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GNF 2 (Synonyms: Bcr-Abl Inhibitor)

Catalog No.GC10858

Le GNF 2 est un inhibiteur compétitif hautement sélectif, allostérique, non ATP de Bcr-Abl. Le GNF 2 inhibe la prolifération de Ba/F3.p210 avec une IC50 de 138 nM .

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GNF 2 Chemical Structure

Cas No.: 778270-11-4

Taille Prix Stock Qté
10mM (in 1mL DMSO)
79,00 $US
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5mg
63,00 $US
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25mg
199,00 $US
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50mg
221,00 $US
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Sample solution is provided at 25 µL, 10mM.

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Background

GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 100 to 300 nM in various cell lines.
BCR-ABL gene is fused by the BCR and ABL1 genes [1]. BCR-ABL increased production of tyrosine kinase and played an essential role in the pathogenesis of chronic myelogenous leukemia (CML) [2].
Unlike imatinib® that competitively inhibited the ATP-binding site of BCR-ABL kinase activity [3], GNF-2 allosterically inhibited (through binding the myristate-binding site of ABL[4]) the proliferation of BCR-ABL positive cell and induces cell apoptosis.  In Ba/F3.p210 Bcr-abl–expressing cells, 48 h treatment of GNF-2 was able to inhibit the proliferation of cells with an IC50 value of 138 nM [5].  In addition, GNF-2 has been found to inhibit E255V and Y253H mutant Ba/F3 cells cell growth, with an IC50 value of 268 and 194 nM, respectively [5]. GNF-2 also caused growth inhibition of K562 and SUP-B15 with an IC50 value of 273 nM and 268 nM, respectively[5].
Injecting with BCR-ABL–expressing Ba/F3-p210 cells, 4 % lymphocytes reduction in eperipheral blood was induced [6].  
References:
[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.

Chemical Properties

Cas No. 778270-11-4 SDF
Synonymes Bcr-Abl Inhibitor
Chemical Name 3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide
Canonical SMILES C1=CC(=CC(=C1)C(=O)N)C2=CC(=NC=N2)NC3=CC=C(C=C3)OC(F)(F)F
Formula C18H13F3N4O2 M.Wt 374.32
Solubility ≥ 18.7mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.6715 mL 13.3576 mL 26.7151 mL
5 mM 0.5343 mL 2.6715 mL 5.343 mL
10 mM 0.2672 mL 1.3358 mL 2.6715 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 1 reference(s) in Google Scholar.)

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