• All
  • Primary Antibodies
  • Conjugated Antibodies for IF
  • Conjugated Antibodies for FC
  • Secondary Antibodies
  • Antibody Labeling KitsNew
  • ELISA Kits
  • IHC Kits
  • Magnetic Cell Separation Kits
  • Cytokines & Growth Factors
  • Neutralizing/activating Antibodies
  • Nanobody-based Reagents
  • Accessory Products and Kits
  • Fusion Proteins
×
×
Host
0
Species Reactivity
0
Species Reactivity
0
Conjugate
0
Conjugate
0
Compatible Species
0
Conjugate
0

AG490

AG490 (Tyrphostin B42) 是一种 EGFR 抑制剂 ，IC50为 0.1 μM。它对 EGFR 的选择性比 ErbB2 高 135 倍，还抑制 JAK2。

CAS号

133550-30-8

分子式

C17H14N2O3

主要靶点

EGFR|Autophagy|JAK|STAT

仅限科研使用

Cat No : CM04882

Print datasheet

Synonyms

Zinc02557947|Tyrphostin AG 490|AG 490|AG-490|Tyrphostin B42

验证数据展示

  • CAS No.: 133550-30-8

    AG490
    CAS#: 133550-30-8

产品信息

AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn, Lck, Syk, Btk, and Src.

CAS号 133550-30-8
分子式 C17H14N2O3
主要靶点 EGFR|Autophagy|JAK|STAT
主要通路 JAK/STAT信号通路|蛋白酪氨酸激酶|干细胞|表观遗传|血管生成|自噬
分子量 294.3
纯度 99.39%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 Zinc02557947|Tyrphostin AG 490|AG 490|AG-490|Tyrphostin B42

靶点活性

EGFR:0.1 μM

体内活性

通过诱导程序性细胞死亡,AG-490（5 μM）几乎完全抑制所有ALL 细胞生长,而不影响正常造血功能。AG-490（30 μM）既对Epo诱导的野生型JAK2磷酸化有抑制作用,也对组成型的JAK2 V617F突变型磷酸化有抑制作用。AG-490（50 μM）对表达Bcr-Abl 突变型E255K和T315I的抗Imatinib的BaF3细胞凋亡具有诱导作用。AG-490（60-100 μM）对Stat3sm组成型激活有抑制作用,且抑制自发的（IC50：75 μM）或IL-2诱导的（IC50：20 μM）蕈菌肿瘤细胞生长。AG-490（100 μM）抑制Akt磷酸化和核因子-κB激活,且激活GSK-3β并导致c-Myc降低。AG-490对EGF依赖的HER 14细胞增殖有抑制作用（IC50：3.5 μM）。通过对JAK3和 STAT5a/b活性的抑制,AG-490有效抑制IL-2调节的人T细胞生长（IC50：25 μM）。 尽管AG-490 （5 μM）单独给药不影响FDrv210H细胞增殖,但其可协同增强STI571对p210bcr-abl的抑制从而促进增殖效果。

体外活性

在体内,AG-490处理可促使小鼠骨髓瘤细胞凋亡,但不影响IL-12诱导的巨噬细胞活化和IFN-γ产量.AG-490（0.5 mg/day）处理裸鼠10天,对JAK2 V617F突变诱导的肿瘤形成及入侵有显著抑制效果.AG-490可大幅降低CD45+和HLA-DR+细胞数,在骨髓中,其可使上述细胞数分别从48% 和46%降低到不可检测水平,这未处理小鼠脾脏中,则从38%和 22% 降低到不可检测水平.

溶解度

DMSO:59 mg/mL (200.47 mM),Ethanol:6 mg/mL (20.38 mM)

细胞实验

Cells are exposed to different concentrations of AG-490 for 16 hours. For the determination of cell proliferation, [3H]tymidine (1 μCi) is added 6 hours or more before the cultures are terminated. Cells are then collected and samples counted in a liquid scintillation counter. (Only for Reference)

参考文献

1.Gazit A, et al. J Med Chem, 1991, 34(6), 1896-1907.
2.Meydan N, et al. Nature, 1996, 379(6566), 645-648.
3.Nielsen M, et al. Proc Natl Acad Sci U S A, 1997, 94(13), 6764-6769.
4.Kirken RA, et al. J Leukoc Biol, 1999, 65(6), 891-899.
5.Sun X, et al. Blood, 2001, 97(7), 22008-22015.
6.Cheppudira BP, et al. Anti-hyperalgesic effects of AG490, a Janus kinase inhibitor, in a rat model of inflammatory pain. Biomed Rep. 2015 Sep;3(5):703-706.
7.Zhu J, Pan X, Lin B, et al. The effect of hirudin on antagonisting thrombin induced apoptosis of human microvascular endothelial cells[J]. Acta cirurgica brasileira. 2019, 34(1).

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
=
×
×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2