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PD 184,352

ALX-270-471

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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.

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Product Details

Alternative Name	2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide, CI-1040
Appearance	White to off-white solid.
CAS	212631-79-3
Couple Target	MEK
Couple Type	Inhibitor
Formula	C₁₇H₁₄ClF₂IN₂O₂
Identity	Determined by NMR.
MW	478.7
Purity	≥95% (HPLC)
Solubility	Soluble in organic solvents.
Source	Synthetic.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

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 — Full Text
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 — Full Text
p90 Ribosomal S6 kinases play a significant role in early gene regulation in the cardiomyocyte response to Gq-protein-coupled receptor stimuli, endothelin-1 and α1-adrenergic receptor agonists: E. Amirak, et al.; Biochem. J. 450, 351 (2013), Application(s): Adult rat heart perfusions and cardiomyocyte treatment, Abstract — Full Text
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 — Full Text
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 — Full Text
Specificity and mechanism of action of some commonly used protein kinase inhibitors: S.P. Davies, et al.; Biochem. J. 351, 95 (2000), Abstract — Full Text
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

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PD 184,352

ALX-270-471

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