Crenolanib

别名: CP-868596, ARO 002 中文名称:克莱拉尼

Crenolanib是一种有效的,选择性PDGFRα/β抑制剂,在CHO细胞中Kd为2.1 nM/3.2 nM,也能有效抑制FLT3,对D842V突变型敏感对V561D突变型不敏感,作用于PDGFR比作用于c-Kit,VEGFR-2,TIE-2,FGFR-2,EGFR,erbB2,和Src的选择性高100倍以上。Crenolanib可辅助诱导线粒体自噬。

Crenolanib Chemical Structure

Crenolanib Chemical Structure

CAS: 670220-88-9

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1542.83 现货
5mg RMB 1385.13 现货
10mg RMB 2623.19 现货
50mg RMB 7929.23 现货
1g RMB 32678.1 现货
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客户使用Selleck的Crenolanib发表文献92

产品质控

批次: 纯度: 99.99%
99.81

Crenolanib相关产品

相关信号通路图

PDGFR抑制剂选择性比较

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
A549 cells Cell viability assay 3.9-1000 nM 72 h a dose-dependent inhibition of cancer cell viability 25328409
MV4-11 Cytotoxicity assay 0.5 to 5000 nM 2 to 8 hrs Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability at 0.5 to 5000 nM incubated for 2 to 8 hrs followed by compound washout by CellTiter-Glo luminescent assay 30742435
MV4-11 Cytotoxicity assay 72 hrs Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay, IC50=0.012μM 30742435
MV4-11 Function assay a decrease in mitochondrial matrix protein aconitase hydratase 2 (ACO2) 25328409
MV4-11 Cytotoxicity assay Cytotoxicity against human MV4-11 cells expressing FLT3 ITD mutant, IC50=0.0015μM 31207462
MOLM13 Cytotoxicity assay Cytotoxicity against human MOLM13 cells expressing FLT3 ITD mutant, IC50=0.0049μM 31207462
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 Crenolanib是一种有效的,选择性PDGFRα/β抑制剂,在CHO细胞中Kd为2.1 nM/3.2 nM,也能有效抑制FLT3,对D842V突变型敏感对V561D突变型不敏感,作用于PDGFR比作用于c-Kit,VEGFR-2,TIE-2,FGFR-2,EGFR,erbB2,和Src的选择性高100倍以上。Crenolanib可辅助诱导线粒体自噬。
靶点
FLT3 [1]
(CHO cells)
PDGFRα [1]
(CHO cells)
PDGFRβ [1]
(CHO cells)
0.74 nM(Kd) 2.1 nM(Kd) 3.2 nM(Kd)
体外研究(In Vitro)
体外研究活性

Crenolanib显著比imatinib有效,能够抑制对imatinib耐药的PDGFRα激酶(D842I,D842V,D842Y,D1842-843IM,和缺失I843)活性。Crenolanib作用于同基因模型系统中D842V,比imatinib有效135倍,IC50大约为10 nM。Crenolanib抑制EOL-1细胞中融合致癌基因的激酶活性,其衍生自慢性噬酸细胞白血病患者,且表达持续活化的FIP1L1- PDGFRα融合激酶,IC50 = 21 nM。Crenolanib也会抑制EOL-1细胞的增殖,IC50 = 0.2 pM。Crenolanib抑制在BaF3细胞中表达的V561D或D842V突变激酶的活化,IC50分别为85 nM或272 nM。Crenolanib抑制H1703非小细胞肺癌细胞系中PDGFRα活化,其能够使包含PDGFRα基因座的4q12区域扩增24倍,IC50为26 nM。[1]

Crenolanib是一种口服具有生物活性的,高度有效的,选择性PDGFR TKI。Crenolanib是苯并咪唑化合物,对PDGFRA和PDGFRB的IC50s分别为0.9 nM和1.8 nM。[2]

激酶实验 PDGFRα激酶活性的生物化学评估
中国仓鼠卵巢(CHO)细胞用突变型或野生型PDGFRα瞬时转染,用不同浓度的Crenolanib处理。涉及重组DNA的实验使用2级生物安全条件,根据指南进行。制备来自细胞系的蛋白质裂解物,使用抗PDGFRα抗体进行免疫沉淀反应,然后用于PDGFRα的连续免疫印迹。使用Photoshop软件进行密度测定以量化药物作用,磷酸-PDGFRα的水平标归一化到总蛋白质。密度测定法和增殖实验结果使用Calcusyn 2.1软件分析,以精确测定IC50值。使用Wilcoxon Rank Sum Test比较Crenolanib对给定突变体的IC50值。
细胞实验 细胞系 EOL-1 细胞系
浓度 0-20 pM
孵育时间 72小时
方法

将细胞以20, 000细胞/孔的密度加入96孔板,与Crenolanib培育72小时,然后使用2,3-bis[2-甲氧基-4-硝基-5-磺苯基]-2H-四唑-5-羰基苯胺 (XTT)-试验测量细胞增殖。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot pAKT / AKT / pMAPK / MAPK / pSTAT5 / STAT5 pFLT3 / FLT3 / pERK / ERK / pS6 / S6 pKIT / KIT 24227820
Growth inhibition assay Cell viability 24623852
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00949624 Completed
Advanced Solid Tumors
Arog Pharmaceuticals Inc.
December 2005 Phase 1

化学信息&溶解度

分子量 443.54 分子式

C26H29N5O2

CAS号 670220-88-9 SDF Download Crenolanib SDF
Smiles CC1(COC1)COC2=CC3=C(C=C2)N(C=N3)C4=NC5=C(C=CC=C5N6CCC(CC6)N)C=C4
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 88 mg/mL ( 198.4 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 88 mg/mL

Water : 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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