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本试剂(2-[(2-氯-4-碘苯基)氨基]-N-(环丙基甲氧基)-3,4-二氟-苯甲酰胺)
仅供科研实验使用,不得用于其他用途！
简介：
货 号：LC2-P-8499
名 称：2-[(2-氯-4-碘苯基)氨基]-N-(环丙基甲氧基)-3,4-二氟-苯甲酰胺
别 名：PD 184352 Free Base
C A S ：212631-79-3
分子量：478.66
分子式：C17H14ClF2IN2O2
纯 度：HPLC/TLC:>99%
说 明：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.
文 献：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).
