208260-29-1 Usage
Description
ZM 336372 is a potent ATP-competitive inhibitor of the Raf-1 protein, which plays a crucial role in the Ras/Raf-1 signaling pathway. This small molecule tyrosine kinase modulator has the unique ability to induce >100-fold activation of Raf-1 in whole cells, despite its inhibitory nature in vitro. It is known for its paradoxical effect on the Raf-1 signaling pathway and its potential applications in inducing apoptosis in certain cancer cell lines.
Uses
Used in Pharmaceutical Industry:
ZM 336372 is used as a small molecule tyrosine kinase modulator for its ability to inhibit the Raf-1 protein, which is involved in the Ras/Raf-1 signaling pathway. This makes it a promising candidate for the development of targeted therapies against various cancers.
Used in Cancer Research:
ZM 336372 is used as an inducer of apoptosis in pancreatic adenocarcinoma cell lines, where it has been shown to be effective in promoting cell death through the phosphorylation of GSK-3β. This suggests its potential use in the development of treatments for pancreatic cancer.
Used in Cellular Proliferation Studies:
In human carcinoid tumor cells, ZM 336372 is used to activate the Raf-1 signaling pathway, leading to the induction of cell cycle inhibitors and suppression of cellular proliferation. This application aids in understanding the role of the Raf-1 pathway in cell growth and the development of potential therapeutic strategies for cancer treatment.
References
1) Hall-Jackson et al. (1999), Paradoxical activation of Raf by a novel Raf inhibitor; Chem. Biol., 6 559
2) Deming et al. (2010), ZM336372 induces apoptosis associated with phosphorylation of GSK-3beta in pancreatic adenocarcinoma cell lines; J. Surg. Res., 161 28
Check Digit Verification of cas no
The CAS Registry Mumber 208260-29-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,0,8,2,6 and 0 respectively; the second part has 2 digits, 2 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 208260-29:
(8*2)+(7*0)+(6*8)+(5*2)+(4*6)+(3*0)+(2*2)+(1*9)=111
111 % 10 = 1
So 208260-29-1 is a valid CAS Registry Number.
InChI:InChI=1/C23H23N3O3/c1-15-7-10-18(24-23(29)17-5-4-6-19(13-17)26(2)3)14-21(15)25-22(28)16-8-11-20(27)12-9-16/h4-14,27H,1-3H3,(H,24,29)(H,25,28)
208260-29-1Relevant articles and documents
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis
Brown, Dearg S.,Belfield, Andrew J.,Brown, George R.,Campbell, Douglas,Foubister, Alan,Masters, David J.,Pike, Kurt G.,Snelson, Wendy L.,Wells, Stuart L.
, p. 5383 - 5387 (2007/10/03)
The discovery, rational analogue design, synthesis and SAR of a novel bisamide class of p38 MAP kinase inhibitor are reported. The activity in vitro is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues, such as 18. A novel p38 MAP kinase inhibitor structural class was discovered through selectivity screening. The rational analogue design, synthesis and structure-activity relationship of this series of bis-amide inhibitors is reported. The inhibition in vitro of human p38α enzyme activity and lipopolysaccharide-induced tumour necrosis factor-α release is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues.
