22-11-2012 дата публикации
Номер: US20120295965A1
Принадлежит:
Disclosed are compositions and methods related to identification of modulators of EGFR and VEGFR. 2. The method of claim 1 , wherein Rand Rare —COOH.3. The method of claim 1 , wherein Rand Rare —H.4. The method of claim 3 , wherein Rand Rare independently halogen claim 3 , —H claim 3 , C-Calkyl.5. The method of claim 3 , wherein Rand Rare independently Br claim 3 , —H claim 3 , C-Calkyl.6. The method of claim 3 , wherein Rand Rare independently —H claim 3 , C-Calkyl.7. The method of claim 3 , wherein Rand Rare independently —H claim 3 , C claim 3 , C claim 3 , C claim 3 , C claim 3 , C claim 3 , Cor Calkyl.9. The method of claim 8 , wherein Ris bromide claim 8 , hydrogen or unsubstituted C claim 8 , C claim 8 , Calkyl.10. The method of claim 8 , wherein Ris —H claim 8 , C claim 8 , C claim 8 , C claim 8 , C claim 8 , C claim 8 , Cor Calkyl.12. The method of claim 1 , wherein the subject is in need of an EGFR and VEGFR inhibitor to treat or prevent a disease.13. The method of claim 12 , wherein the disease is cancer or a malignant disease.14. The method of claim 13 , wherein the cancer is skin cancer claim 13 , colorectal cancer claim 13 , breast cancer claim 13 , thyroid cancer claim 13 , non-small cell lung cancer claim 13 , lung cancer claim 13 , or pancreatic cancer.15. A method to synthesize dual EGFR and VEGFR inhibitor claim 13 , comprising linking a thieno[3 claim 13 ,2-β]-thiophene scaffold with a building block that is a known fragment and functional group important for interactions with EGFR or VEGFR.16. A method of screening dual EGFR and VEGFR inhibitors claim 13 , comprising the steps:a. selecting at least two distinct cell lines each expressing at least one receptor of EGFR or VEGFR,b. selecting at least two markers, wherein one marker is the agonist for one of the two receptors, and another marker is an activator that transactivates another one of the two receptors,c. incubating each marker in the absence and presence of a test compound to its ...
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