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GNF-7

Catalog No. T3196 CAS 839706-07-9

Synonyms: GNF7, GNF 7

GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.

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GNF-7, CAS 839706-07-9

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Purity: 98%

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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 WT:133 nM, Bcr-Abl:61 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].

Synonyms	GNF7, GNF 7
Molecular Weight	547.542
Formula	C28H24F3N7O2
CAS No.	839706-07-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: <1 mg/mL

DMSO: 16 mg/mL (29.2 mM)

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Choi HG, et al. J Med Chem. 2010, 53(15), 5439-5448. 2. Nonami A, et al. Blood. 2015, 125(20), 3133-3143.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Anti-Cardiovascular Disease Compound Library TGF-beta/Smad Compound Library Neurotransmitter Receptor Compound Library Inhibitor Library Fluorochemical Library Kinase Inhibitor Library Cytoskeletal Signaling Pathway Compound Library Neuronal Signaling Compound Library Angiogenesis related Compound Library

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Keywords

GNF-7 839706-07-9 蛋白酪氨酸激酶神经科学细胞骨架血管生成 AChR ACK Bcr-Abl inhibit GNF7 Inhibitor leukemia T315I mutation chronic GNF 7 CML Ack1 myelogenous TNK2 Activated Cdc42 kinase 1 AML inhibitor

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