GNF 2 (Synonyms: Bcr-Abl Inhibitor) |
カタログ番号GC10858
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GNF 2 は、Bcr-Abl の高度に選択的なアロステリック非 ATP 阻害剤です。 GNF 2 は Ba/F3.p210 の増殖を 138 nM の IC50 で阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 778270-11-4
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 778270-11-4 | SDF | |
| 同義語 | 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 |
| 溶解度 | ≥ 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6715 mL | 13.3576 mL | 26.7151 mL |
| 5 mM | 534.3 μL | 2.6715 mL | 5.343 mL |
| 10 mM | 267.2 μL | 1.3358 mL | 2.6715 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)