BMS-599626 Hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BMS-599626是一种选择性的HER1和HER2抑制剂,IC50值分别为22 nM和32 nM [1]。
HER(人表皮生长因子受体)是EGFR / ErbB家族的成员之一,并在细胞增殖和分化的转导中起重要作用。据报道,HER的异常表达与癌症有关联,HER抑制被认为是治疗癌症的一种有希望的策略[1]。
BMS-599626是一种强效的HER抑制剂,并且具有比报道的其他抑制剂更高的抑制能力。用HER1和HER2高表达的乳房肿瘤细胞系(HCC202、HCC1942和AU565)测试时,BMS-599626治疗抑制细胞增殖,而对无HER1或HER2表达的A2780细胞没有影响[1]。通过抑制HER,接受BMS-599626治疗的OV202细胞显著抑制细胞增殖并增强细胞凋亡[2]。用表达CD8-HER2融合蛋白的SAL2细胞测试时,BMS-599626治疗抑制受体的磷酸化和MAPK的磷酸化,IC50值分别为0.3和0.22 μM/L [1]。
在SAL2肿瘤细胞异种移植小鼠模型中,60 mg/kg浓度的BMS-599626口服给药剂量依赖性地抑制SAL2细胞生长并显著延迟肿瘤生长[1]。
参考文献:
[1]. Wong, T.W., et al., Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res, 2006. 12(20 Pt 1): p. 6186-93.
[2]. Haluska, P., et al., HER receptor signaling confers resistance to the insulin-like growth factor-I receptor inhibitor, BMS-536924. Mol Cancer Ther, 2008. 7(9): p. 2589-98.
Storage | Store at -20°C |
M.Wt | 567.01 |
Cas No. | 873837-23-1 |
Formula | C27H28ClFN8O3 |
Synonyms | AC480;BMS-599626 HCl;BMS599626;BMS 599626;AC-480 |
Solubility | ≥29.05 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | [(3S)-morpholin-3-yl]methyl N-[4-[[1-[(3-fluorophenyl)methyl]indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamate;hydrochloride |
SDF | Download SDF |
Canonical SMILES | CC1=C2C(=NC=NN2C=C1NC(=O)OCC3COCCN3)NC4=CC5=C(C=C4)N(N=C5)CC6=CC(=CC=C6)F.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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