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LY3009120

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产品编号 T6882Cas号 1454682-72-4
别名 DP-4978

LY3009120 (DP-4978) 是一种泛RAF 抑制剂,其抑制BRAFV600E、BRAFWT 和CRAFWT 的IC50分别为 5.8、9.1和15 nM。

LY3009120
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LY3009120

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纯度: 99.54%
产品编号 T6882 别名 DP-4978Cas号 1454682-72-4

LY3009120 (DP-4978) 是一种泛RAF 抑制剂,其抑制BRAFV600E、BRAFWT 和CRAFWT 的IC50分别为 5.8、9.1和15 nM。

规格价格库存数量
2 mg¥ 452现货
5 mg¥ 697现货
10 mg¥ 1,134现货
25 mg¥ 2,240现货
50 mg¥ 3,355现货
100 mg¥ 4,350现货
200 mg¥ 6,190现货
1 mL x 10 mM (in DMSO)¥ 736现货
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产品介绍

生物活性
产品描述
LY3009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. Phase 1.
靶点活性
B-Raf (V600E):5.8 nM, B-Raf (WT):15 nM, C-Raf:4.3 nM
体外活性
LY3009120抑制A375细胞和HCT116细胞的生长,其IC50分别为9.2 μM和220 μM。同时,LY3009120也对酪氨酸激酶KDR有抑制作用,其IC50为3.9 μM。[1]
体内活性
在携带BRAF V600E ST019VR PDX肿瘤的大鼠中,LY3009120 (15或30 mg/kg, p.o.)表现出剂量依赖性的肿瘤生长抑制效果。在裸鼠植入A375异种移植瘤中,单次口服LY3009120 (3到50 mg/kg, p.o.)显示出对磷酸化ERK的剂量依赖性抑制,其中抑制磷酸化ERK 50%所需剂量(EC50)为4.36 mg/kg,达到抑制磷酸化ERK 50%的血浆浓度(EC50)为68.9 ng/mL或165 nM。[1]
激酶实验
Kinase activity measurement using KiNativ assays: Compounds are screened in A375 cell lysates using the ATP-based probe at 5 μM. IC50 values are reported in micromolar units. Cell pellets are resuspended in four volumes of lysis buffer [25 mM Tris pH 7.6, 150 mM NaCl, 1% CHAPS, 1% Tergitol NP-40 type, 1% v/v phosphatase inhibitor cocktail II], sonicated using a tip sonicator, and dounce homogenized. Lysates are cleared by centrifugation at 100,000 g for 30 min. The cleared lysates are filtered through a 0.22 μM syringe filter, and gel filtered into reaction buffer [20 mM Hepes pH 7.8, 150 mM NaCl, 0.1% triton X-100, 1% v/v phosphatase inhibitor cocktail II]. MnCl2 is then added to the lysate to a final concentration of 20 mM prior to inhibitor treatment and probe labeling. Final inhibitor concentrations used for IC50 determinations are 10, 1, 0.1, and 0.01 μM. ATP competition experiments are performed at 1,000, 100, 10, and 1 μM ATP. All inhibitor treatments are performed at room temperature.
细胞实验
Brie?y, cells are grown in DMEM high glucose supplemented with 10% characterized fetal bovine serum and 1% penicillin/streptomycin/L -glutamine at 37℃, 5% CO2, and 95% humidity. Cells are allowed to expand until 70-95% con?uency. A serial dilution of test compound is dispensed into a 384-well black clear bottom plate. 625 cells are added per well in 50 μL of complete growth medium. Plates are incubated for 67 h at 37℃, 5% CO2 , and 95% humidity. Then, 10 μL of a 440 μM solution of resazurin in PBS is added to each well of the plate and plates are incubated for an additional 5 h at 37℃, 5% CO2, and 95% humidity. Plates are read on a Synergy2 reader using an excitation of 540 nm and an emission of 600 nm. Data are analyzed using Prism software to calculate IC 50 values.(Only for Reference)
动物实验
Animal Models: Female NIH nude rats bearing BRAF V600E ST019VR PDX tumorsFormulation: 20% cyclodextrin, 25 mM phosphate, pH2.0Dosages: 30 mg/kgAdministration: p.o.[1]
别名DP-4978
化学信息
分子量424.51
分子式C23H29FN6O
CAS No.1454682-72-4
SmilesCNc1ncc2cc(c(C)nc2n1)-c1cc(NC(=O)NCCC(C)(C)C)c(F)cc1C
密度no data available
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 10 mg/mL (23.56 mM)
溶液配制表
1mg5mg10mg50mg
1 mM2.3557 mL11.7783 mL23.5566 mL117.7829 mL
5 mM0.4711 mL2.3557 mL4.7113 mL23.5566 mL
10 mM0.2356 mL1.1778 mL2.3557 mL11.7783 mL
20 mM0.1178 mL0.5889 mL1.1778 mL5.8891 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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