Tandutinib
Tandutinib is an inhibitor of several kinases, including FMS-like tyrosine kinase 3 (FLT3), PDGFR, and Kit. Tandutinib exhibits anticancer chemotherapeutic and anti-angiogenic activities and currently shows mixed results in clinical trials as a potential treatment for several cancers. In vivo, tandutinib inhibits phosphorylation of c-Kit, Akt, mTOR, and p70S6 kinase; it also increases activation of caspase 3 and the ratio of Bax/Bcl-2 and decreases expression of cyclin D1, resulting in apoptosis. In animal models, tandutinib decreases expression of COX-2 and VEGF, decreasing vessel formation and inhibiting growth of colon cancer xenografts. In an in vivo model of medulloblastoma, this compound decreases tumor volume.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18974796
| Cas No. |
387867-13-2 |
|---|---|
| Purity |
≥98% |
| Formula |
C31H42N6O4 |
| Formula Wt. |
562.7 |
| IUPAC Name |
4-[6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-yl]-N-(4-propan-2-yloxyphenyl)piperazine-1-carboxamide |
| Melting Point |
177-178°C |
| Appearance |
Yellow Crystal Powder |
Ponnurangam S, Standing D, Rangarajan P, et al. Tandutinib inhibits the Akt/mTOR signaling pathway to inhibit colon cancer growth. Mol Cancer Ther. 2013 May;12(5):598-609. PMID: 23427297.
Ohshima-Hosoyama S, Davare MA, Prajapati SI, et al. Preclinical testing of tandutinib in a transgenic medulloblastoma mouse model. J Pediatr Hematol Oncol. 2012 Mar;34(2):116-21. PMID: 22146535.
Griswold IJ, Shen LJ, La Rosée P, et al. Effects of MLN518, a dual FLT3 and KIT inhibitor, on normal and malignant hematopoiesis. Blood. 2004 Nov 1;104(9):2912-8. PMID: 15242881.
