P-8499 PD 184352, Free Base, >99%

Synonyms : [CI-1040]

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  • 10 mg
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  • 25 mg
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  • 50 mg
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  • 100 mg
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  • 200 mg
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  • 500 mg
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  • 1 g
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  • M.W. 478.66
  • C17H14ClF2IN2O2
  • [212631-79-3]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 50 mg/mL; soluble in ethanol at 8.3 mg/mL with slight warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 5-10 µM buffers, serum, or other additives may increase or decrease the aqueous solu. Disposal: A.

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  • PD184352 is an inhibitor of mitogen activated protein kinase kinase (MEK or MAPKK).
  • Antitumor activity of PD184352 is evident in preclinical models, including pancreas, colon, and breast cancers, which are associated with its inhibition of pERK. Allen, L.F., et al. "CI-1040 (PD184352), a targeted signal transduction inhibitor of MEK (MAPKK)." Semin. Oncol. 30: 105-116 (2003).
  • PD184352 profoundly inhibited the growth of, and induced apoptosis in, ovarian tumor cells with mutations in either KRAS or BRAF. However, ovarian cancer cells containing wild-type sequences were not sensitive to PD184352. Pohl, G., et al. "Inactivation of the mitogen-activated protein kinase pathway as a potential target-based therapy in ovarian serous tumors with KRAS or BRAF mutations." Cancer Res. 65: 1994-2000 (2005).
  • PD184352 inhibited C-Raf with an IC50 of 12 nM and inhibited more than 90% of ERK phosphorylation at a concentration of 10 nM. In vivo, PD184352 decreased adenoma formation and significantly restored lung structure. Kramer, B.W., et al. "Use of mitogenic cascade blockers for treatment of C-Raf induced lung adenoma in vivo: CI-1040 strongly reduces growth and improves lung structure." BMC Cancer 4: 24 (2004).
  • PD184352 inhibited the MAPK pathway and induced apoptosis through a pathway involved in dephosphorylation, aggregation of Fas-associated death domain protein, and death receptor-independent caspase-8 activation. Meng, X.W., et al. "Central Role of Fas-associated Death Domain Protein in Apoptosis Induction by the Mitogen-activated Protein Kinase Kinase Inhibitor CI-1040 (PD184352) in Acute Lymphocytic Leukemia Cells in Vitro." J. Biol. Chem. 278: 47326-47339 (2003).
  • However, PD184352 suffered from poor pharmacokinetics because of its low solubility and rapid clearance. Barrett, S.D., et al. "The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901." Bioorg. Med. Chem. Lett. 18: 6501-6504 (2008).
  • Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.