Description
Tyrphostin AG-490 inhibits HER-2 driven cell proliferation with IC50 of 3.5 uM. Corresponding to the specific dose-dependent inhibition of constitutively activated JAK2 in pre-B acute leukemia (ALL) cells, AG-490 (5 uM) almost completely blocks the growth of all ALL cells by inducing programmed cell death, with no deleterious effect on normal hematopoiesis. AG-490 does not inhibit the activities of Lck, Lyn, Btk, Syk, and Src. AG-490 (60-100 uM) blocks the constitutive activation of Stat3sm, and inhibits spontaneous as well as interleukin 2-induced growth of mycosis fungoides (MF) tumor cells with IC50 values of 75 uM and 20 uM, respectively. AG-490 potently inhibits IL-2-mediated human T cell growth with an IC50 of 25 uM by blocking the activities of JAK3 and STAT5a/b. Although AG-490 alone has no effect on proliferation of FDrv210H cells at a concentration of 5 uM, AG-490 can synergize with STI571 to enhance its inhibitory effect on p210bcr-abl driven proliferation. AG-490 significantly inhibits the constitutive activation of Stat3 in MOPC, MPC11, and S194 cells, leading to dramatic dose-dependent apoptosis. AG-490 (100 uM) inhibits Akt phosphorylation, inhibits the activation of nuclear factor-κB, and causes the activation of GSK-3β, leading to the reduction of c-Myc. AG-490 (50 uM) can induce apoptosis of imatinib-resistant BaF3 cells expressing T315I and E255K mutants of Bcr-Abl. AG-490 at 30 uM inhibits not only Epo-induced phosphorylation of wild-type JAK2 but also constitutive phosphorylation of the JAK2 V617F mutant. AG-490 also potently inhibits cytokine-independent cell growth induced by the JAK2 V617F mutant in BaF3 cells. |
|
Cat No |
Size |
Price($) |
 |
BC093-010 |
10mg |
0 |
|
BC093-025 |
25mg |
0 |
|
BC093-100 |
100mg |
0 |
|
|
|
M.W 294.30
Formular C17H14N2O3
Solubility Soluble in DMSO at 200 mg/mL
Purity >99%
Biological Activity
Selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 uM for EGFR and ErbB2 respectively). Inhibitor of JAK2, JAK3/STAT, JAK3/AP-1 and JAK3/MAPK pathways and potently inhibits cytokine-independent cell growth in vitro and tumor cell invasion in vivo
Synonym
AG 490, Tyrphostin B42, N-Benzyl-3,4-dihydroxy-benzylidenecyanoacetamide
Store at -20oC, Desiccate
|
|
普瑞麦迪(北京)实验室技术有限公司
