEK/ERK signaling by PD 325901 greatly enhances the cytotoxicity induced by arsenic trioxide (ATO) through a caspase-dependent mechanism in human myeloma cell lines and in tumor cells from patients with multiple myeloma.  Lunghi, P., et al.  "Targeting MEK/MAPK signal transduction module potentiates ATO-induced apoptosis in multiple myeloma cells through multiple signaling pathways."  Blood 112:  2450-2462 (2008).
A CAS number previously in use for this compound, 870474-62-7, has been deleted by Chemical Abstracts Service.
We note that one of our competitors, Reagents Direct, as of March 28, 2011, is claiming 99.7% purity for its PD 325901, Free Base.  This claim is not credible in general chemical terms for this complex organic compound, nor in terms of the sensitivity and reproducibility of generally utilized analytical techniques.
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 12 mg/mL; soluble in ethanol at 6.3 mg/mL with slight warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 µM buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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