208260-29-1 Usage
Description
The Ras/Raf-1 signalling pathway is a well-characterized system that links receptor tyrosine kinase (RTK) activation with changes in gene expression and cell behavior. Raf-1 is a serine/threonine protein kinase that phosphorylates and activates MAPK-kinase (MEK) in response to activation by Ras. ZM 336372 is a potent ATP-competitive inhibitor of Raf-1 in vitro (IC50 = 70 nM) with the paradoxical effect of inducing >100-fold activation of Raf-1 in whole cells. Activation of the Raf-1 signalling pathway using ZM 336372 in human carcinoid tumor cells results in induction of cell cycle inhibitors and suppression of cellular proliferation.
Uses
Different sources of media describe the Uses of 208260-29-1 differently. You can refer to the following data:
1. It is small molecule tyrosine kinase modulator.
2. It is small molecule tyrosine kinase modulator. ZM336372 induces apoptosis associated with phosphorylation of GSK-3β in pancreatic adenocarcinoma cell lines.
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.
