Crenolanib (CP-868596)

Catalog No.S2730 Synonyms: ARO 002

Crenolanib (CP-868596) Chemical Structure

Molecular Weight(MW): 443.54

Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM in CHO cells, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock

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4 Customer Reviews

  • 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.

    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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM in CHO cells, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src.
Targets
PDGFRα [1]
(CHO cells)
PDGFRβ [1]
(CHO cells)
2.1 nM(Kd) 3.2 nM(Kd)
In vitro

Crenolanib is significantly more potent than imatinib in inhibiting the kinase activity of imatinib-resistant PDGFRα kinases (D842I, D842V, D842Y, D1842-843IM, and deletion I843). Crenolanib is 135-fold more otent than imatinib against D842V in the isogenic model system, with an IC50 of approximately 10 nM. Crenolanib inhibits the kinase activity of the fusion oncogene in EOL-1 cell line, which is derived from a patient with chronic eosinophilic leukemia and expresses the constitutively activated FIP1L1- PDGFRα fusion kinase, with IC50 = 21 nM. Crenolanib also inhibits the proliferation of EOL-1 cells with IC50 = 0.2 pM. Crenolanib inhibits the activation of V561D or D842V-mutant kinases expressed in BaF3 cells with IC50 with 85 nM or 272 nM, respectively. Crenolanib inhibits PDGFRα activation in H1703 non-small cell lung cancer cell line which has 24-fold amplification of the 4q12 region that contains the PDGFRα locus, with IC50 with 26 nM. [1] Crenolanib is an orally bioavailable, highly potent and selective PDGFR TKI. Crenolanib is a benzimidazole compound that has IC50s of 0.9 nM and 1.8 nM for PDGFRA and PDGFRB, respectively. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL60 NVLs[|hPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlu3TWM2OD1zwsGwMlA{KM7:TR?= MnfXNlU2QTd5NUS=
HL60/VCR MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXuPJpKSzVyPU[uPVPDuTBwMEOg{txO M{PKdVI2PTl5N{W0
K562 MkLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPUTWM2OD1zLkRCtVAvODNizszN MnPNNlU2QTd5NUS=
K562/ABCB1 NHGyZ4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDsNJlVUUN3ME20MlY4yrFyLkCxJO69VQ>? NHS2VJYzPTV7N{e1OC=>
K562/ABCG2 M3zIfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rDPGlEPTB;MT61OOKyOC5yMzFOwG0> MYiyOVU6Pzd3NB?=
HL60 M3TYV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\UTWM2OD1zLkS2xtExNjB2IN88US=> M3HCUVI2PTl5N{W0
HL60/ADR M{HqS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4P3WGlEPTB;MT63NuKyOC5yNjFOwG0> NGiyRXczPTV7N{e1OC=>
HL60 NYfBc|MxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfFSIlKSzVyPUCuPFbDuTBwMEKg{txO NGLUbVczPTV7N{e1OC=>
HL60+PSC-833 MlG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nEcGlEPTB;MT6zNuKyOC5yNjFOwG0> NFr3[XAzPTV7N{e1OC=>
HL60/VCR NVHHfmFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{ixNmlEPTB;Nj6yO:KyOC5yMjFOwG0> NW\lWXhLOjV3OUe3OVQ>
HL60/VCR+PSC-833 Mn3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwOEVCtVAvODRizszN MWKyOVU6Pzd3NB?=
K562 NWrMZYN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPsV5AxUUN3ME2yMlAzyrFyLkC1JO69VQ>? NInQWnozPTV7N{e1OC=>
K562+PSC-833 MlnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TTbGlEPTB;Mj6wNuKyOC5yODFOwG0> MXWyOVU6Pzd3NB?=
K562/ABCB1 NIW4PGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;E[pBKSzVyPUSuOFnDuTBwMESg{txO NFzGZ|MzPTV7N{e1OC=>
K562/ABCB1+PSC-833 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEC0d2VKSzVyPUKuNFbDuTBwMEig{txO MV2yOVU6Pzd3NB?=
A549  NFjDfZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{f6TlAuOTByMDDuUS=> M3LlZVI1NzR6L{eyJIg> NVfmeZhmcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? MWeyOVMzQDRyOR?=
A549 MUXBdI9xfG:|aYOgRZN{[Xl? NGr0NIE2ODBibl2= MYS0PEBp M33XZolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MYCyOVMzQDRyOR?=
A549 Mo\YSpVv[3Srb36gRZN{[Xl? MWmxNk42NzJ3L{WwJI5O MlrFNVAhcA>? NF74XXFqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= MV[yOVMzQDRyOR?=
M21 NV\IV5ZOSXCxcITvd4l{KEG|c3H5 NH7pdVMyKM7:TR?= MmHrNlQhcA>? NELQVFRqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IIPp[45q\mmlYX70cJkh[2:vYnnu[YQhf2m2aDD2[Y12emGoZX7pZi=> MlnaNlQ4OzJzN{K=
M21R MUTBdI9xfG:|aYOgRZN{[Xl? MX2xJO69VQ>? MXeyOEBp NWTYVlBucW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigeoVufXKjZnXubYI> NUfTRoxkOjR5M{KxO|I>
TPF-10-741 M4D4PGFxd3C2b4Ppd{BCe3OjeR?= NVqxTIk5OSEQvF2= NX\qWYV6OjRiaB?= MVvpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4ZX31doFn\W6rYh?= M1r4SFI1PzN{MUey
Ba/F3 ITD NILB[nVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTTTWM2OD1zLkOg{txO MVeyOFIzPzh{MB?=
Ba/F3 ITD/D835Y MnrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRThwNzFOwG0> M4TERlI1OjJ5OEKw
Ba/F3 WT D835Y M2jCfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTZwOTFOwG0> MUSyOFIzPzh{MB?=
Ba/F3 WT D835F MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3OweWlEPTB;Nj61JO69VQ>? NUXVNZBnOjR{Mke4NlA>
Ba/F3 WT D835H M2ntT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrvS49KSzVyPUG5Mlgh|ryP NV7TepFOOjR{Mke4NlA>
Ba/F3 WT D835N NHzrdnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3ONoRKSzVyPUSuN{DPxE1? MUSyOFIzPzh{MB?=
Ba/F3 WT D835V M3v6WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3vPFNKUUN3ME2yMlMh|ryP NY\IXZl4OjR{Mke4NlA>
Ba/F3 ITD/F691L NXTmTINrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfwTWM2OD14Nz64JO69VQ>? M4XTXFI1OjJ5OEKw
MV4-11 MXLD[YxtKF[rYXLsbZR6KEG|c3H5 NVjwN4l5OC1zIN88US=> NWrTdXp5PzJiaB?= NYL1[3lDcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NWHRW2h{OjRyNE[wNVQ>
MOLM-13 NVTXeYRMS2WubDDWbYFjdGm2eTDBd5NigQ>? NWTEUJJTOC1zIN88US=> NXL4c5AyPzJiaB?= NGP2bldqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 Ml7mNlQxPDZyMUS=
PL21 NUPFV284S2WubDDWbYFjdGm2eTDBd5NigQ>? MX2wMVExOCEQvF2= M1uwUlczKGh? NF6yOWRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NYr6XXJNOjRyNE[wNVQ>
OCI-AML3 NGi1WJNE\WyuIG\pZYJtcXS7IFHzd4F6 MXGwMVExOCEQvF2= NIWxN5E4OiCq MXrpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M2LhTFI1ODR4MEG0
THP-1 M2P5emNmdGxiVnnhZoxqfHliQYPzZZk> NVnJTlZTOC1zMECg{txO Ml\lO|IhcA>? MnL3bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MXOyOFA1PjBzNB?=
U937 NGPZNnlE\WyuIG\pZYJtcXS7IFHzd4F6 NETGZW8xNTFyMDFOwG0> MWe3NkBp NHnIOWZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M4ryb|I1ODR4MEG0

