GNF 2
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.
GNF 2是一种高选择性的和非ATP竞争性的Bcr-Abl抑制剂,在多种细胞系中其IC50值为100-300 nM。
BCR-ABL基因由BCR和ABL基因融合而成[1]。BCR-ABL提高酪氨酸激酶的产生,在慢性髓细胞性白血病(CML)的发病中起重要作用[2]。
不同于竞争性抑制BCR-ABL激酶活性ATP结合位点的imatinib[3],GNF-2变构抑制(通过结合ABL的豆蔻酸结合位点[4])BCR-ABL阳性细胞的增殖并诱导细胞凋亡。在表达Bcr-abl的Ba/F3.p210细胞中,GNF-2处理48小时能够抑制细胞增殖,IC50值为138 nM [5]。此外,GNF-2能够抑制E255V和Y253H突变的Ba/F3细胞生长,IC50值分别为268 nM和194 nM [5]。GNF-2也会抑制K562和SUP-B15的生长,IC50值分别为273 nM和268 nM [5]。
注射表达BCR-ABL的Ba/F3-p210细胞能够诱导外周血中淋巴细胞减少4% [6]。
参考文献:
[1]. REDDY, K. S. & GROVE, B. 1998. A Philadelphia-Negative Chronic Myeloid Leukemia with a BCR/ABL Fusion Gene on Chromosome 9. Cancer Genetics and Cytogenetics, 107, 48-50.
[2]. RUMPOLD, H. & WEBERSINKE, G. 2011. Molecular pathogenesis of Philadelphia-positive chronic myeloid leukemia - is it all BCR-ABL Curr Cancer Drug Targets, 11, 3-19.
[3]. SEGGEWISS, R., LORE, K., GREINER, E., MAGNUSSON, M. K., PRICE, D. A., DOUEK, D. C., DUNBAR, C. E. & WIESTNER, A. 2005. Imatinib inhibits T-cell receptor-mediated T-cell proliferation and activation in a dose-dependent manner. Blood, 105, 2473-2479.
[4]. FABBRO, D., MANLEY, P. W., JAHNKE, W., LIEBETANZ, J., SZYTTENHOLM, A., FENDRICH, G., STRAUSS, A., ZHANG, J., GRAY, N. S., ADRIAN, F., WARMUTH, M., PELLE, X., GROTZFELD, R., BERST, F., MARZINZIK, A., COWAN-JACOB, S. W., FURET, P. & MESTAN, J. 2010. Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site. Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics, 1804, 454-462.
[5]. ADRIAN, F. J., DING, Q., SIM, T., VELENTZA, A., SLOAN, C., LIU, Y., ZHANG, G., HUR, W., DING, S., MANLEY, P., MESTAN, J., FABBRO, D. & GRAY, N. S. 2006. Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol, 2, 95-102.
[6]. ADRIAN, F. J., DING, Q., SIM, T., VELENTZA, A., SLOAN, C., LIU, Y., ZHANG, G., HUR, W., DING, S., MANLEY, P., MESTAN, J., FABBRO, D. & GRAY, N. S. 2006. Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol, 2, 95-102.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 374.32 |
Cas No. | 778270-11-4 |
Formula | C18H13F3N4O2 |
Solubility | insoluble in H2O; ≥18.7 mg/mL in DMSO; ≥9.8 mg/mL in EtOH with gentle warming |
Chemical Name | 3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide |
SDF | Download SDF |
Canonical SMILES | C1=CC(=CC(=C1)C(=O)N)C2=CC(=NC=N2)NC3=CC=C(C=C3)OC(F)(F)F |
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。 |
Description | GNF 2是一种高选择性的和非ATP竞争性的Bcr-Abl抑制剂。 | |||||
靶点 | Bcr-Abl | |||||
IC50 | 268 nM (SUP-B15 cell line) 273 nM (K562 cell line) |
质量控制和MSDS
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