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:

  • 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.

    Clin Cancer Res 2013 19(24), 6935-42. 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 MkjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXFTWM2OD1zwsGwMlA{KM7:TR?= M3nBfFI2PTl5N{W0
HL60/VCR MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjrSHlbUUN3ME22Mlk{yrFyLkCzJO69VQ>? M1\ET|I2PTl5N{W0
K562 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3EUY1OUUN3ME2xMlPDuTBwMEOg{txO NFO5TIwzPTV7N{e1OC=>
K562/ABCB1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7Xb4dvUUN3ME20MlY4yrFyLkCxJO69VQ>? NHHBXXozPTV7N{e1OC=>
K562/ABCG2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHr2d25KSzVyPUGuOVTDuTBwMEOg{txO MkTyNlU2QTd5NUS=
HL60 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYH0W5JvUUN3ME2xMlQ3yrFyLkC0JO69VQ>? NX;1XlhxOjV3OUe3OVQ>
HL60/ADR MkLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYP4bIZJUUN3ME2xMlczyrFyLkC2JO69VQ>? MU[yOVU6Pzd3NB?=
HL60 M3[ze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1f5NmlEPTB;MD64OuKyOC5yMjFOwG0> MnvXNlU2QTd5NUS=
HL60+PSC-833 NHKxTppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXETpY3UUN3ME2xMlMzyrFyLkC2JO69VQ>? NFP4VYgzPTV7N{e1OC=>
HL60/VCR MlHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTZwMkhCtVAvODJizszN Mn;WNlU2QTd5NUS=
HL60/VCR+PSC-833 M133O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPRdohwUUN3ME2wMlg1yrFyLkC0JO69VQ>? Ml65NlU2QTd5NUS=
K562 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;kUmlEPTB;Mj6wNuKyOC5yNTFOwG0> NXy3dVF{OjV3OUe3OVQ>
K562+PSC-833 NWDx[2dkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTJwMENCtVAvODhizszN MUeyOVU6Pzd3NB?=
K562/ABCB1 NHrjeVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moe1TWM2OD12LkS5xtExNjB2IN88US=> NXnOWXFbOjV3OUe3OVQ>
K562/ABCB1+PSC-833 Mlm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\tTWM2OD1{LkC2xtExNjB6IN88US=> MmrmNlU2QTd5NUS=
A549  NYfqdnZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDzVZUxNTFyMECgcm0> M3XMbVI1NzR6L{eyJIg> NVzmcVFHcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? M1flc|I2OzJ6NEC5
A549 M2XqZ2Fxd3C2b4Ppd{BCe3OjeR?= MYe1NFAhdk1? MUi0PEBp M3nxb4lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NFzUfIYzPTN{OESwPS=>
A549 MojBSpVv[3Srb36gRZN{[Xl? Mm[zNVIvPS9{NT:1NEBvVQ>? NFSzV3QyOCCq NV73ZmpDcW6qaXLpeJMh[2WubDDtbYdz[XSrb36= MWWyOVMzQDRyOR?=
M21 NVn3UHM2SXCxcITvd4l{KEG|c3H5 NUTOVZpoOSEQvF2= MVKyOEBp NHHOTWNqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IIPp[45q\mmlYX70cJkh[2:vYnnu[YQhf2m2aDD2[Y12emGoZX7pZi=> MWeyOFc{OjF5Mh?=
M21R MX;BdI9xfG:|aYOgRZN{[Xl? MlLSNUDPxE1? M1\0PFI1KGh? MXHpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4ZX31doFn\W6rYh?= MX:yOFc{OjF5Mh?=
TPF-10-741 M3HzXGFxd3C2b4Ppd{BCe3OjeR?= NXPSN2V1OSEQvF2= MmXtNlQhcA>? MYPpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4ZX31doFn\W6rYh?= M3H2U|I1PzN{MUey
Ba/F3 ITD NWjRSYh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LZ[GlEPTB;MT6zJO69VQ>? M{fRb|I1OjJ5OEKw
Ba/F3 ITD/D835Y MoDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\ybmlEPTB;OD63JO69VQ>? M3ztcFI1OjJ5OEKw
Ba/F3 WT D835Y M4q4VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\NTYtKSzVyPU[uPUDPxE1? Mor2NlQzOjd6MkC=
Ba/F3 WT D835F MnzYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DQRWlEPTB;Nj61JO69VQ>? NXzm[GM6OjR{Mke4NlA>
Ba/F3 WT D835H M4DLOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfOTWM2OD1zOT64JO69VQ>? M3rKVFI1OjJ5OEKw
Ba/F3 WT D835N M2\NZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGiwb5ZKSzVyPUSuN{DPxE1? NFTEeGEzPDJ{N{iyNC=>
Ba/F3 WT D835V M2XPNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTJwMzFOwG0> NGDDbHAzPDJ{N{iyNC=>
Ba/F3 ITD/F691L MmjpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHRe|c4UUN3ME22O{45KM7:TR?= M3vCeFI1OjJ5OEKw
MV4-11 MnLoR4VtdCCYaXHicIl1gSCDc4PhfS=> MVqwMVEh|ryP M1fENlczKGh? NWHGRVFycW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NEHHOZEzPDB2NkCxOC=>
MOLM-13 MlTXR4VtdCCYaXHicIl1gSCDc4PhfS=> NWnxOoxNOC1zIN88US=> NIrJOIg4OiCq NGr4bJNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NYTudnlkOjRyNE[wNVQ>
PL21 NWe2Rm91S2WubDDWbYFjdGm2eTDBd5NigQ>? NX3yfZZ4OC1zMECg{txO NV7YcFljPzJiaB?= NXHhWWhHcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NI\4N|AzPDB2NkCxOC=>
OCI-AML3 M3u1dmNmdGxiVnnhZoxqfHliQYPzZZk> NGHZNo0xNTFyMDFOwG0> M2PLV|czKGh? M2HPeIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MmLxNlQxPDZyMUS=
THP-1 MWDD[YxtKF[rYXLsbZR6KEG|c3H5 MXSwMVExOCEQvF2= M{T4dVczKGh? NETGNZFqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MmKxNlQxPDZyMUS=
U937 MonQR4VtdCCYaXHicIl1gSCDc4PhfS=> NFjQdZExNTFyMDFOwG0> M4fHSlczKGh? M2LUdIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NEi0ToIzPDB2NkCxOC=>

... 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 从左到右依次加入纯溶剂:
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
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID