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.

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In DMSO USD 190 In stock
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6 Customer Reviews

  • 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.

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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.
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/VCR M2TTW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGH3TG9KSzVyPU[uPVPDuTBwMEOg{txO M3\xelI2PTl5N{W0
K562 NH3xToNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7KTWM2OD1zLkRCtVAvODNizszN NInNeFAzPTV7N{e1OC=>
K562/ABCB1 NVO5OnlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\rd|lGUUN3ME20MlY4yrFyLkCxJO69VQ>? NWfYcINDOjV3OUe3OVQ>
K562/ABCG2 M1K5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrNU2dKSzVyPUGuOVTDuTBwMEOg{txO NFe2OWIzPTV7N{e1OC=>
HL60 NX3xcIxZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELsc5FKSzVyPUGuOFbDuTBwMESg{txO MljQNlU2QTd5NUS=
HL60 M3TpVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4noPWlEPTB;MD64OuKyOC5yMjFOwG0> MXqyOVU6Pzd3NB?=
HL60+PSC-833 NYnYb3g4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTFTWM2OD1zLkOyxtExNjB4IN88US=> MkDENlU2QTd5NUS=
HL60/VCR+PSC-833 MkHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzkbIFzUUN3ME2wMlg1yrFyLkC0JO69VQ>? MVuyOVU6Pzd3NB?=
K562 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTJwMENCtVAvODVizszN NFruUFgzPTV7N{e1OC=>
K562+PSC-833 NYjMdFF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWq1Wo96UUN3ME2yMlAzyrFyLkC4JO69VQ>? NXfLTWlFOjV3OUe3OVQ>
K562/ABCB1 NF20NWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPETWM2OD12LkS5xtExNjB2IN88US=> MnLDNlU2QTd5NUS=
K562/ABCB1+PSC-833 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLlWHBNUUN3ME2yMlA3yrFyLkC4JO69VQ>? MWCyOVU6Pzd3NB?=
A549  MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4C4S|AuOTByMDDuUS=> MV[yOE81QC95MjDo M1G4VolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> MoO5NlU{Ojh2MEm=
A549 M4LYNmFxd3C2b4Ppd{BCe3OjeR?= MYe1NFAhdk1? NF7yO441QCCq NHLMcJhqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NIniNlMzPTN{OESwPS=>
A549 NYL3THh2TnWwY4Tpc44hSXO|YYm= MoLJNVIvPS9{NT:1NEBvVQ>? Mn61NVAhcA>? MnyzbY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? MmP1NlU{Ojh2MEm=
M21 MnXsRZBweHSxc3nzJGF{e2G7 MWixJO69VQ>? M4T5dlI1KGh? NEnaXJNqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IIPp[45q\mmlYX70cJkh[2:vYnnu[YQhf2m2aDD2[Y12emGoZX7pZi=> MUGyOFc{OjF5Mh?=
M21R NIHzZnBCeG:ydH;zbZMhSXO|YYm= Ml;PNUDPxE1? M3LWeVI1KGh? M1TZPYlv\HWlZYOgZ4VtdCCjcH;weI9{cXNic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\lcZVz[W[nbnni MWWyOFc{OjF5Mh?=
TPF-10-741 M{D0bmFxd3C2b4Ppd{BCe3OjeR?= MVOxJO69VQ>? NUCyfJJ1OjRiaB?= NUnnO4xMcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigeoVufXKjZnXubYI> M4nY[VI1PzN{MUey
Ba/F3 ITD M1TwV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHuTWM2OD1zLkOg{txO MXqyOFIzPzh{MB?=
Ba/F3 ITD/D835Y M1q4eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vyRWlEPTB;OD63JO69VQ>? M1HxRlI1OjJ5OEKw
Ba/F3 WT D835Y M1rCNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvQTWM2OD14Lkmg{txO NEjOdHMzPDJ{N{iyNC=>
Ba/F3 WT D835F NGrye|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PxWWlEPTB;Nj61JO69VQ>? Mnf1NlQzOjd6MkC=
Ba/F3 WT D835H MnrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\5U5FFUUN3ME2xPU45KM7:TR?= NGPs[4szPDJ{N{iyNC=>
Ba/F3 WT D835N Mmj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHf5ZYJKSzVyPUSuN{DPxE1? M4\nXVI1OjJ5OEKw
Ba/F3 WT D835V NELaUWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33GeWlEPTB;Mj6zJO69VQ>? NUnOdlByOjR{Mke4NlA>
Ba/F3 ITD/F691L MnjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\kTWM2OD14Nz64JO69VQ>? M2LvO|I1OjJ5OEKw
MV4-11 M{P5[WNmdGxiVnnhZoxqfHliQYPzZZk> MVewMVEh|ryP M4DnOFczKGh? M2f3colvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NYLKVWtEOjRyNE[wNVQ>
MOLM-13 NUDncYF6S2WubDDWbYFjdGm2eTDBd5NigQ>? MlLjNE0yKM7:TR?= NHztXGg4OiCq M{X0bIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MnXENlQxPDZyMUS=
PL21 MWnD[YxtKF[rYXLsbZR6KEG|c3H5 NHHYTJgxNTFyMDFOwG0> NY\uRVBOPzJiaB?= MX;pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MmWzNlQxPDZyMUS=
OCI-AML3 MkCzR4VtdCCYaXHicIl1gSCDc4PhfS=> M13GRlAuOTByIN88US=> NX3sOHY2PzJiaB?= MlrkbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? Mm\RNlQxPDZyMUS=
THP-1 MYfD[YxtKF[rYXLsbZR6KEG|c3H5 M1P4PFAuOTByIN88US=> M2[xXVczKGh? M2\VfYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? Mmn0NlQxPDZyMUS=
U937 M2nlNGNmdGxiVnnhZoxqfHliQYPzZZk> M4D1elAuOTByIN88US=> M{fsSFczKGh? NIfX[JhqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 Mo[xNlQxPDZyMUS=

... Click to View More Cell Line Experimental Data


Kinase Assay:


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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:


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  • 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 88 mg/mL warmed (198.4 mM)
Ethanol 7 mg/mL (15.78 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* 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


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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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