Crenolanib (CP-868596)

目录号:S2730 别名: ARO 002

Crenolanib (CP-868596) Chemical Structure

Molecular Weight(MW): 443.54

Crenolanib (CP-868596)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。

规格 价格 库存 购买数量  
RMB 1542.83 现货
RMB 1385.13 现货
RMB 2623.19 现货
RMB 7929.23 现货
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客户使用该产品的5个实验数据:

  • Clin Cancer Res 2013 19(24), 6935-42. Crenolanib (CP-868596) purchased from Selleck.

    Western blot analysis using 4G10 and anti-FLT3 antibody after immunoprecipitation with anti-FLT3 antibody and Western blot analysis of phospho-ERK (pERK) and ERK performed on whole cell lysates from HB119 and Molm14 cells. Cells were exposed to 100 nM crenolanib for 60 min.

    Proc Natl Acad Sci U S A 2014 111(14), 5319-24. Crenolanib (CP-868596) purchased from Selleck.

  • Concurrent treatment with Crenolanib and AG1478 enhances apoptosis as monitored by Caspase-3 and PARP-1 cleavage, either in GBM c-CSC or p-CSC, except for p-CSC3. Instead, Crenolanib alone is less effective in inducing apoptosis either in c-CSC or p-CSC pools. High PDGFR α expression is a distinctive feature of p-CSC pools and its expression is de-repressed following AG1478 treatment clearly evident in case 1 and 2, while its expression is downmodulated following Crenolanib treatment in all cases reported.

    Mol Cancer 2014 13(1), 247. Crenolanib (CP-868596) purchased from Selleck.

    Western blot analysis of CCSMC phenotype-related proteins, including α-SMA, desmin, vimentin, and collagen-I, after treatment with PDGF-BB at 20 ng/ml, Crenolanib at 100 nM. P <0.05 was considered statistically significant.

    PLoS One, 2017, 12(2):e0172191. Crenolanib (CP-868596) purchased from Selleck.

  • A549 cells were incubated with crenolanib (500 nM) for 48 hours. The nuclei were stained with Hoechst and analyzed using a fluorescent microscope. The representative images are shown. Red arrows indicate apoptotic cells with condensed or fragmented DNA.

    Onco Targets Ther 2014 7, 1761-8. Crenolanib (CP-868596) purchased from Selleck.

