LY3009120

别名: DP-4978

LY03009120 (DP-4978)是一种有效的泛Raf抑制剂,在A375细胞中对A-raf,B-Raf,和 C-Raf的IC50分别为44 nM,31-47 nM,和 42 nM。LY03009120 可诱导自噬。Phase 1。

LY3009120 Chemical Structure

LY3009120 Chemical Structure

CAS: 1454682-72-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1466.01 现货
5mg 1207.33 现货
25mg 3906.82 现货
100mg 8154.89 现货
1g 24488.1 现货
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细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
HCT116 Function assay <100 nM Paradoxical activation of RAS/RAF/MEK signaling pathway in human HCT116 cells expressing wild type BRAF assessed as ERK phosphorylation at <100 nM 25965804
A375 Function assay 15 mins Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.042μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to ZAK in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.039μM. 25965804
A375 Function assay 72 hrs Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay, IC50=0.037μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.031μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to EphA2 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.02μM. 25965804
A375 Antiproliferative assay 72 hrs Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay, IC50=0.0092μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.044μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to p38 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.061μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to FYN in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.091μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to MAP3K1 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.098μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to EphB4 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.1μM. 25965804
HCT116 Antiproliferative assay 67 hrs Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay, IC50=0.22μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to CSK in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.29μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to SRC in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.31μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to ABL in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.38μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to IRAK1 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.39μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to GCN2 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.45μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to JNK in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.47μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to MAP2K5 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.8μM. 25965804
A375 Function assay 15 mins Competitive binding affinity to KHS1 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.97μM. 25965804
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells after 72 hrs by Cell-Titer Glo assay, IC50=0.1μM. 30529543
SK-MEL-2 Antiproliferative assay 72 hrs Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by Cell-Titer Glo assay, IC50=0.2μM. 30529543
A375 Antiproliferative assay 72 hrs Antiproliferative activity against human A375 cells after 72 hrs by Cell-Titer Glo assay, IC50=0.3μM. 30529543
SW579 Antiproliferative assay 72 hrs Antiproliferative activity against human SW579 cells after 72 hrs by Cell-Titer Glo assay, IC50=0.9μM. 30529543
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells after 72 hrs by Cell-Titer Glo assay, IC50=0.9μM. 30529543
HepG2 Antiproliferative assay 72 hrs Antiproliferative activity against human HepG2 cells after 72 hrs by Cell-Titer Glo assay, IC50=2.6μM. 30529543
HCT116 Function assay Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA, IC50=0.15μM. 25965804
A375 Function assay In vivo inhibition of BRAF V600E mutant in human A375 cells xenografted in po dosed NIH nude rat assessed as plasma concentration required to inhibit ERK phosphorylation by 50%, INH=0.165μM. 25965804
A375 Function assay Inhibition of desthiobiotin-ATP acylphosphate probe binding to B-Raf in human A375 cells by MS analysis, IC50=0.031μM. 30529543
A375 Function assay Inhibition of desthiobiotin-ATP acylphosphate probe binding to C-Raf in human A375 cells by MS analysis, IC50=0.042μM. 30529543
A375 Function assay Inhibition of desthiobiotin-ATP acylphosphate probe binding to A-Raf in human A375 cells by MS analysis, IC50=0.044μM. 30529543
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生物活性

