PD 153035
- 貨號 Cat. No.
- P-360
- 規格 Size
- 10 x 0.1 mg 1mg 5x1mg
Description
PD 153035
Potent EGF Receptor Tyrosine Kinase Inhibitor
| Product#: | P-360 |
| Sizes: |
| 10 x 0.1 mg |
| 1 mg |
| 5 x 1 mg |
is a small molecule derivated from brominated anilinoquinazoline which inhibits tyrosine kinase activity of the EGFR by competition at the ATP binding site. PD 153035 is a highly potent inhibitor for auto and hetro tyrosine kinase activity of EGF receptor (ERB2) at sub nM concentrations and inhibits other purified tyrosine kinases only at micromolar or higher concentrations.1-3
PD 153053 abolished all growth effects mediated by the addition of exogenous EGF in a receptor number-dependent manner and shows a remarkable apoptotic and cytotoxic activity against several types of tumor cell lines that overexpress the EGF receptor in vitro and in vivo .4-8
| M.W.: | 360.21 |
| Structure: |
 |
| Purity: | >99% |
| Bioassay: |
| PD 153035 inhibits EGF receptor activation. |
 |
3T3-L1 cells were serum starved for 3h and preincubated with different concentrations of PD 153035 for 2h. The cells were then stimulated with 200ng/ml EGF for 10 min. The cell proteins were resolved by SDS PAGE and detected with either Anti-phospho EGFr (upper panel) or Anti-phospho ERK1/2 (lower panel). |
| References: |
1. | Fry, D.W. et al. (1994) Science 265, 1093. |
2. | Kunkel, M.W. et al. (1996) Invest. New Drugs 13, 295. |
3. | Bridges, A.J. et al. (1996) J. Med. Chem. 39, 267. |
4. | Bos, M. et al. (1997) Clin. Cancer Res. 3, 2099. |
5. | Goossens, J.F. et al. (2001) Biochemistry 40, 4663. |
6. | Faust, R.A. et al. (1999) Oral Oncol. 35 290. |
7. | Kunkel, M.W. et al. (1996) Invest New Drugs, 13. 295. |
8. | Fredriksson, A. et al. (1999) Life Sci. 65, 165. |
PD 153035