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GNF-7Type II Bcr-Abl inhibitor

GNF-7

Catalog No. B6033
Size Price Stock Qty
5mg $105.00 In stock
25mg $350.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 839706-07-9 SDF Download SDF
Chemical Name (Z)-N-(4-methyl-3-(1-methyl-7-((6-methylpyridin-3-yl)amino)-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)phenyl)-3-(trifluoromethyl)benzimidic acid
Canonical SMILES CC1=C(N(C2=O)CC(C(N2C)=N3)=CN=C3NC4=CN=C(C=C4)C)C=C(/N=C(O)/C5=CC(C(F)(F)F)=CC=C5)C=C1
Formula C28H24F3N7O2 M.Wt 547.53
Solubility Soluble in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

IC50:The IC50 of GNF-7is 0.005, 0.001, and 0.008 µM in Colo205, SW620, and TrkC-Ba/F3 cells, respectively.

GNF-7 is the type-II inhibitor of T315I-Bcr-Abl [1]. BCR-ABL, constitutively activated tyrosine kinase, is an oncogene associated with chronic myelogenous leukemia (CML) and some cases ofacute lymphocytic leukemia in humans.

In vitro:GNF-7 showed excellent growth inhibitory activity against some human cancer cells. The IC50 of GNF-7is 0.005, 0.001, and 0.008 µM when tested in Colo205, SW620, and TrkC-Ba/F3 cell line, respectively.GNF-7 showed little effect on HEK293T cells, a normal cell line [1].After treated for 24h (7.5mg/kg QD or 15 mg/kg QD), GNF-7 significantly decreaseddisease burden in mice and prolonged overall survival compared to vehicle-controls [2].

In vivo:In acute myelogenous leukemia and lymphoblastic leukemia models, GNF-7 potently and selectively inhibited NRAS-dependent cells [2]. In theT315I-Bcr-Abl-Ba/F3 cell line bioluminescent xenograft mouse model,oral administration of GNF-7 with 10or20mg/kgexhibited significant efficacy against T315I-Bcr-Abl without appreciable toxicity [1].

References:
Choi H G, Ren P, Adrian F, et al.  A type-II kinase inhibitor capable of inhibiting the T315I “gatekeeper” mutant of Bcr-Abl[J]. Journal of medicinal chemistry, 2010, 53(15): 5439-5448.
Nonami A, Sattler M, Weisberg E, et al.  Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach[J]. Blood, 2015, 125(20): 3133-3143.