产品描述 LY03009120 (DP-4978)是一种有效的泛Raf抑制剂,在A375细胞中对A-raf,B-Raf,和 C-Raf的IC50分别为44 nM,31-47 nM,和 42 nM。LY03009120 可诱导自噬。Phase 1。
靶点
C-Raf [1]
(Cell-free assay)
BRAF(V600E) [1]
(Cell-free assay)
BRAF WT [1]
(Cell-free assay)
4.3 nM 5.8 nM 15 nM
体外研究(In Vitro)
体外研究活性 LY3009120抑制A375和 HCT116细胞的生长,IC50分别为9.2和220 μM。LY3009120抑制酪氨酸激酶KDR,IC50为3.9 μM。[1]
激酶实验 使用KiNativ试验测定激酶活性
化合物在A375细胞裂解物中使用基于ATP的探针在5 µM下筛选。IC50值以微摩尔单位表示。细胞沉淀重悬浮在4体积裂解缓冲液[25 mM Tris pH 7.6,150 mM NaCl,1% CHAPS,1% Tergitol NP-40 型,1% v/v 磷酸酶抑制剂混合物II]中,使用尖端超声波仪声处理,并均质化。裂解产物通过100,000 g下离心分离30分钟除去。澄清的裂解液通过0.22 μM注射过滤器和凝胶过滤到反应缓冲液[20 mM Hepes pH 7.8,150 mM NaCl,0.1% triton X-100,1% v/v 磷酸酶抑制剂混合物II]。抑制剂处理和探针标记之前,将终浓度为20 mM 的MnCl2加入裂解液。用于IC50测定的终抑制剂浓度为10,1,0.1,和 0.01 μM。ATP竞争性实验在1,000,100,10,和1 μM ATP下进行。所有抑制剂的处理在室温下进行。
细胞实验 细胞系 A375 和 HCT116 细胞
浓度 0.51 μM
孵育时间 67 h
方法 简而言之,细胞在DMEM高浓度葡萄糖中生长,用10%胎牛血清和1%青霉素/链霉素/L-谷氨酰胺增补,在37℃,5% CO2,和95%湿度下培育。允许细胞扩增到70-95%的融合度。连续稀释的测试化合物分配加入到384孔黑色透明底板。每孔加入包含625个细胞的50 μL完全生长培养基。板在37℃,5% CO2,和95%湿度下培育67小时。然后,10 μL包含440 μM 刃天青的PBS溶液加入板的每孔中,板在37℃,5% CO2,和95%湿度下再培育5小时。板在Synergy2阅读器上使用540 nm激发波长和600 nm发射波长读取。得到的数据使用Prism软件分析以计算IC 50值。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-EGFR / EGFR / p-BRAF / BRAF / p-CRAF / CRAF / p-MEK / MEK / p-AKT / AKT Beclin-1 / Mcl-1 / LC3 / p62 27999210
体内研究(In Vivo)
体内研究活性 在负荷BRAF V600E ST019VR PDX肿瘤的大鼠体内,LY3009120 (15 or 30 mg/kg, p.o.)剂量依赖性抑制肿瘤生长。在负荷A375异种移植物的裸鼠体内,LY3009120 (3到50 mg/kg, p.o.)单剂量口服治疗剂量依赖性抑制磷酸-ERK,4.36 mg/kg剂量下抑制50%磷酸- ERK (EC50),68.9 ng/mL或165 nM血浆浓度下达到50%磷酸- ERK (EC50) 抑制率。[1]
动物实验 Animal Models 负荷BRAF V600E ST019VR PDX肿瘤的雌性 NIH裸鼠
Dosages 30 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02014116 Terminated
Neoplasms|Neoplasm Metastasis|Melanoma|Carcinoma Non-Small-Cell Lung|Colorectal Neoplasms
Eli Lilly and Company
November 26 2013 Phase 1

化学信息&溶解度

分子量 424.51 分子式

C23H29FN6O

CAS号 1454682-72-4 SDF Download LY3009120 SDF
Smiles CC1=CC(=C(C=C1C2=C(N=C3C(=C2)C=NC(=N3)NC)C)NC(=O)NCCC(C)(C)C)F
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 20 mg/mL ( (47.11 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
I am trying to figure out solubility of the drug LY3009120 Catalog #7842 for in vivo studies. I need some details on the formulation and how it is made to dissolve the chemical?

回答:
It can dissolve in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at 1 mg/ml clearly, and in 0.5% CMC Na at 30 mg/ml as a suspension.

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