DCC-2036
| CAS号 | 1020172-07-9 | 货号 | BCP02345 |
| 中文名 | DCC-2036 | ||
| 英文名 | DCC-2036 | ||
| 中文别名 | N-[3-叔丁基-1-(喹啉-6-基)-1H-吡唑-5-基]-N; | ||
| 英文别名 | DCC 2036;DCC2036;Rebastinib; | ||
| 分子式 | C30H28FN7O3 | 分子量 | 553.59 |
| 生物活性 | DCC-2036 shows the potent inhibitory activities against purified native Abl1 in unphosphorylated (u-Abl1native) and phosphorylated (p-Abl1native) forms, unphosphorylated and phosphorylated gatekeeper mutant Abl1T315I, and the activation loop mutant Abl1H396P in a non-ATP-competitive manner with IC50 of 0.8 nM, 2 nM, 1.4 nM, 5 nM, and 4 nM, respectively. Moreover, DCC-2036 also inhibits the Src family kinases Src, LYN, FGR, and HCK, and the receptor TKs KDR, FLT3, and TIE2 with IC50 of 34 nM, 29 nM, 38 nM, 40 nM, 4 nM, 2 nM and 6 nM, respectively.DCC-2036 shows the anti-proliferative activities against Ba/F3 cells expressing native or mutant Bcr-Abl1 with IC50 ranging from 2 nM to 150 nM. In addition, DCC-2036 also inhibits proliferation of the Ph+ cell line K562 (IC50 5.5 nM), and induces apoptosis in both Bcr-Abl1-expressing Ba/F3 and K562 cells potently. [1] A recent study shows that DCC-2036 shows the selectivity for growth inhibition of Bcr-Abl-positive cells by its marked inhibiti | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase | ||
| 靶 点 | Src/Bcr Abl Tie2 FLT3 | ||
结构式
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