1198408-78-4 Usage
Biological Activity
ldn-211904 is an inhibitor of erythropoietin-producing hepatocellular carcinoma (eph) receptors.erythropoietin-producing hepatocellular carcinoma (eph) receptors, a group of highly conserved transmembrane proteins composed of multiple domains, participate in various cell signaling pathways. so far, 16 eph receptors have been identified in vertebrates, which can be divided into two major classes (epha and ephb) based on sequence similarity. mammals including humans have 14 eph receptors (epha1–epha8, epha10, ephb1–ephb4 and ephb6).
in vitro
previous study found that ldn-211904, a 4-piperidinyl analog, retained significant ephb3 inhibitory activity, and also had greater aqueous solubility due to the presence of a basic amine. ldn-211904 was profiled for functional inhibitory activity against a panel of 288 kinases and the results showed that ldn-211904 was quite selective for tyrosine kinases. the only noted exceptions were the three serine/threonine kinases p38a, p38b, and qik. in addition, only ldn-211904 showed moderate selectivity among the tyrosine kinases and little selectivity verses other epha and ephb subtypes, except for epha6 and epha7. moreover, ldn-211904 demonstrated the best stability with a t1/2 of 348 min and a clint of 4 μl/min/mg protein [1].
IC 50
79 nm for ephb3
references
[1] qiao, l. ,choi, s.,case, a., et al. structure-activity relationship study of ephb3 receptor tyrosine kinase inhibitors. bioor. med. chem. lett. 19(21), 6122-6126 (2009).
Check Digit Verification of cas no
The CAS Registry Mumber 1198408-78-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,9,8,4,0 and 8 respectively; the second part has 2 digits, 7 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 1198408-78:
(9*1)+(8*1)+(7*9)+(6*8)+(5*4)+(4*0)+(3*8)+(2*7)+(1*8)=194
194 % 10 = 4
So 1198408-78-4 is a valid CAS Registry Number.
1198408-78-4Relevant articles and documents
Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors
Qiao, Lixin,Choi, Sungwoon,Case, April,Gainer, Thomas G.,Seyb, Kathleen,Glicksman, Marcie A.,Lo, Donald C.,Stein, Ross L.,Cuny, Gregory D.
supporting information; experimental part, p. 6122 - 6126 (2010/06/16)
A structure-activity relationship study for a 2-chloroanilide derivative of pyrazolo[1,5-a]pyridine revealed that increased EphB3 kinase inhibitory activity could be accomplished by retaining the 2-chloroanilide and introducing a phenyl or small electron donating substituents to the 5-position of the pyrazolo[1,5-a]pyridine. In addition, replacement of the pyrazolo[1,5-a]pyridine with imidazo[1,2-a]pyridine was well tolerated and resulted in enhanced mouse liver microsome stability. The structure-activity relationship for EphB3 inhibition of both heterocyclic series was similar. Kinase inhibitory activity was also demonstrated for representative analogs in cell culture. An analog (32, LDN-211904) was also profiled for inhibitory activity against a panel of 288 kinases and found to be quite selective for tyrosine kinases. Overall, these studies provide useful molecular probes for examining the in vitro, cellular and potentially in vivo kinase-dependent function of EphB3 receptor.
