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.

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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 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLENndKSzVyPUJCtVAvODNizszN M4f4XVI2PTl5N{W0
HL60/VCR NFj6c2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3QTWM2OD14LkmzxtExNjB|IN88US=> NIXIO2ozPTV7N{e1OC=>
K562 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:1WoFKSzVyPUGuN:KyOC5yMzFOwG0> MnewNlU2QTd5NUS=
K562/ABCB1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrrTYtKSzVyPUSuOlfDuTBwMEGg{txO NHHlWnozPTV7N{e1OC=>
K562/ABCG2 NXHRcmRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjJTWM2OD1zLkW0xtExNjB|IN88US=> MVeyOVU6Pzd3NB?=
HL60 NFKxPZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;HWowzUUN3ME2xMlQ3yrFyLkC0JO69VQ>? MnfiNlU2QTd5NUS=
HL60/ADR NYDDVZpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MliyTWM2OD1zLkeyxtExNjB4IN88US=> NFqwS20zPTV7N{e1OC=>
HL60 Mkn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7IeGpTUUN3ME2wMlg3yrFyLkCyJO69VQ>? MUeyOVU6Pzd3NB?=
HL60+PSC-833 M2LyXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTMTWM2OD1zLkOyxtExNjB4IN88US=> NHLZflEzPTV7N{e1OC=>
HL60/VCR Ml\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{T0d2lEPTB;Nj6yO:KyOC5yMjFOwG0> M4jMc|I2PTl5N{W0
HL60/VCR+PSC-833 MnH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXkfIZKSzVyPUCuPFTDuTBwMESg{txO NVv1VGtlOjV3OUe3OVQ>
K562 NWrOeHRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHWTWM2OD1{LkCyxtExNjB3IN88US=> NH7sT24zPTV7N{e1OC=>
K562+PSC-833 NV\1TJoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTCTWM2OD1{LkCyxtExNjB6IN88US=> NVXKRZdHOjV3OUe3OVQ>
K562/ABCB1 NX7zdHdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrPTWM2OD12LkS5xtExNjB2IN88US=> M3XkVlI2PTl5N{W0
K562/ABCB1+PSC-833 NEPTSoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTyUIRKSzVyPUKuNFbDuTBwMEig{txO MYGyOVU6Pzd3NB?=
A549  M2SyVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoC1NE0yODByIH7N MkP2NlQwPDhxN{KgbC=> M2\DTolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> MnHPNlU{Ojh2MEm=
A549 MUPBdI9xfG:|aYOgRZN{[Xl? NECyRo82ODBibl2= NE\I[Yw1QCCq NICyWWxqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NEfCO4czPTN{OESwPS=>
A549 NInwb49HfW6ldHnvckBCe3OjeR?= NGn0U4oyOi53L{K1M|UxKG6P M{HROVExKGh? MnTsbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? MVuyOVMzQDRyOR?=
M21 Ml:1RZBweHSxc3nzJGF{e2G7 NWrsVmxIOSEQvF2= NYPRW5ppOjRiaB?= NVHTVIFXcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigeoVufXKjZnXubYI> M1;R[FI1PzN{MUey
M21R M{[2XmFxd3C2b4Ppd{BCe3OjeR?= M2TrXVEh|ryP Ml;NNlQhcA>? MVvpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4ZX31doFn\W6rYh?= M1LQUVI1PzN{MUey
TPF-10-741 MkPCRZBweHSxc3nzJGF{e2G7 NHz3NnEyKM7:TR?= NVzWXop[OjRiaB?= MXjpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4ZX31doFn\W6rYh?= NYfzVYdUOjR5M{KxO|I>
Ba/F3 ITD NYrMZ5lxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWP5OopMUUN3ME2xMlMh|ryP MVmyOFIzPzh{MB?=
Ba/F3 ITD/D835Y NWHhdHpHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkD6TWM2OD16Lkeg{txO MnPJNlQzOjd6MkC=
Ba/F3 WT D835Y NU\6T3liT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTZwOTFOwG0> MlLLNlQzOjd6MkC=
Ba/F3 WT D835F M4rJc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;5[2lEPTB;Nj61JO69VQ>? NEDKVYszPDJ{N{iyNC=>
Ba/F3 WT D835H MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mln5TWM2OD1zOT64JO69VQ>? NGPqWJgzPDJ{N{iyNC=>
Ba/F3 WT D835N MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXVTGJKSzVyPUSuN{DPxE1? NEPGeGwzPDJ{N{iyNC=>
Ba/F3 WT D835V MoXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TpSWlEPTB;Mj6zJO69VQ>? M4LOPFI1OjJ5OEKw
Ba/F3 ITD/F691L NFn4SY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXK5[o5HUUN3ME22O{45KM7:TR?= NXr3RYJlOjR{Mke4NlA>
MV4-11 NIPmb4dE\WyuIG\pZYJtcXS7IFHzd4F6 NVjqZ4h4OC1zIN88US=> NIXCWGM4OiCq NWrVVldxcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVPUNZpTOjRyNE[wNVQ>
MOLM-13 MoPYR4VtdCCYaXHicIl1gSCDc4PhfS=> MUCwMVEh|ryP NWHyZVd{PzJiaB?= NEfs[mdqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MnXwNlQxPDZyMUS=
PL21 NYrncFRCS2WubDDWbYFjdGm2eTDBd5NigQ>? MXewMVExOCEQvF2= NEPTU|Y4OiCq NV2yUlNScW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NHHMVFgzPDB2NkCxOC=>
OCI-AML3 M4ewfmNmdGxiVnnhZoxqfHliQYPzZZk> NUH3e2lGOC1zMECg{txO MX63NkBp MUDpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MWWyOFA1PjBzNB?=
THP-1 NX:xeFVFS2WubDDWbYFjdGm2eTDBd5NigQ>? MYOwMVExOCEQvF2= MUe3NkBp MnvzbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NGrIWI8zPDB2NkCxOC=>
U937 M1PkU2NmdGxiVnnhZoxqfHliQYPzZZk> M1jWRVAuOTByIN88US=> NFzEZVg4OiCq NV\KZmpNcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M3n2cVI1ODR4MEG0

... 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 (200.65 mM) warming
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