首页 工具
登录
购物车
LY3009120

LY3009120

产品编号 T6882   CAS 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。

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
LY3009120 Chemical Structure
LY3009120, CAS 1454682-72-4
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
产品目录号及名称: LY3009120 (T6882)
点击图片重新获取验证码
选择批次  
纯度: 99.54%
纯度: 99.54%
纯度: 99.08%
纯度: 98%
纯度: 96.96%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
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, BRAF(V600E):5.8 nM, BRAF WT:15 nM
体外活性 LY3009120 inhibits the cell growth of A375 and HCT116 cells with the IC50 of 9.2 and 220 μM, respectively. LY3009120 inhibits the tyrosine kinase KDR with the IC50 of 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

T6882_1

CRYSTAL STRUCTURE OF BRAF(V600E) IN COMPLEX WITH LY3009120 COMPND

分子量 424.51
分子式 C23H29FN6O
CAS No. 1454682-72-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 10 mg/mL (23.56 mM)

溶液配制表

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

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
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Henry JR, et al. J Med Chem. 2015, 58(10), 4165-4179. 2. Patricelli MP, et al. Chem Biol.2011, 18(6), 699-710.
Agerafenib Sorafenib-d3 Rineterkib GSK1904529A SB-590885 L-779450 BRAF inhibitor NSC-70220

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌药物库 抗癌临床化合物库 酪氨酸激酶分子库 经典已知活性库 临床期小分子药物库 NO PAINS 化合物库 HIF-1化合物库 抗前列腺癌化合物库 自噬库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

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: 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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步: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
计算 重置

技术支持

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。

Keywords

LY3009120 1454682-72-4 Autophagy MAPK Raf Raf kinases DP 4978 inhibit LY 3009120 LY-3009120 DP4978 DP-4978 Inhibitor inhibitor

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