Formulation: A solid
Formal Name: 4-ethyl-N-[3-[(4-methyl-1-piperazinyl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)-benzamide
Purity: ≥98%
Formula Markup: C30H29F3N6O
Formula Weight: 546,6
Shelf life (days): 1460
CAS Number: 1429617-90-2
Notes: 7rh is an inhibitor of discoidin domain receptor 1 (DDR1; IC50 = 6.8 nM).{66917} It is selective for DDR1 over DDR2, Bcr-Abl, and c-Kit (IC50s = 101.4, 355, and >10,000 nM, respectively). 7rh inhibits the proliferation of A549, H23, and H460 non-small cell lung cancer (NSCLC) and K562 leukemia cells (IC50s = 2.7, 2.1, 3, and 0.038 µM, respectively). It also inhibits the invasion and cell-matrix adhesion of H23 cells when used at a concentration of 5 µM. 7rh (8 mg/kg) reduces tumor volume in a CNE-2 nasopharyngeal carcinoma mouse xenograft model when administered alone or in combination with dasatinib (Item No. 11498).{66918}
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