BMS-599626

BMS-599626

中文名称BMS-599626
中文同义词[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;HER1和HER2高效抑制剂(BMS-599626 HYDROCHLORIDE);BMS-599626 盐酸盐;化合物 T5390
英文名称BMS-599626
英文同义词[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;BMS-599626 (AC480);BMS-599626 (Hydrochloride);BMS-599626 HCl;AC480;BMS-599626 HCL;BMS599626;BMS 599626;AC-480;BMS-599626 hydrochloride (AC480;CS-173;AC480 HCl
CAS号873837-23-1
分子式C27H28ClFN8O3
分子量567.0144232
EINECS号
相关类别细胞生物学试剂
Mol文件873837-23-1.mol
结构式BMS-599626 结构式

BMS-599626 性质

储存条件Store at -20°C
溶解度DMSO 中≥29.05 mg/mL;不溶于乙醇;不溶于水
形态粉末

BMS-599626 用途与合成方法

BMS-599626 Hydrochloride (AC480 Hydrochloride) 是一种选择性的口服生物利用度 HER1 和 HER2 抑制剂,其 IC50 分别为 20和 30 nM。

BMS-599626 Hydrochloride 对 HER4 的 IC50 值为 190 nM,对 VEGFR2、c-Kit、Lck、MEK的抑制强度降低了 100 倍。BMS-599626 Hydrochloride 抑制肿瘤细胞增殖,并有可能增加肿瘤对放疗的反应。

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.

BMS-599626 Hydrochloride (60-240 mg/kg; p.o.; daily for 14 days) results in a dose-dependent inhibition of Sal2 tumor growth.
BMS-599626 Hydrochloride treatment results in the inhibition of GEO xenograft tumor growth when given once daily for 14 days. In addition to efficacy in the Sal2, GEO, and KPL4 models, BMS-599626 has similar antitumor activity in other HER2 amplified xenograft models including the BT474 breast and N87 gastric tumors, as well as other HER1-overexpressing non-small-cell lung tumors (A549 and L2987).
BMS-599626 Hydrochloride given before and during irradiation improved the radioresponse of HN5 tumors in vivo.

Animal Model: Athymic female nude mice ( nu/nu mice, Sal2 tumor model)
Dosage: 60, 120, 240 mg/kg
Administration: Oral; daily for 14 days
Result: Resulted in a dose-dependent inhibition of Sal2 tumor growth.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-12010BMS-599626
BMS-599626 Hydrochloride
873837-23-15mg837元
2024/01/25HY-12010BMS-599626
BMS-599626 Hydrochloride
873837-23-110mM * 1mLin DMSO1044元

BMS-599626 上下游产品信息

"BMS-599626"相关产品信息
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