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GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $37 | In Stock | |
5 mg | $87 | In Stock | |
10 mg | $147 | In Stock | |
25 mg | $297 | In Stock | |
50 mg | $463 | In Stock | |
100 mg | $739 | In Stock | |
1 mL x 10 mM (in DMSO) | $97 | In Stock |
Description | GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively. |
Targets&IC50 | BCR-ABL:61 nM, BCR-ABL (WT):133 nM |
In vitro | GNF-7 shows potent antiproliferative activity against wild-type and mutant Bcr-Abl Ba/F3 cells with IC50 less than 11 nM. In human colon cancer cells (Colo205 and SW620), GNF-7 also displays excellent growth inhibitory activity with IC50 of 5 nM and 1 nM, respectively. [1] GNF-7, potently and selectively inhibits NRAS-dependent acute myelogenous leukemia and acute lymphoblastic leukemia cells through combined inhibition of ACK1/AKT and GCK. [2] |
In vivo | GNF-7 exhibits excellent pharmacokinetic parameters in mice. In a bioluminescent xenograft mouse model using a transformed T315I-Bcr-Abl-Ba/F3 cell line, GNF-7 (10 mg/kg, p.o.) effectively inhibits tumor growth. [1] In NSG mice bearing human mutant NRAS-expressing MOLT-3-luc+ tumors, GNF-7 (15 mg/kg, p.o.) significantly decreases disease burden, prolongs overall survival, and causes strong suppression of phospho-AKT and phospho-RPS6. [2] |
Kinase Assay | For kinase assays, purified CDC5L(295-795)-His6 is mixed with [γ-32P]ATP, COS-7 cell extract, and incubated in 100 μL 20 mM HEPES, pH 7.5, 50 mM NaCl, 2 mM MnCl2, 10 mM MgCl2, 0.5% NP-40, 0.5 mM PMSF, 5 mM benzamidine hydrochloride, 5 mM NaF, 1 mM NaVO3 and the specific inhibitor at 30°C for 10 minutes. Cell extract as a source of kinase activity is prepared from subconfluent, serum-stimulated COS-7 cells lysed in 20 mM HEPES-NaOH, pH 7.5, 50 mM NaCl, 1% Triton X-100, 10% glycerol, protease and phosphotase inhibitors. Phosphorylated proteins are separated by electrophoresis in 15% polyacrylamide-SDS gels. Specific inhibitors included 20 μM staurosporine, 10 μM genistein, 1 μM CVT-313, 10 μM Rp-MB-cAMPS and 50 μM PD98059[1]. |
Alias | GNF7 |
Molecular Weight | 547.53 |
Formula | C28H24F3N7O2 |
Cas No. | 839706-07-9 |
Smiles | CN1C(=O)N(Cc2cnc(Nc3ccc(C)nc3)nc12)c1cc(NC(=O)c2cccc(c2)C(F)(F)F)ccc1C |
Relative Density. | 1.404 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 16 mg/mL (29.2 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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