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.
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 MlGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonWTWM2OD1zwsGwMlA{KM7:TR?= Mn\jNlU2QTd5NUS=
HL60/VCR M3HicGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjDNopUUUN3ME22Mlk{yrFyLkCzJO69VQ>? NWq5OpRTOjV3OUe3OVQ>
K562 MlfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTFwM9MxNE4xOyEQvF2= NX62WGFyOjV3OUe3OVQ>
K562/ABCB1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;2TWlEPTB;ND62O:KyOC5yMTFOwG0> NXP1WYdvOjV3OUe3OVQ>
K562/ABCG2 M3nqfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLiTWM2OD1zLkW0xtExNjB|IN88US=> MkL5NlU2QTd5NUS=
HL60 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nMXGlEPTB;MT60OuKyOC5yNDFOwG0> MnmwNlU2QTd5NUS=
HL60/ADR MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETqcIlKSzVyPUGuO|LDuTBwME[g{txO M1jLdVI2PTl5N{W0
HL60 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoizTWM2OD1yLki2xtExNjB{IN88US=> M2P2R|I2PTl5N{W0
HL60+PSC-833 MmjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XBPGlEPTB;MT6zNuKyOC5yNjFOwG0> MUmyOVU6Pzd3NB?=
HL60/VCR MnH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HHSmlEPTB;Nj6yO:KyOC5yMjFOwG0> NYHPSJZIOjV3OUe3OVQ>
HL60/VCR+PSC-833 M2PNcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnv4TWM2OD1yLki0xtExNjB2IN88US=> NHrU[2szPTV7N{e1OC=>
K562 NFnvVlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTRTWM2OD1{LkCyxtExNjB3IN88US=> NVfqTZVDOjV3OUe3OVQ>
K562+PSC-833 MnvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIna[GtKSzVyPUKuNFLDuTBwMEig{txO NICxNGQzPTV7N{e1OC=>
K562/ABCB1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXL0dGdrUUN3ME20MlQ6yrFyLkC0JO69VQ>? M2HCXFI2PTl5N{W0
K562/ABCB1+PSC-833 MmL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPPcXdyUUN3ME2yMlA3yrFyLkC4JO69VQ>? M4D1SlI2PTl5N{W0
A549  MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWGwMVExODBibl2= MYWyOE81QC95MjDo NIfnUYVqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 Mlz3NlU{Ojh2MEm=
A549 MUjBdI9xfG:|aYOgRZN{[Xl? NVrnbXJ3PTByIH7N MnHJOFghcA>? NEn3Z3FqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NEnYZ|EzPTN{OESwPS=>
A549 NFv5WWxHfW6ldHnvckBCe3OjeR?= MXOxNk42NzJ3L{WwJI5O NYfqbnlnOTBiaB?= NWW3XlhIcW6qaXLpeJMh[2WubDDtbYdz[XSrb36= NIDSXlIzPTN{OESwPS=>
M21 NFixXFJCeG:ydH;zbZMhSXO|YYm= NInNcJgyKM7:TR?= MU[yOEBp NGTON2JqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IIPp[45q\mmlYX70cJkh[2:vYnnu[YQhf2m2aDD2[Y12emGoZX7pZi=> MkHiNlQ4OzJzN{K=
M21R MVXBdI9xfG:|aYOgRZN{[Xl? MVqxJO69VQ>? MonsNlQhcA>? NUj4WXE3cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigeoVufXKjZnXubYI> MX:yOFc{OjF5Mh?=
TPF-10-741 NGT1[o5CeG:ydH;zbZMhSXO|YYm= MnzaNUDPxE1? MViyOEBp MmfZbY5lfWOnczDj[YxtKGGyb4D0c5NqeyC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnXteZJi\mWwaXK= NF:2bJIzPDd|MkG3Ni=>
Ba/F3 ITD NVziZ4lvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjhepVKSzVyPUGuN{DPxE1? NG\WUVAzPDJ{N{iyNC=>
Ba/F3 ITD/D835Y NWXnNIZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRThwNzFOwG0> NVrBcWpLOjR{Mke4NlA>
Ba/F3 WT D835Y MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2n2TmlEPTB;Nj65JO69VQ>? MUeyOFIzPzh{MB?=
Ba/F3 WT D835F NGW5TolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTZwNTFOwG0> M2DPRVI1OjJ5OEKw
Ba/F3 WT D835H MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFS4V3JKSzVyPUG5Mlgh|ryP MnLQNlQzOjd6MkC=
Ba/F3 WT D835N M2fxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlz5TWM2OD12LkOg{txO NGe5dVUzPDJ{N{iyNC=>
Ba/F3 WT D835V MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLaTWM2OD1{LkOg{txO MX6yOFIzPzh{MB?=
Ba/F3 ITD/F691L NIi1SoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzLXnlKSzVyPU[3Mlgh|ryP NF\tbZczPDJ{N{iyNC=>
MV4-11 MXPD[YxtKF[rYXLsbZR6KEG|c3H5 MoXjNE0yKM7:TR?= NGLic4E4OiCq MU\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NV30[Vl{OjRyNE[wNVQ>
MOLM-13 MXfD[YxtKF[rYXLsbZR6KEG|c3H5 MYewMVEh|ryP NG\3UGE4OiCq M3fXXolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NYfHfpJxOjRyNE[wNVQ>
PL21 M1;T[GNmdGxiVnnhZoxqfHliQYPzZZk> M3rnOlAuOTByIN88US=> M{PZSlczKGh? MnzTbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M4XwVVI1ODR4MEG0
OCI-AML3 MnWzR4VtdCCYaXHicIl1gSCDc4PhfS=> M17uTFAuOTByIN88US=> NHj5PWs4OiCq NW\o[2lRcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NITV[HczPDB2NkCxOC=>
THP-1 MYXD[YxtKF[rYXLsbZR6KEG|c3H5 M{LNT|AuOTByIN88US=> Mn;iO|IhcA>? MWPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MYKyOFA1PjBzNB?=
U937 NGrCSZpE\WyuIG\pZYJtcXS7IFHzd4F6 NXLXTHNDOC1zMECg{txO NYnqcFBnPzJiaB?= NUXFfFVJcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= Mo\2NlQxPDZyMUS=

... 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 88 mg/mL warmed (198.4 mM)
Ethanol 7 mg/mL (15.78 mM)
Water Insoluble
In vivo Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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
Formula

C26H29N5O2

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