CAS NO: | 627518-40-5 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 325.34 |
Cas No. | 627518-40-5 |
Formula | C18H16FN3O2 |
Solubility | ≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
Chemical Name | (Z)-N-(6,7-dimethoxy-1,2-dihydroindeno[1,2-c]pyrazol-3(4H)-ylidene)-3-fluoroaniline |
Canonical SMILES | COC1=C(OC)C=C2C(CC3=C2NN/C3=N\C4=CC=CC(F)=C4)=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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.