別品名 |
Tyrphostin B42, N-Benzyl-3,4-dihydroxy-benzylidenecyanoacetamide
|
別包装 |
あり
|
純度 |
>=98%
|
分子量 |
294.31
|
CAS RN® |
133550-30-8
|
化合物の概要 |
JAK2 inhibitor, potential EGFR inhibitor.
|
構造 |
C17H14N2O3
|
溶媒 |
Soluble in DMSO.
|
使用目的 |
Tyrphostin AG490 inhibits JAK2 and exhibits anti-diabetic, anti-atherosclerotic, immunosuppressive, and anticancer activities. Tyrphostin AG490 inhibits joint inflammation in vivo by suppressing activation of STAT3, production of TNF-α and RANKL, and differentiation of osteoclasts. Tyrphostin AG490 also induces programmed cell death and inhibits invasion and adhesion of leukemia cells. In animal models of atherosclerosis, tyrphostin AG490 decreases activity and expression of Nox and levels of CD68, decreasing the formation of atherosclerotic lesions. Additionally, tyrphostin AG490 increases expression of PPARγ and decreases blood glucose levels in vivo, preventing the onset of autoimmune type 1 diabetes. This compound also inhibits expression of MCP-1, IFNγ, and MHC class II, decreases infiltration of T cells and macrophages, and suppresses deposition of IgG in animal models of lupus nephritis. Tyrphostin AG490 may also inhibit EGFR.
|
その他 |
[融点]215℃-216.5℃ [外観]Greenish-yellow microcrystalline powder
|
参考文献 |
Gyurkovska V, Stefanova T, Dimitrova P, et al. Tyrosine Kinase Inhibitor Tyrphostin AG490 Retards Chronic Joint Inflammation in Mice. Inflammation. 2014 Aug;37(4):995-1005. PMID: 24473905.Davoodi-Semiromi A, Hassanzadeh A, Wasserfall CH, et al. Tyrphostin AG490 agent modestly but significantly prevents onset of type 1 in NOD mouse; implication of immunologic and metabolic effects of a Jak-Stat pathway inhibitor. J Clin Immunol. 2012 Oct;32(5):1038-47. PMID: 22661285. Fenyo IM, Florea IC, Raicu M, et al. Tyrphostin AG490 reduces NAPDH oxidase activity and expression in the aorta of hypercholesterolemic apolipoprotein E-deficient mice. Vascul Pharmacol. 2011 Mar-Jun;54(3-6):100-6. PMID: 21457788.Wang S, Yang N, Zhang L, et al. Jak/STAT signaling is involved in the inflammatory infiltration of the kidneys in MRL/lpr mice. Lupus. 2010 Sep;19(10):1171-80. PMID: 20501525.Caceres-Cortes JR. A potent anti-carcinoma and anti-acute myeloblastic leukemia agent, AG490. Anticancer Agents Med Chem. 2008 Oct;8(7):717-22. PMID: 18855573.
|
※サムネイル画像をクリックすると拡大画像が表示されます。
|
|
|
メーカー |
品番 |
包装 |
LKT
|
T9969
|
25 MG
|
※表示価格について
当社在庫 |
なし
|
納期目安 |
1週間程度
|
法規制 |
劇
|
保存温度 |
4℃
|
|