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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5 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.

    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 M{[4emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPvTWM2OD1zwsGwMlA{KM7:TR?= MoDqNlU2QTd5NUS=
HL60/VCR NYT1TGNrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnWNmpvUUN3ME22Mlk{yrFyLkCzJO69VQ>? Mk\3NlU2QTd5NUS=
K562 MnPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVGyXlRYUUN3ME2xMlPDuTBwMEOg{txO MVyyOVU6Pzd3NB?=
K562/ABCB1 NGrpXIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DrNWlEPTB;ND62O:KyOC5yMTFOwG0> Mmm5NlU2QTd5NUS=
K562/ABCG2 NF31ZYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTtTWM2OD1zLkW0xtExNjB|IN88US=> NHnJOmQzPTV7N{e1OC=>
HL60 MoPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTvTWM2OD1zLkS2xtExNjB2IN88US=> NHHuWIgzPTV7N{e1OC=>
HL60/ADR NHG5d2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\4TJBKSzVyPUGuO|LDuTBwME[g{txO M37jUVI2PTl5N{W0
HL60 NWrSNIh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHKV|M2UUN3ME2wMlg3yrFyLkCyJO69VQ>? NYnnOYhvOjV3OUe3OVQ>
HL60+PSC-833 NVH0NYF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\XTWM2OD1zLkOyxtExNjB4IN88US=> NIPrR2EzPTV7N{e1OC=>
HL60/VCR M4jyb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPMd|FKSzVyPU[uNlfDuTBwMEKg{txO MUeyOVU6Pzd3NB?=
HL60/VCR+PSC-833 MnrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITDd2NKSzVyPUCuPFTDuTBwMESg{txO MojnNlU2QTd5NUS=
K562 M1X6fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXEfFlKSzVyPUKuNFLDuTBwMEWg{txO NHL2O4szPTV7N{e1OC=>
K562+PSC-833 M1;ZOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTJwMENCtVAvODhizszN NYPvcFF4OjV3OUe3OVQ>
K562/ABCB1 NYnJe2lnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfFTWM2OD12LkS5xtExNjB2IN88US=> M3PGRlI2PTl5N{W0
K562/ABCB1+PSC-833 NXfTS2hKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{WzXWlEPTB;Mj6wOuKyOC5yODFOwG0> NEe3OGozPTV7N{e1OC=>
A549  NInFUnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLEOmIxNTFyMECgcm0> MUOyOE81QC95MjDo NVXK[4hlcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? MXOyOVMzQDRyOR?=
A549 MVPBdI9xfG:|aYOgRZN{[Xl? MlTiOVAxKG6P NUD2SZdwPDhiaB?= MnrBbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MYKyOVMzQDRyOR?=
A549 M1fUUWZ2dmO2aX;uJGF{e2G7 M4TzSFEzNjVxMkWvOVAhdk1? NHTaOlMyOCCq NITBdnNqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= MoLaNlU{Ojh2MEm=
M21 NFHuWGVCeG:ydH;zbZMhSXO|YYm= NXK3O|BlOSEQvF2= NXviRYczOjRiaB?= NVPFdVZHcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigeoVufXKjZnXubYI> NILTbVUzPDd|MkG3Ni=>
M21R M3\vZWFxd3C2b4Ppd{BCe3OjeR?= MmLKNUDPxE1? MoPrNlQhcA>? NGqzT3FqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IIPp[45q\mmlYX70cJkh[2:vYnnu[YQhf2m2aDD2[Y12emGoZX7pZi=> NYrlXIlUOjR5M{KxO|I>
TPF-10-741 MVnBdI9xfG:|aYOgRZN{[Xl? NFG2VngyKM7:TR?= MmPDNlQhcA>? M3LnR4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\lcZVz[W[nbnni NGfFdHUzPDd|MkG3Ni=>
Ba/F3 ITD NGTFXYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnz4TWM2OD1zLkOg{txO MUGyOFIzPzh{MB?=
Ba/F3 ITD/D835Y M{jS[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7WcY5WUUN3ME24Mlch|ryP MWOyOFIzPzh{MB?=
Ba/F3 WT D835Y NUSyVZpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\6TI9KSzVyPU[uPUDPxE1? NIH4VW0zPDJ{N{iyNC=>
Ba/F3 WT D835F MnjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfremEzUUN3ME22MlUh|ryP NVTKfFlsOjR{Mke4NlA>
Ba/F3 WT D835H MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;XOYNEUUN3ME2xPU45KM7:TR?= M1fq[lI1OjJ5OEKw
Ba/F3 WT D835N MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTRwMzFOwG0> M4LCZVI1OjJ5OEKw
Ba/F3 WT D835V MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PaW2lEPTB;Mj6zJO69VQ>? MmLMNlQzOjd6MkC=
Ba/F3 ITD/F691L NGDHfHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1W1T2lEPTB;NkeuPEDPxE1? MVOyOFIzPzh{MB?=
MV4-11 M1;VPGNmdGxiVnnhZoxqfHliQYPzZZk> NVLYeZo4OC1zIN88US=> NHvBdJA4OiCq Ml:wbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MX[yOFA1PjBzNB?=
MOLM-13 MWHD[YxtKF[rYXLsbZR6KEG|c3H5 NFfTeo0xNTFizszN M2PwWlczKGh? MU\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NXHxWpVJOjRyNE[wNVQ>
PL21 Moi2R4VtdCCYaXHicIl1gSCDc4PhfS=> M2\IflAuOTByIN88US=> MYe3NkBp MXHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NYHvZZhKOjRyNE[wNVQ>
OCI-AML3 NVnHOGN5S2WubDDWbYFjdGm2eTDBd5NigQ>? MlHINE0yODBizszN NYS5c3g3PzJiaB?= NFPvVFBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NFnyXFQzPDB2NkCxOC=>
THP-1 NFvUbo5E\WyuIG\pZYJtcXS7IFHzd4F6 MnPINE0yODBizszN NGnXUlE4OiCq MnOxbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NV;adlBbOjRyNE[wNVQ>
U937 Mnn0R4VtdCCYaXHicIl1gSCDc4PhfS=> M{i5NFAuOTByIN88US=> MWi3NkBp NIfZeIZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MnjtNlQxPDZyMUS=

... 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:
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
Synonyms ARO 002

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID