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
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用该产品的6个实验数据:

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

    NSG mice were inoculated with 1x106 MOLM-13 cells (ffluc+GFP+662 ) and on day 7 were treated with 5x106 FLT3-CAR T-cells alone (CD4+:CD8+ ratio = 1:1), crenolanib alone (15mg/kg body weight as i.p. injection), or both (combination), or were left untreated. The first dose of crenolanib was given on day 7 and mice received 15 doses (Monday-Friday) for 3 consecutive weeks. (a) Serial bioluminesence (BL) imaging to assess leukemia progression/regression in each treatment group.

    Leukemia, 2018, 32(5):1168-1179. 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 MnfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPYOGhKSzVyPUJCtVAvODNizszN MmjINlU2QTd5NUS=
HL60/VCR NXrWU3Y4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzMNJNKSzVyPU[uPVPDuTBwMEOg{txO MWmyOVU6Pzd3NB?=
K562 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDGOnhKSzVyPUGuN:KyOC5yMzFOwG0> MmDVNlU2QTd5NUS=
K562/ABCB1 M1f0W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4n2O2lEPTB;ND62O:KyOC5yMTFOwG0> NUjKVW1uOjV3OUe3OVQ>
K562/ABCG2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfYdZBKSzVyPUGuOVTDuTBwMEOg{txO NFXjZ2wzPTV7N{e1OC=>
HL60 NFHFWXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3zTWM2OD1zLkS2xtExNjB2IN88US=> M2TGNVI2PTl5N{W0
HL60/ADR NIfONI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfrUVBKSzVyPUGuO|LDuTBwME[g{txO Mnn1NlU2QTd5NUS=
HL60 MoD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwOEdCtVAvODJizszN M33LZVI2PTl5N{W0
HL60+PSC-833 M2LqPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoC1TWM2OD1zLkOyxtExNjB4IN88US=> NYPSfXRlOjV3OUe3OVQ>
HL60/VCR MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPjNnBKSzVyPU[uNlfDuTBwMEKg{txO NU\JUmtbOjV3OUe3OVQ>
HL60/VCR+PSC-833 Mn60S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwOEVCtVAvODRizszN MnrlNlU2QTd5NUS=
K562 M4n6fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLXbnlKSzVyPUKuNFLDuTBwMEWg{txO MmPTNlU2QTd5NUS=
K562+PSC-833 NGXpZmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjk[IJKSzVyPUKuNFLDuTBwMEig{txO M2f5RVI2PTl5N{W0
K562/ABCB1 NFXXUGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILuN4pKSzVyPUSuOFnDuTBwMESg{txO NX\5[lk{OjV3OUe3OVQ>
K562/ABCB1+PSC-833 NHP1VldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\HPIxEUUN3ME2yMlA3yrFyLkC4JO69VQ>? NX3BVIwyOjV3OUe3OVQ>
A549  Mon3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrQNE0yODByIH7N M{PTdVI1NzR6L{eyJIg> NIPkWHZqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MX:yOVMzQDRyOR?=
A549 M4PQXGFxd3C2b4Ppd{BCe3OjeR?= NYXSbFhpPTByIH7N Mn3XOFghcA>? NX7rWVBqcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= M4i1[|I2OzJ6NEC5
A549 MVfGeY5kfGmxbjDBd5NigQ>? NYTCWYdFOTJwNT:yOU82OCCwTR?= MoXKNVAhcA>? MofkbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? MkHQNlU{Ojh2MEm=
M21 NIj2OVRCeG:ydH;zbZMhSXO|YYm= MnPwNUDPxE1? M37JVFI1KGh? MoHJbY5lfWOnczDj[YxtKGGyb4D0c5NqeyC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnXteZJi\mWwaXK= M2\wZ|I1PzN{MUey
M21R Mk\qRZBweHSxc3nzJGF{e2G7 MVuxJO69VQ>? MUGyOEBp MknVbY5lfWOnczDj[YxtKGGyb4D0c5NqeyC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnXteZJi\mWwaXK= M2rDNlI1PzN{MUey
TPF-10-741 MWTBdI9xfG:|aYOgRZN{[Xl? NVzOcXJbOSEQvF2= NXjmbmZ3OjRiaB?= M4fZNolv\HWlZYOgZ4VtdCCjcH;weI9{cXNic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\lcZVz[W[nbnni NWj5eZNXOjR5M{KxO|I>
Ba/F3 ITD NFnMdI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fFbmlEPTB;MT6zJO69VQ>? M{DEXlI1OjJ5OEKw
Ba/F3 ITD/D835Y NEHuPIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXLTWM2OD16Lkeg{txO M1;MUFI1OjJ5OEKw
Ba/F3 WT D835Y Mn\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTZwOTFOwG0> NHzBT2QzPDJ{N{iyNC=>
Ba/F3 WT D835F NGq3bWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfwU3dKSzVyPU[uOUDPxE1? NX25VmY4OjR{Mke4NlA>
Ba/F3 WT D835H NHXZeZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37MNGlEPTB;MUmuPEDPxE1? MWWyOFIzPzh{MB?=
Ba/F3 WT D835N NXjSN|VXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTRwMzFOwG0> NEfJXG8zPDJ{N{iyNC=>
Ba/F3 WT D835V MoXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTJwMzFOwG0> NXTPU4FFOjR{Mke4NlA>
Ba/F3 ITD/F691L Mn3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFeyXYhKSzVyPU[3Mlgh|ryP M3rtdlI1OjJ5OEKw
MV4-11 MWrD[YxtKF[rYXLsbZR6KEG|c3H5 NEnMeZExNTFizszN NIjrZmw4OiCq M3zEN4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M3rIV|I1ODR4MEG0
MOLM-13 NW[4WZNyS2WubDDWbYFjdGm2eTDBd5NigQ>? NFS3e4ExNTFizszN NIDzUXk4OiCq MlLlbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M{W3S|I1ODR4MEG0
PL21 NI\BdIpE\WyuIG\pZYJtcXS7IFHzd4F6 MVGwMVExOCEQvF2= M{LNc|czKGh? MUHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NXXUTm9MOjRyNE[wNVQ>
OCI-AML3 NYDVOm1GS2WubDDWbYFjdGm2eTDBd5NigQ>? NXfsRmFpOC1zMECg{txO MlXsO|IhcA>? NFK2NYlqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M2foe|I1ODR4MEG0
THP-1 NYHjbmFkS2WubDDWbYFjdGm2eTDBd5NigQ>? NYKzfGxLOC1zMECg{txO NWPFRoFFPzJiaB?= NULsOZBkcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVTh[W44OjRyNE[wNVQ>
U937 MVvD[YxtKF[rYXLsbZR6KEG|c3H5 NEnzeG4xNTFyMDFOwG0> MlzUO|IhcA>? MnG0bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MkHBNlQxPDZyMUS=

... 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
NCT00949624 Completed Advanced Solid Tumors Arog Pharmaceuticals Inc. December 2005 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

PDGFR Signaling Pathway Map

PDGFR Inhibitors with Unique Features

相关PDGFR产品

Tags: 购买Crenolanib (CP-868596) | Crenolanib (CP-868596)供应商 | 采购Crenolanib (CP-868596) | Crenolanib (CP-868596)价格 | Crenolanib (CP-868596)生产 | 订购Crenolanib (CP-868596) | Crenolanib (CP-868596)代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID