GNE-9815
目录号: PL10766 纯度: ≥98%
CAS No. :2729996-45-4
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中文名称
GNE-9815
英文名称
GNE-9815
英文别名
GNE9815;GNE-9815
Cas No.
2729996-45-4
分子式
C26H22FN5O2
分子量
455.48
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
GNE-9815 (化合物 7) 是一种高选择性的、具有较好口服生物利用度的泛型 RAF 抑制剂,其对 CRAF 和 BRAF 的 Ki 值分别为 0.062 和 0.19 nM。GNE-9815 联合 MEK 抑制剂 Cobimetinib (HY-13064) 显示出协同调节 MAPK 途径的作用。GNE-9815 可用于 KRAS 突变型癌症的研究。
生物活性
GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits K i values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers.
性状
Solid
IC50 & Target[1][2]
CRAF 0.062 nM (Ki) Braf 0.19 nM (Ki)
体外研究(In Vitro)
GNE-9815 shows synergistic activity in KRAS mutant A549 and HCT116 cancer cells in combination with the MEK inhibitor Cobimetinib. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GNE-9815 (15 mg/kg; p.o.; single) demonstrates synergistic MAPK pathway modulation when combines with the MEK inhibitor Cobimetinib in an HCT116 xenograft mouse model.
GNE-9815 (5 mg/kg; p.o.; single) shows good oral bioavailability and (1 mg/kg; i.v.; single) exhibits low blood clearance, moderate volume of distribution, and short half-life. 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;In solvent -80°C 6 months
参考文献
[1]. Huestis MP, et al. Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor. ACS Med Chem Lett. 2021 Apr 21;12(5):791-797.
溶解度数据
In Vitro: DMSO : 50 mg/mL (109.77 mM; ultrasonic and warming and heat to 80°C)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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