GNF-5
目录号: PL04516 纯度: ≥99%
CAS No. :778277-15-9
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中文名称
GNF-5
中文别名
GNF-5 抑制剂;N-(2-羟基乙基)-3-[6-[[4-(三氟甲氧基)苯基]氨基]-4-嘧啶基]苯甲酰胺
英文名称
GNF-5
英文别名
N-(2-Hydroxyethyl)-3-(6-((4-(trifluoromethoxy)phenyl)amino)pyrimidin-4-yl)benzamide;GNF-5;GNF 5;N-(2-hydroxyethyl)-3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide;Benzamide, N-(2-hydroxyethyl)-3-(6-((4-(trifluoromethoxy)phenyl)amino)-4-pyrimidinyl)-;CHEBI:806423;CHEMBL1257423;N-(2-hydroxyethyl)-3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide;QC-4300;SureCN924071;UNII-3ZUA56XMQQ;GNF5;3ZUA56XMQQ;N-(2-Hydroxyethyl)-3-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]benzamide;N-(2-hydroxyethyl)-3-(6-{[4-(trifluoromethoxy)phenyl]amino}pyrimidin-4-yl)benzamide;IIQUYGWWHIHOCF-UHF
Cas No.
778277-15-9
分子式
C20H17F3N4O3
分子量
418.37
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GNF-5 是 GNF-2 的 n -羟乙基羧酰胺类似物,是一种 Bcr-Abl 抑制剂,具有口服活性。GNF-5 具有 Bcr-Abl 抑制活性,其 IC50 值为 0.22 μ M。GNF-5 具有良好的药代动力学特性。GNF-5 可用于多种癌症如慢性粒细胞白血病 (Chronic myelogenous leukemia, CML) 和乳腺癌的研究。
生物活性
GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC 50 value of 0.22 μM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer.
性状
Solid
IC50 & Target[1][2]
IC50: 0.22 μM (Abl)
体外研究(In Vitro)
GNF-5 has inhibition of wild-type Abl with an IC50 value of 0.22 μM but no inhibition for myristate site mutant E505K (IC50 >10 μM). has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
GNF-5 (5 mg/kg iv. or 20 mg/kg oral) has suitable pharmacokinetic parameters.
GNF-5 (oral, 50 or 100 mg/kg, twice daily, for 7 days) shows efficacious in vivo but can observe relapses.
GNF-5 (75 mg/kg, b.i.d) inhibits T315I Bcr-Abl combination with nilotinib in vivo. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Zhang J, et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 2010 Jan 28;463(7280):501-6.
[2]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183.
溶解度数据
In Vitro: DMSO : ≥ 49 mg/mL (117.12 mM)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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