PD 184,352 (2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide, CI-1040)

MEK (MAPKK) inhibitor. Potent and selective MAPK (ERK kinase 1; MEK1) activation inhibitor (IC50 = 300 nM in vitro, IC50 = 2 nM in vivo). Suppresses activation of MAPK but does not block its activity. Antiproliferative. Causes cell-cycle arrest in G1 phase. Tumor suppressor. Apoptosis inducer.\n\nStorage and Stability:\nShort-term Storage: +4 degrees C\nLong-term Storage: -20 degrees C\nStable for at least 2 years after receipt when stored at -20 degrees C.

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SPECIFICATIONS

Catalog Number

045129

Size

1mg

Purity

>95% (HPLC, NMR)

References

Product Reference: \n?Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo: J.S. Sebolt-Leopold, et al.; Nat. Med. 5, 810 (1999)\n?Specificity and mechanism of action of some commonly used protein kinase inhibitors: S.P. Davies, et al.; Biochem. J. 351, 95 (2000)\n?Identification of a novel mitogen-activated protein kinase kinase activation domain recognized by the inhibitor PD 184352: A.M. Delaney, et al.; Mol. Cell. Biol. 22, 7593 (2002)\n?Cell-cycle arrest by PD184352 requires inhibition of extracellular signal-regulated kinases (ERK) 1/2 but not ERK5/BMK1: M.S. Squires, et al.; Biochem. J. 366, 673 (2002)\n?CI-1040 (PD184352), a targeted signal transduction inhibitor of MEK (MAPKK): L.F. Allen, et al.; Semin. Oncol. 30, 105 (2003) (Review)\n?The mitogen-activated protein kinase/extracellular signal-regulated kinase kinase inhibitor PD184352 (CI-1040) selectively induces apoptosis in malignant schwannoma cell lines: R.R. Mattingly, et al.; J. Pharmacol. Exp. Ther. 316, 456 (2006)\n?

Alternative Names

2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide, CI-1040