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:

[1]

+ Expand

Biochemical Assessment of PDGFRα Kinase Activity:

Chinese hamster ovary (CHO) cells are transiently transfected with mutated or wild type PDGFRα constructs and treated with various concentrations of Crenolanib. Experiments involving recombinant DNA are performed using biosafety level 2 conditions in accordance with guidelines. Protein lysates from cell lines are prepared and subjected to immunoprecipitation using anti-PDGFRα antibodies followed by sequential immunoblotting for PDGFRα. Densitometry is performed to quantify drug effect using Photoshop software, with the level of phosphor- PDGFRα normalized to total protein. Densitometry and proliferation experimental results are analyzed using Calcusyn 2.1 software to mathematically determine the IC50 values. The Wilcoxon Rank Sum Test is used to compare the IC50 values of Crenolanib for a given mutation.
Cell Research:

[1]

+ Expand
  • Cell lines: EOL-1 cell line
  • Concentrations: 0-20 pM
  • Incubation Time: 72 hours
  • Method:

    Cells are added to 96-well plates at densities of 20, 000 cells/well and incubated with Crenolanib for 72 hours before measuring cellular proliferation using a 2,3-bis[2-methoxyl-4-nitro-5-sulfophenyl]-2H-tetrazolium-5-carboxanilide (XTT)-based assay.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 89 mg/mL warmed (200.65 mM)
Ethanol 7 mg/mL (15.78 mM)
Water <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 443.54
Formula

C26H29N5O2

CAS No. 670220-88-9
Storage powder
in solvent
Synonyms ARO 002

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID