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Submit ReviewPD 184352 is a selective MEK inhibitor (Ki = 300 nM in vitro). Suppresses FGF-mediated angiogenesis in vivo and decreases VEGF expression. Enhances the therapeutic efficacy of taxol (Cat. No. 1097) in vivo. Orally active.
Sold for research purposes under agreement from Pfizer Inc.
M. Wt | 478.66 |
Formula | C17H14ClF2IN2O2 |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 212631-79-3 |
PubChem ID | 6918454 |
InChI Key | GFMMXOIFOQCCGU-UHFFFAOYSA-N |
Smiles | FC1=C(NC2=CC=C(I)C=C2Cl)C(C(NOCC3CC3)=O)=CC=C1F |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 47.87 | 100 | |
ethanol | 11.97 | 25 |
The following data is based on the product molecular weight 478.66. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.09 mL | 10.45 mL | 20.89 mL |
5 mM | 0.42 mL | 2.09 mL | 4.18 mL |
10 mM | 0.21 mL | 1.04 mL | 2.09 mL |
50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
References are publications that support the biological activity of the product.
Allen et al (2003) CI-1040 (PD184252), a targeted signal transduction inhibitor of MEK (MAPKK). Semin.Oncol. 30 105 PMID: 14613031
McDaid et al (2005) Enhancement of the therapeutic efficacy of Tax. by the mitogen-activated protein kinase kinase inhibitor CI-1040 in nude mice bearing human heterotransplants. Cancer Res. 65 2854 PMID: 15805287
Solit et al (2006) BRAF mutation predicts sensitivity to MEK inhibition. Nature 439 358 PMID: 16273091
If you know of a relevant reference for PD 184352, please let us know.
Keywords: PD 184352, PD 184352 supplier, pfizer, mek1, mek2, mkk1, mkk2, inhibitors, inhibits, selective, mapk, signaling, signalling, map, kinases, PD184352, CI1040, CI-1040, MEK, 4237, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for PD 184352 include:
W Michael et al (2013) Subtype-specific MEK-PI3 kinase feedback as a therapeutic target in pancreatic adenocarcinoma. Mol Cancer Ther 12 2213-25 PMID: 23918833
Wouters et al (2014) Central role for protein kinase C in oxyt. and epidermal growth factor stimulated cyclooxygenase 2 expression in human myometrial cells. Genes Cancer 7 357 PMID: 24916153
Martin et al (2014) miR-155 induced transcriptome changes in the MCF-7 breast cancer cell line leads to enhanced mitogen activated protein kinase signaling. J Exp Bot 5 353 PMID: 25352952
Wang et al (2015) Activation of protein synthesis in mouse uterine epithelial cells by OE-17β is mediated by a PKC-ERK1/2-mTOR signaling pathway. BMC Res Notes 112 E1382 PMID: 25733860
Do you know of a great paper that uses PD 184352 from Tocris? Please let us know.
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The role of MAPK pathways (JNK, p38 and ERK) was studied in the LPA induced pro-inflammatory phenotype in microglia. In this case cells were incubated for the indicated time points with LPA (1µM) in the presence or absence of PD98059 (10µM) or PD184352 (10µM). A series of assays were performed. The effect of PD1843452 was more prominent in slightly inhibiting the expression of pp65.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.