627518-40-5 Usage
Biological Activity
jnj-10198409 is a small molecule inhibitor of platelet-derived growth factor (pdgf-bb) tyrosine kinase [1].platelet-derived growth factor (pdgf) is a ubiquitous mitogen involved in regulating cell growth and division, embryonic development, cell proliferation, cell migration, and angiogenesis. overexpression of pdgf has been associated with several diseases such as atherosclerosis, fibrotic disorders and malignancies. inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (pdgf-bb) receptor can have potent antiangiogenic and antiproliferative activity. recombinant pdgf is used in medicine to help heal chronic ulcers and in orthopedic surgery and periodontistry to treat bone loss [2].in human coronary artery smooth muscle cells, jnj-10198409 inhibited the activity of platelet-derived growth factor (pdgf-bb) tyrosine kinase with an ic50 value of 4.2 nm when tested. jnj-10198409 was a competitive antagonist of the atp binding and hydrolysis at pdgf-bb receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis [1].
references
[1] ho c y, ludovici d w, maharoof u s m, et al. (6, 7-dimethoxy-2, 4-dihydroindeno [1, 2-c] pyrazol-3-yl) phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells[j]. journal of medicinal chemistry, 2005, 48(26): 8163-8173.[2] raines e w, bowen-pope d f, ross r. platelet-derived growth factor[m]//peptide growth factors and their receptors i. springer berlin heidelberg, 1990: 173-262.
Check Digit Verification of cas no
The CAS Registry Mumber 627518-40-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 6,2,7,5,1 and 8 respectively; the second part has 2 digits, 4 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 627518-40:
(8*6)+(7*2)+(6*7)+(5*5)+(4*1)+(3*8)+(2*4)+(1*0)=165
165 % 10 = 5
So 627518-40-5 is a valid CAS Registry Number.
627518-40-5Relevant articles and documents
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: Platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells
Ho, Chih Y.,Ludovici, Donald W.,Maharoof, Umar S. M.,Mei, Jay,Sechler, Jan L.,Tuman, Robert W.,Strobel, Eric D.,Andraka, Laura,Yen, Hwa-Kwo,Leo, Gregory,Li, Jian,Almond, Harold,Lu, Hong,DeVine, Ann,Tominovich, Rose M.,Baker, Judith,Emanuel, Stuart,Gruninger, Robert H.,Middleton, Steven A.,Johnson, Dana L.,Galemmo Jr., Robert A.
, p. 8163 - 8173 (2005)
A series of (6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl) phenylamines has been optimized to preserve both potent kinase inhibition activity against the angiogenesis target, the receptor tyrosine kinase of Platelet-Derived Growth Factor-BB (PDGF-BB