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GNF-7

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

Catalog No. T3196Cas No. 839706-07-9

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Purity:99.47%

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COA HNMR HPLC

GNF-7

Catalog No. T3196Cas No. 839706-07-9

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

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Pack Size	Price	Availability
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

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Product Introduction

Bioactivity

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

Chemical Properties

Molecular Weight	547.53
Formula	C₂₈H₂₄F₃N₇O₂
Cas No.	839706-07-9

Storage & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	1.8264 mL	9.1319 mL	18.2638 mL	91.3192 mL
5 mM	0.3653 mL	1.8264 mL	3.6528 mL	18.2638 mL
10 mM	0.1826 mL	0.9132 mL	1.8264 mL	9.1319 mL
20 mM	0.0913 mL	0.4566 mL	0.9132 mL	4.5660 mL

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