Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 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 * 10 mM (in DMSO) | ¥ 736 | 现货 |
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 | C-Raf:4.3 nM, B-Raf (V600E):5.8 nM, B-Raf (WT):15 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 | In rats bearing BRAF V600E ST019VR PDX tumors, LY3009120 (15 or 30 mg/kg, p.o.) shows a dose-dependent tumor growth inhibition. In nude rats bearing A375 xenograft, single dose oral treatment with LY3009120 (3 to 50 mg/kg, p.o.) shows a dose dependent inhibition of phospho-ERK, with a dose for 50% inhibition of phospho-ERK (EC50) of 4.36 mg/kg, with plasma concentration to achieve 50% inhibition of phospho-ERK (EC50) of 68.9 ng/mL or 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 |
化合物与蛋白结合的复合物 |
CRYSTAL STRUCTURE OF BRAF(V600E) IN COMPLEX WITH LY3009120 COMPND |
分子量 | 424.51 |
分子式 | C23H29FN6O |
CAS No. | 1454682-72-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (23.56 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3557 mL | 11.7783 mL | 23.5566 mL | 58.8914 mL |
5 mM | 0.4711 mL | 2.3557 mL | 4.7113 mL | 11.7783 mL | |
10 mM | 0.2356 mL | 1.1778 mL | 2.3557 mL | 5.8891 mL | |
20 mM | 0.1178 mL | 0.5889 mL | 1.1778 mL | 2.9446 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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: 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 μL,一共给药动物10 只,您使用的配方为5% 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 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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