CAS NO: | 1267949-42-7 |
包装: | 50mg, 100mg, 250mg |
规格: | ≥98% |
DW532 is one of simplified analogues of hematoxylin that has shown broad-spectrum inhibition on tyrosine kinases and in vitro anti-cancer activities. DW532 inhibited EGFR and VEGFR2 in vitro kinase activity (the IC50 were 4.9 and 5.5 μmol/L, respectively), and suppressed their downstream signaling. DW532 dose-dependently inhibited tubulin polymerization via direct binding to tubulin, thus disrupting the mitotic spindle assembly and leading to abnormal cell division. In a panel of human cancer cells, DW532 (1 and 10 μmol/L) induced G2/M phase arrest and cell apoptosis, which subsequently resulted in cytotoxicity. Knockdown of BubR1 or Mps1, the two core proteins of the spindle assembly checkpoint dramatically decreased DW532-induced cell cycle arrest in MDA-MB-468 cells. Moreover, treatment with DW532 potently and dose-dependently suppressed angiogenesis in vitro and in vivo. ( Acta Pharmacol Sin. 2014 Jul;35(7):916-28.) References: Peng T, Wu JR, Tong LJ, Li MY, Chen F, Leng YX, Qu R, Han K, Su Y, Chen Y, Duan WH, Xie H, Ding J. Identification of DW532 as a novel anti-tumor agent targeting both kinases and tubulin. Acta Pharmacol Sin. 2014 Jul;35(7):916-28. doi: 10.1038/aps.2014.33. Epub 2014 May 26. PubMed PMID: 24858311; PubMed Central PMCID: PMC4088284.
纯度:≥98%
CAS:1267949-42-7