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PD-184352 is an anticancer chemotherapeutic MEK1/2 and Raf inhibitor that is particularly effective against cancers harboring B-Raf or RAS mutations such as V600E. PD-184352 enhances p53 accumulation and caspase activation, increases levels of pro-apoptotic Bim protein, and decreasing levels of cyclin D1, inducing cell cycle arrest and apoptosis in several cancer cell lines. This compound also induces tumor regression in animal models carrying lung tumors.
| Cas No. | 212631-79-3 |
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| Purity | ≥98% |
| Formula | C17H14ClF2IN2O2 |
| Formula Wt. | 478.66 |
| Chemical Name | 2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluoro-benzamide |
| IUPAC Name | 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide |
| Synonym | CI-1040 |
| Solubility | Soluble in DMSO |
| Appearance | White to off white powder |
| Store Temp | Ambient |
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| Ship Temp | Ambient |
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| Info Sheet | |
| Brochures |
Wickenden JA, Jin H, Johnson M, et al. Colorectal cancer cells with the BRAF(V600E) mutation are addicted to the ERK1/2 pathway for growth factor-independent survival and repression of BIM. Oncogene. 2008 Dec 4;27(57):7150-61. PMID: 18806830.
Lunghi P, Giuliani N, Mazzera L, et al. Targeting MEK/MAPK signal transduction module potentiates ATO-induced apoptosis in multiple myeloma cells through multiple signaling pathways. Blood. 2008 Sep 15;112(6):2450-62. PMID: 18583568.
Bain J, Plater L, Elliott M, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. PMID: 17850214.
Ji H, Wang Z, Perera SA, et al. Mutations in BRAF and KRAS converge on activation of the mitogen-activated protein kinase pathway in lung cancer mouse models. Cancer Res. 2007 May 15;67(10):4933-9. PMID: 17510423.
Squires MS, Nixon PM, Cook SJ. Cell-cycle arrest by PD184352 requires inhibition of extracellular signal-regulated kinases (ERK) 1/2 but not ERK5/BMK1. Biochem J. 2002 Sep 1;366(Pt 2):673-80. PMID: 12069688.
