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MEK protein kinase inhibitor PD 184352, 1 mg  

MEK protein kinase inhibitor PD 184352, 1 mg

2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4 Difluorobenzamide

Synonyms: CI-1040, PD184352, PD-184352, PD0184352
PD 184352 (CI-1040) is an orally active, highly specific, small-molecule inhibitor of MEK1

More details

PKI-PD184-001

Availability: within 3 days

155,00 €

Background: PD 184352 is an orally active, highly specific, small-molecule inhibitor of MEK1. It is not competitive for ATP in vitro and it exerts its inhibition via an allosteric mechanism. PD184352 can block the activation of MEK by Raf, as well as inhibiting the active (Raf phosphorylated or mutationally activated) form of the kinase with an IC50 value below 20 nM. Although no inhibition of JNK/SAPK, p38 was detected, activation of MEK5-ERK5 pathway was inhibited at micromolar concentrations.

Chemical formula: C17H14CIF2N2O2
Molecular Weight: 478.7  g/mol
Purity: 95%
Appearance: White to off-white solid
Solubility: soluble in DMSO
CAS Number: 212631-79-3

Product specific literature references:

Sebolt-Leopold JS. (2000) "Development of anticancer drugs targeting the MAP kinase pathway". Oncogene 19(56):6594-9.

Arslan MA, Kutuk O, Basaga H. (2006) "Protein kinases as drug targets in cancer". Curr Cancer Drug Targets. 6(7):623-34

Raymond R. Mattingly, Janice M. Kraniak, Joshua T. Dilworth, Patricia Mathieu, Beverly Bealmear, James E. Nowak, Joyce A. Benjamins, Michael A. Tainsky, and John J. Reiners, Jr. (2006) "The Mitogen-Activated Protein Kinase/Extracellular Signal-Regulated Kinase Kinase Inhibitor PD184352 (CI-1040) Selectively Induces Apoptosis in Malignant Schwannoma Cell Lines". J Pharmacol Exp Ther 316(1):456-65.

Kramer BW, G�tz R, Rapp UR. (2004) "Use of mitogenic cascade blockers for treatment of C-Raf induced lung adenoma in vivo: CI-1040 strongly reduces growth and improves lung structure". BMC Cancer. 1;4:24

D. Y. Mitchell, J. M. Reid, R. E. Parchment, M. B. Meyer, J. S.Leopold, R. Herrera, J. R. Piens, L. M. Bruzek, L. J. Hanson, K.Van Becelaere, T. Carlson, C. Packard, A. A. Adjei, and P. M.LoRusso. (2002) "Pharmacokinetics (PK) and pharmacodynamics (PD) of the oral MEK inhibitor, CI-1040, following multiple dose administration to patients with advanced cancer." Proc. Am. Soc. Clin. Oncol. 21:81.

Dai Y, Yu C, Singh V, Tang L, Wang Z, McInistry R, Dent P, Grant S. (2001) "Pharmacological inhibitors of the mitogen-activated protein kinase (MAPK) kinase/MAPK cascade interact synergistically with UCN-01 to induce mitochondrial dysfunction and apoptosis in human leukemia cells". Cancer Res. 61(13):5106-15.

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