GNF-7|839706-07-9|-陌孚医药/Medlife

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GNF-7

目录号: PL01794 纯度: ≥98%

CAS No. :839706-07-9

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中文名称	GNF-7
中文别名	GNF-7 抑制剂;N-[3-[1,4-二氢-1-甲基-7-[(6-甲基-3-吡啶基)氨基]-2-氧代嘧啶并[4,5-D]嘧啶-3(2H)-基]-4-甲基苯基]-3-(三氟甲基)苯甲酰胺
英文名称	GNF-7
英文别名	BenzaMide, N-[3-[1,4-dihydro-1-Methyl-7-[(6-Methyl-3-pyridinyl)aMino]-2-oxopyriMido[4,5-d]pyriMidin-3(2H)-yl]-4-Methylphenyl]-3-(trifluoroMethyl)-;BENZAMIDE, N-[3-[1,4-DIHYDRO-1-METHYL-7-[(6-METHYL-3-PYRIDINYL)AMINO]-2-OXOPYRIMIDO[4,5-D]PYRIMIDIN-3(2H)-YL]-4-METHYLP...;BenzaMide, N-[3-[1,4-dihydro-1-Methyl-7-[(6-Methyl-3-pyridinyl)aMino]-2-oxopyriMido[4,5-d]pyriMidin-3(2H)-yl]-4-Methylphenyl];GNF 7;GNF-7;N-[4-methyl-3-[1-methyl-7-[(6-methylpyridin-3-yl)amino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-3-yl]phenyl]-3-(trifluoromethyl)benzamide;N-(4-Methyl-3-(1-methyl-7-(6-methylpyridin-3-ylamino)-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)phenyl)-3-(trifluoromethyl)benzamide;N-[3-[1,4-Dihydro-1-methyl-7-[(6-methyl-3-pyridinyl)amino]-2-oxopyrimido[4,5-d]pyrimidin-3(2H)-yl]-4-methylphenyl]-3-(trifluoromethyl)-benzamide
Cas No.	839706-07-9
分子式	C₂₈H₂₄N₇O₂F₃
分子量	547.53
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	GNF-7 是一种多重激酶抑制剂。GNF-7 是 Bcr-Abl 的抑制剂，对 Bcr-Abl^WT 和 Bcr-Abl^T315I 作用的 IC₅₀ 值分别为 133 nM 和 61 nM。GNF-7 对 ACK1 和 GCK 也具有抑制活性，IC₅₀ 分别为 25 nM 和 8 nM。GNF-7 可用于血液恶性肿瘤的研究。
生物活性	GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC 50 s of 133 nM and 61 nM for Bcr-Abl and Bcr-Abl, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC 50 s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies.
性状	Solid
IC50 & Target[1][2]	IC50: 133 nM (Bcr-Abl), 61 nM (Bcr-Abl), 25 nM (ACK1), 8 nM (GCK)
体外研究(In Vitro)	GNF-7 potently inhibits wild-type Bcr-Abl (IC50<5 nM) and Bcr-Abl mutants such as T315I (IC50=11 nM), G250E (IC50<5 nM), E255V (IC50=10 nM), F317L (IC50<5 nM) and M351T (IC50<5 nM) in cellular assays. GNF-7 (1 μM; 2 hours) suppresses AKT/mTOR signaling and GCK downstream. GNF-7 (1 μM; 24 hours) induces of apoptosis and cell cycle arrest in NRAS mutant cell lines. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	GNF-7 (10-20 mg/kg; o.p.; daily; for 7 days) displays significant in vivo efficacy against T315I Bcr-Abl in the bioluminescent xenograft mouse model. GNF-7 exhibits moderate oral bioavailability (mice 36%) and C max (mice 3616 nM) following oral administration (mice 20 mg/kg). GNF-7 exhibits terminal elimination half-lives (mice 3.8 h) due to high plasma clearance (8.6 mL/min/kg) following intravenous injection (mice 5 mg/kg). 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]. Lu X, et al. Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3458-63. [2]. Choi HG, et al. A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. J Med Chem. 2010 Aug 12;53(15):5439-48.

溶解度数据	In Vitro: DMSO : ≥ 33 mg/mL (60.27 mM)配制储备液

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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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