中文名 | BMS-599626 (Hydrochloride) |
英文名 | BMS-599626 (Hydrochloride) |
别名 | BMS-599626 盐酸盐 HER1和HER2高效抑制剂(BMS-599626 HYDROCHLORIDE) [4-[[1-[(3-氟苯基)甲基]-1H-吲唑-5-基]氨基]-5-甲基吡咯并[2,1-F][1,2,4]三嗪-6-基]氨基甲酸 (3S)-3-吗啉基甲基酯盐酸盐 |
英文别名 | AC480 AC-480 CS-173 AC480 HCl BMS599626 BMS 599626 BMS-599626 HCl BMS-599626 HCL BMS-599626 (AC480) BMS-599626 (Hydrochloride) BMS-599626 hydrochloride(AC480 [4-[[1-[(3-Fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid (3S)-3-morpholinylmethyl ester hydrochloride |
CAS | 873837-23-1 |
化学式 | C27H28ClFN8O3 |
分子量 | 567.0144232 |
溶解度 | 10毫米DMSO |
存储条件 | -20℃ |
体外研究 | BMS-599626 Hydrochloride inhibits the proliferation of tumor cells that are dependent on HER1/HER2 signaling.BMS-599626 Hydrochloride (0.03-8 μM; 1 huors) results in the inhibition of receptor autophosphorylation, as well as MAPK phosphorylation, with IC 50 s of 0.3 and 0.22 μM, respectively, in Sal2 cells which express a CD8HER2 fusion protein. BMS-599626 Hydrochloride abrogates HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC 50 s in the range of 0.24 to 1 μM.In GEO cells, HER1 phosphorylation is stimulated by treatment with EGF and is inhibited by BMS-599626 Hydrochloride (IC 50 =0. 75 μM).There is also nearly complete inhibition of EGF-dependent MAPK (0. 8 μM) but only partial inhibition of AKT signaling.The latter likely reflects the activation of AKT by multiple upstream signals.Treatment of N87 cells with BMS-599626 Hydrochloride leads to the inhibition of HER2 (0. 38 μM), which is expressed to a high level because of gene amplification, as well as MAPK and AKT phosphorylation (0.35 μM for both). At the molecular level, in HN-5 cells the agent (BMS-599626 Hydrochloride) inhibits the expression of pEGFR, pHER2, cyclins D and E, pRb, pAkt, pMAPK, pCDK1 and 2, CDK 6, and Ku70 proteins. BMS-599626 Hydrochloride also induced accumulation of cells in the G1 cell cycle phase, inhibited cell growth, enhanced radiosensitivity, and prolonged the presence of γ-H AX foci up to 24 h after radiation. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.764 ml | 8.818 ml | 17.636 ml |
5 mM | 0.353 ml | 1.764 ml | 3.527 ml |
10 mM | 0.176 ml | 0.882 ml | 1.764 ml |
5 mM | 0.035 ml | 0.176 ml | 0.353 ml |
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