Research Area
Product Type
United States ( Change Country )
XL647 Chemical Structure
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Biological Activity
The activity of EXEL-7647 (XL647), a novel spectrum-selective kinase inhibitor with potent activity against the EGF and vascular endothelial growth factor receptor tyrosine kinase families, against both wild-type (WT) and mutant EGFR in vitro and in vivo[1,2] .
EXEL-7647 potently inhibits the EGFR and ErbB2 with IC50 0.3 and 16 nM respectively[2] .
EXEL-7647 inhibits cellular proliferation and EGFR pathway activation in the erlotinib-resistant H1975 cell line that harbors a double mutation (L858R and T790M) in the EGFR gene. EXEL-7647 substantially inhibited the growth of H1975 xenograft tumors and reduced both tumor EGFR signaling and tumor vessel density. Additionally, EXEL-7647 substantially inhibited the growth and vascularization of MDAMB-231 xenografts, a model which is more reliant on signaling through vascular endothelial growth factor receptors[2] .
References on XL647
- [1] Clin Cancer Res. 2008 Apr 15;14(8):2465-75.
- [2] Clin Cancer Res. 2007 Jun 15;13(12):3713-23
Chemical Information
| Molecular Weight (WM): | 491.39 |
|---|---|
| Formula: | C24H25Cl2FN4O2 |
| CAS No.: | 651031-01-5 |
| Synonyms: |
EXEL-7647
|
| Dissolve in (25°C): | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Receptor Tyrosine Kinase >> EGFR >> EGFR Inhibitors
Angiogenesis >> EGFR >> EGFR Inhibitors
JAK / STAT >> EGFR >> EGFR Inhibitors
Angiogenesis >> EGFR >> EGFR Inhibitors
JAK / STAT >> EGFR >> EGFR Inhibitors
Notes:
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