BMS 599626 dihydrochloride
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 dihydrochloride是EGFR和ErbB2的强效选择性抑制剂,IC50值分别为22和32 nM[1].
表皮生长因子受体(EGFR)是表皮生长因子的细胞表面受体,在肿瘤侵袭和癌细胞增殖中起重要作用.受体酪氨酸蛋白激酶erbB-2(ErbB2)是人表皮生长因子受体,在乳腺癌中发挥关键作用.
BMS 599626 dihydrochloride是EGFR和ErbB2的有效选择性抑制剂.BMS-599626抑制HER4,IC50值为190 nM.在SAL2\N87和GEO肿瘤细胞中,BMS-599626以剂量依赖的方式抑制HER1和HER2的磷酸化和细胞增殖.在AU565乳腺癌细胞中,1 μM的BMS-599626抑制HER1/HER2异二聚体的形成[1].在形成HER1/HER2异二聚体的肿瘤细胞中,BMS-599626抑制异二聚体化[2].
在L2987人肺肿瘤异种移植模型中,60 mg/kg的BMS-599626以剂量依赖的方式抑制并延迟肿瘤生长[1].
参考文献：
[1]. Gavai AV, Fink BE, Fairfax DJ, et al. Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases. J Med Chem, 2009, 52(21): 6527-6530.
[2]. Wong TW, Lee FY, Yu C, 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): 6186-6193.
| Physical Appearance | White solid |
| Storage | Store at -20°C |
| M.Wt | 603.48 |
| Formula | C27H27FN8O3·2HCl |
| Solubility | Soluble in DMSO > 10 mM |
| Chemical Name | (E)-(S)-morpholin-3-ylmethyl hydrogen ((Z)-4-((1-(3-fluorobenzyl)-1H-indazol-5-yl)imino)-5-methyl-1,4-dihydropyrrolo[2,1-f][1,2,4]triazin-6-yl)carbonimidate dihydrochloride |
| SDF | Download SDF |
| Canonical SMILES | CC(C(/N=C(OC[C@]1([H])COCCN1)\O)=CN2NC=N/3)=C2C3=N\C4=CC=C5C(C=NN5CC6=CC(F)=CC=C6)=C4.Cl.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
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