Tyrphostin AG 1296
- 貨號 Cat. No.
- T-770
- 規格 Size
- 1 mg 5x1mg 5mg
Description
Tyrphostin AG 1296
PDGF Receptor Tyrosine Kinase Inhibitor
| Product#: | T-770 |
| Sizes: |
| 1 mg |
| 5 x 1 mg |
| 5 mg |
| M.W.: | 266.30 |
| CAS No.: | [146535-11-7] |
| Structure: |
 |
| Purity: | >98% |
| Bioassay: |
| Tyrphostin AG 1296 (AG 1296) inhibits the kinase activity of PDGF receptor (PDGFR). |
 |
3T3-L1 cells were serum starved for 3 h and incubated in presence or absence of different concentrations of AG 1296 (#T-770) for 30 min. The cells were stimulated with 10 ng/ml PDGF BB to induce PDGFR activity. The cells proteins were extracted and analyzed by Western blot using anti-phospho-PDGFR and anti-phospho-ERK1/2. The kinase activity of PDGFR decreases as a function of AG 1296 concentration increase. |
| References: |
1. | Kovalenko, M. et al. (1994) Cancer Res. 54, 6106. |
2. | Milenkovic, I. et al. (2003) Invest. Ophthalmol. Vis. Sci. 44,1211. |
3. | Iwasaki, H. et al. (1999) Endocrinology, 140, 4659. |
4. | Levitzki, A. and Gazit, A. (1995) Science 267, 1782. |
5. | Rice, A.B. et al. (1999) Am. J. Pathol. 155, 213. |
6. | Krystal, G.W. et al. (1997) Cancer Res. 57, 2203. |
7. | Tse, K.F. et al. (2001) Leukemia 15, 1001. |
8. | Matthews, W. et al. (1991) Cell 65,1143. |
Tyrphostin AG1296 is a tyrosine kinase blocker which selectively inhibits platelet-derived growth factor (PDGF) a- and b-receptor kinases and the PDGF-dependent signaling in many cell types. Tyrphostin AG1296 also inhibits the PDGF dependent transactivation of the P2Y and Endothelin receptors-evoked cell proliferation and MAPK activation.1-4
This PDGF receptor (PDGFR) blocker has no effect on epidermal growth factor (EGF) receptor autophosphorylation; weak effects on DNA synthesis stimulated by insulin, by EGF, or by a combination of both; and over an order of magnitude weaker blocking effect on fibroblast growth factor-dependent (FGF) DNA synthesis.5-8 Tyrphostin AG1296 also potently inhibits the signaling of stem cell factor (SCF) receptor (c-Kit) and its upstream effector Kit receptor tyrosine kinase and the tyrosine kinase activity of FLT3-ITD which both have a strong sequence similarity with other members of the class III receptor tyrosine kinase but has no effect on the autophosphorylation of vascular endothelial growth factor (VEGF) receptor. 7,8