货号 | 4965/10 |
别名 | 6-(2,6-Dichlorophenyl)-2-[(4-fluoro |
供应商 | Tocris |
生物活性 | ATP-competitive inhibitor of p210bcr/abl tyrosine kinase; selectively induces apoptosis in chronic myeloid leukemia (CML) K562 cells. Inhibits in vivo tyrosine phosphorylation of Gab2, CrkL and p210bcr/abl(IC50 values are 80, 80 and 170 nM respectively). Potently inhibits p210bcr/ablautophosphorylationin vitro(IC50 = 5 nM). Also potently inhibits c-Src and KIT (IC50 values are 0.8 and 50 nM, respectively). |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 429.27 |
分子式 | C21H15Cl2FN4 |
可溶性/溶解性 | Soluble to 50 mM in DMSO |
参考文献 | Corbinet al (2004) Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970. Blood 104 3754. PMID: 15304388. La Roséeet al (2002) Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to imatinib mesylate (Gleevec, STI571). Cancer Res. 62 7149. PMID: 12499247. Dorseyet al (2000) The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210bcr-abl tyrosine kinase and induces apoptosis of K562 leukemic cells. Cancer Res. 60 3127. PMID: 10866298. |