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Cat.No.ABP000919 Chemical NameCI-1040/CI1040,PD184352 MDL: MFCD02683961 MolFormulaC17H14ClF2IN2O2 MolWeight478.659 Purity 99%

Chemical Name : CI-1040/CI1040,PD184352

CAS : 212631-79-3

Synonyms: 4-iodophenylamino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide;PD184352

Solubility:20 mmol/L in DMSO

Storage:-20C 2 years


AZD6244 (ARRY-142886), a novel inhibitor of MEK1/2 kinases, effectively inhibited the proliferation of acute biphenotypic leukemia MV4-11 and acute monocytic leukemia MOLM13 cells. The concentrations that inhibited 50% growth were approximately 0.3 and 1.2 M, respectively, as measured by thymidine uptake on day 2 of culture. AZD6244 potently down-regulated the levels of phospho-ERK1/2 and its downstream effector, p-p70S6K, in the MV4-11 and MOLM13 cells as measured by Western blot analysis. Four BRAF mutant lines exhibited growth inhibition at low doses of the drug, with GI50 concentrations ranging from 14 to 50 nM, predominantly via a G0/G1 arrest, comparable with findings in a sensitive BRAF mutant melanoma cell line. In contrast, two BRAF wild-type lines were significantly less sensitive, with GI50 values greater than 200 nM. Nude mouse xenograft tumors derived from the BRAF mutant line ARO exhibited dosedependent growth inhibition by AZD6244, with effective treatment at 10 mg/kg by oral gavage. This effect was primarily cytostatic and associated with marked inhibition of ERK phosphorylation.


1. Blockade of MEK/ERK signaling enhances sunitinib-induced growth inhibition and apoptosis of leukemia cells possessing activating mutations of the FLT3 gene. Nishioka, C., Ikezoe, T., Yang, J., Takeshita, A., Taniguchi, A., Komatsu, N., Togitani, K., et al. 2008 Leukemia Research 32 (6), pp. 865-872

2. The mitogen-activated protein/extracellular signal-regulated kinase kinase inhibitor AZD6244 (ARRY-142886) induces growth arrest in melanoma cells and tumor regression when combined with docetaxel. Haass, N.K., Sproesser, K., Nguyen, T.K., Contractor, R., Medina, C.A., Nathanson, K.L., Herlyn, M., Smalley, K.S.M.. 2008 Clinical Cancer Research 14 (1), pp. 230-239

3. Selective growth inhibition in BRAF mutant thyroid cancer by the mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244. Ball, D.W., Jin, N., Rosen, D.M., Dackiw, A., Sidransky, D., Xing, M., Nelkin, B.D.. 2007 Journal of Clinical Endocrinology and Metabolism 92 (12), pp. 4712-4718

4. AZD6244 and doxorubicin induce growth suppression and apoptosis in mouse models of hepatocellular carcinoma. Huynh, H., Chow, P.K.H., Soo, K.-C.. 2007 Molecular Cancer Therapeutics 6 (9), pp. 2468-2476