GNF-7

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GNF-7

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

839706-07-9

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
5mg	电议
25mg	电议

产品介绍

GNF-7 是一种多激酶抑制剂。 GNF-7 是一种 Bcr-Abl 抑制剂，对 Bcr-AblWT 和 Bcr-AblT315I 的 IC50 分别为 133 nM 和 61 nM。 GNF-7 还具有对 ACK1（活化的 CDC42 激酶 1）和 GCK（生发中心激酶）的抑制活性，IC50 分别为 25 nM 和 8 nM。 GNF-7可用于血液系统恶性肿瘤的研究。

Cas No.	839706-07-9
化学名	(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
分子式	C₂₈H₂₄F₃N₇O₂
分子量	547.53
溶解度	≥ 5.48mg/mL in DMSO
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	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: [1].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. [2].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.