产品安全说明书

PDGFR抑制剂选择性比较

生物活性

产品描述 Crenolanib (CP-868596)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。
靶点
PDGFRα [1]
(CHO cells)
PDGFRβ [1]
(CHO cells)
2.1 nM(Kd) 3.2 nM(Kd)
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL60 NX\3b4dxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rtfWlEPTB;MdMxNE4xOyEQvF2= MVSyOVU6Pzd3NB?=
HL60/VCR MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;5TWM2OD14LkmzxtExNjB|IN88US=> NEW0SlAzPTV7N{e1OC=>
K562 NGG0cXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXTTmV5UUN3ME2xMlPDuTBwMEOg{txO MWiyOVU6Pzd3NB?=
K562/ABCB1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M36yO2lEPTB;ND62O:KyOC5yMTFOwG0> NXTMd2lvOjV3OUe3OVQ>
K562/ABCG2 MnXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDtTWM2OD1zLkW0xtExNjB|IN88US=> NXzIeoVNOjV3OUe3OVQ>
HL60 Mof2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTFwNEdCtVAvODRizszN M13oSVI2PTl5N{W0
HL60/ADR Mof3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTFwN{NCtVAvODZizszN NYq2Z41yOjV3OUe3OVQ>
HL60 NH7mS|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTBwOEdCtVAvODJizszN MX2yOVU6Pzd3NB?=
HL60+PSC-833 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrhWGV3UUN3ME2xMlMzyrFyLkC2JO69VQ>? Mk\0NlU2QTd5NUS=
HL60/VCR MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XJS2lEPTB;Nj6yO:KyOC5yMjFOwG0> MnL3NlU2QTd5NUS=
HL60/VCR+PSC-833 NH;US|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{myUmlEPTB;MD64OOKyOC5yNDFOwG0> MUCyOVU6Pzd3NB?=
K562 NVPRSXFJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonqTWM2OD1{LkCyxtExNjB3IN88US=> M2X4NFI2PTl5N{W0
K562+PSC-833 M{DvO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rtWWlEPTB;Mj6wNuKyOC5yODFOwG0> MkLzNlU2QTd5NUS=
K562/ABCB1 NG\BcIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTRwNEpCtVAvODRizszN M{izSFI2PTl5N{W0
K562/ABCB1+PSC-833 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV[xRXg2UUN3ME2yMlA3yrFyLkC4JO69VQ>? M2HFdFI2PTl5N{W0
A549  M1LVeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MViwMVExODBibl2= M3LHd|I1NzR6L{eyJIg> Moq2bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> NV;zc2lsOjV|Mki0NFk>
A549 MWLBdI9xfG:|aYOgRZN{[Xl? NVnxR5h[PTByIH7N M1;hc|Q5KGh? NFX4S3pqdmS3Y3XzJINmdGxiYYDvdJRwe2m| Mm\mNlU{Ojh2MEm=
A549 MU\GeY5kfGmxbjDBd5NigQ>? M1nYZVEzNjVxMkWvOVAhdk1? M{L3R|ExKGh? M{HVS4lvcGmkaYTzJINmdGxibXnndoF1cW:w M3rsfFI2OzJ6NEC5
M21 NV6zWGl5SXCxcITvd4l{KEG|c3H5 M{XNTlEh|ryP M4DQbFI1KGh? NGTGcohqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IIPp[45q\mmlYX70cJkh[2:vYnnu[YQhf2m2aDD2[Y12emGoZX7pZi=> NFfrd2czPDd|MkG3Ni=>
M21R NGL2TWRCeG:ydH;zbZMhSXO|YYm= MorSNUDPxE1? MVWyOEBp MnjibY5lfWOnczDj[YxtKGGyb4D0c5NqeyC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnXteZJi\mWwaXK= NX3BPVVjOjR5M{KxO|I>
TPF-10-741 NGPFeo1CeG:ydH;zbZMhSXO|YYm= Ml3CNUDPxE1? MnyzNlQhcA>? MYDpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4ZX31doFn\W6rYh?= NXTyZmV3OjR5M{KxO|I>
Ba/F3 ITD MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTFwMzFOwG0> NGXsd3UzPDJ{N{iyNC=>
Ba/F3 ITD/D835Y MnLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PmcWlEPTB;OD63JO69VQ>? MnnpNlQzOjd6MkC=
Ba/F3 WT D835Y M{XNO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXnN|RKSzVyPU[uPUDPxE1? MWiyOFIzPzh{MB?=
Ba/F3 WT D835F MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLqTWM2OD14LkWg{txO Mlq0NlQzOjd6MkC=
Ba/F3 WT D835H M1jvW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTF7Lkig{txO MVOyOFIzPzh{MB?=
Ba/F3 WT D835N MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnPSJQ4UUN3ME20MlMh|ryP NGjxbYgzPDJ{N{iyNC=>
Ba/F3 WT D835V MlfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn71TWM2OD1{LkOg{txO MXSyOFIzPzh{MB?=
Ba/F3 ITD/F691L MoLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoL5TWM2OD14Nz64JO69VQ>? NESzO40zPDJ{N{iyNC=>
MV4-11 NVH4Oo1KS2WubDDWbYFjdGm2eTDBd5NigQ>? M17qT|AuOSEQvF2= NHe4T2Q4OiCq NEHacnRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NUj6Xm9JOjRyNE[wNVQ>
MOLM-13 NVznWpdwS2WubDDWbYFjdGm2eTDBd5NigQ>? M4HOb|AuOSEQvF2= NEDX[2k4OiCq NIjGeY9qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M3;jdlI1ODR4MEG0
PL21 M2O4dWNmdGxiVnnhZoxqfHliQYPzZZk> NIHlN24xNTFyMDFOwG0> M1PaXFczKGh? Mmf5bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M3r4UlI1ODR4MEG0
OCI-AML3 NVy4cHIxS2WubDDWbYFjdGm2eTDBd5NigQ>? M1jrPFAuOTByIN88US=> MYe3NkBp NYnVVFNGcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NWnEcYd2OjRyNE[wNVQ>
THP-1 NE\4cnZE\WyuIG\pZYJtcXS7IFHzd4F6 MlTuNE0yODBizszN NXn6W2p1PzJiaB?= MWnpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MUWyOFA1PjBzNB?=
U937 MmDmR4VtdCCYaXHicIl1gSCDc4PhfS=> NH[zdGExNTFyMDFOwG0> Ml;PO|IhcA>? MV7pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NVrRRYpuOjRyNE[wNVQ>

... Click to View More Cell Line Experimental Data

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

+ 展开

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:

[1]

+ 展开
  • Cell lines: EOL-1 细胞系
  • Concentrations: 0-20 pM
  • Incubation Time: 72小时
  • Method: 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。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 88 mg/mL warmed (198.4 mM)
Ethanol 7 mg/mL (15.78 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 443.54
化学式

C26H29N5O2

CAS号 670220-88-9
稳定性 powder
in solvent
别名 ARO 002

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01522469 Completed Relapsed or Refractory Acute Myeloid Leukemia With FLT3 Activating Mutations Arog Pharmaceuticals Inc. July 2012 Phase 2
NCT01243346 Completed D842-related Mutant GIST Arog Pharmaceuticals Inc. April 2011 Phase 2
NCT01229644 Terminated Glioma Arog Pharmaceuticals Inc. April 2011 Phase 2
NCT00386555 Withdrawn Carcinoma Non-Small-Cell Lung Arog Pharmaceuticals Inc. May 2007 Phase 2
NCT00949624 Completed Advanced Solid Tumors Arog Pharmaceuticals Inc. December 2005 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID