Potent and selective inhibitor of MAPK (ERK kinase 1; MEK1) activation (IC50=300nM in vitro, IC50=2nM in vivo). Suppresses activation of MAPK but does not block its activity. Strongly suppresses growth of human implanted colon tumors in mice.
Product Details
| Alternative Name: | 2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide, CI-1040 |
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| Formula: | C17H14ClF2IN2O2 |
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| MW: | 478.7 |
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| Source: | Synthetic. |
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| CAS: | 212631-79-3 |
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| Purity: | ≥95% (HPLC) |
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| Identity: | Determined by NMR. |
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| Appearance: | White to off-white solid. |
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| Solubility: | Soluble in organic solvents. |
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| Shipping: | Ambient |
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| Long Term Storage: | -20°C |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Qing Yan Li Ge Tang, a Chinese Herbal Formula, Induces Autophagic Cell Death through the PI3K/Akt/mTOR Pathway in Nasopharyngeal Carcinoma Cells In Vitro: C.H. Yang, et al.; Evid. Based Complement. Alternat. Med.
1155, 9925684 (2021),
Abstract;
Nrf2/Keap1 Pathway and Expression of Oxidative Stress Lesions 8-hydroxy-2’-deoxyguanosine and Nitrotyrosine in Melanoma: H.R. Hintsala, et al.; Anticancer Res.
36, 1497 (2016),
Application(s): Inhibiting MEK1/MEK2 by blocking ERK phosphorylation,
Abstract;
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Serine-727 phosphorylation activates hypothalamic STAT-3 independently from tyrosine-705 phosphorylation: A. Breit, et al.; Mol. Endocrinol.
29, 445 (2015),
Application(s): Western Blotting,
Abstract;
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The effects of a novel MEK inhibitor PD184161 on MEK-ERK signaling and growth in human liver cancer: P.J. Klein, et al.; Neoplasia
8, 1 (2006),
Abstract;
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Effects of the MEK inhibitor CI-1040 (PD 184352) on progenitor growth from normal and myelodysplastic marrow: D.P. Steensma, et al.; Haematologica
88, 1072 (2003),
Abstract;
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),
Abstract;
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Specificity and mechanism of action of some commonly used protein kinase inhibitors: S.P. Davies, et al.; Biochem. J.
351, 95 (2000),
Abstract;
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Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo: J.S. Sebolt-Leopold, et al.; Nat. Med.
5, 810 (1999),
Abstract;
