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
USD 170 In stock
USD 320 In stock
USD 970 In stock
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5 Customer Reviews

  • Clin Cancer Res 2013 19(24), 6935-42. 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.
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 MlKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDkTWM2OD1zwsGwMlA{KM7:TR?= M4\GdVI2PTl5N{W0
HL60/VCR NVLoeHFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\vTWM2OD14LkmzxtExNjB|IN88US=> M2fTeFI2PTl5N{W0
K562 NWTiZmd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkSyTWM2OD1zLkRCtVAvODNizszN NYe1Z4FmOjV3OUe3OVQ>
K562/ABCB1 NF7mcotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\r[WlEPTB;ND62O:KyOC5yMTFOwG0> NY\R[4RqOjV3OUe3OVQ>
K562/ABCG2 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTIfW1XUUN3ME2xMlU1yrFyLkCzJO69VQ>? NIG2b4ozPTV7N{e1OC=>
HL60 NXfGSoNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTFwNEdCtVAvODRizszN MnzDNlU2QTd5NUS=
HL60/ADR M3ftO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq2TWM2OD1zLkeyxtExNjB4IN88US=> M3X1OlI2PTl5N{W0
HL60 NWTVXGlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{m1dWlEPTB;MD64OuKyOC5yMjFOwG0> NWTHSGZyOjV3OUe3OVQ>
HL60+PSC-833 NH31NFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDjTWM2OD1zLkOyxtExNjB4IN88US=> MlS1NlU2QTd5NUS=
HL60/VCR MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULxSHEyUUN3ME22MlI4yrFyLkCyJO69VQ>? NH;aeVAzPTV7N{e1OC=>
HL60/VCR+PSC-833 NIjDbYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1r2NWlEPTB;MD64OOKyOC5yNDFOwG0> MkDkNlU2QTd5NUS=
K562 M2rCeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTJwMENCtVAvODVizszN NIrVV5ozPTV7N{e1OC=>
K562+PSC-833 M1vzemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonkTWM2OD1{LkCyxtExNjB6IN88US=> NYS2V2RQOjV3OUe3OVQ>
K562/ABCB1 NYrWclhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnj2TWM2OD12LkS5xtExNjB2IN88US=> NUPM[nA4OjV3OUe3OVQ>
K562/ABCB1+PSC-833 M13XRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;RTWM2OD1{LkC2xtExNjB6IN88US=> Ml3ZNlU2QTd5NUS=
A549  NIry[FNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXuwMVExODBibl2= M4nFWFI1NzR6L{eyJIg> M2WwSIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> NVLs[JdJOjV|Mki0NFk>
A549 NIPWRmxCeG:ydH;zbZMhSXO|YYm= NX72bGJlPTByIH7N MnLxOFghcA>? MXPpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NYLrNWV[OjV|Mki0NFk>
A549 NYXSbZB2TnWwY4Tpc44hSXO|YYm= MYmxNk42NzJ3L{WwJI5O MYGxNEBp Mne0bY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25? NWW3PFVjOjV|Mki0NFk>
M21 MkHKRZBweHSxc3nzJGF{e2G7 M3PUVFEh|ryP MViyOEBp Ml;TbY5lfWOnczDj[YxtKGGyb4D0c5NqeyC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnXteZJi\mWwaXK= MUCyOFc{OjF5Mh?=
M21R NVnsW|hVSXCxcITvd4l{KEG|c3H5 MmfuNUDPxE1? NV7URZRkOjRiaB?= M{L4colv\HWlZYOgZ4VtdCCjcH;weI9{cXNic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\lcZVz[W[nbnni NIG0RXgzPDd|MkG3Ni=>
TPF-10-741 NEPxeVBCeG:ydH;zbZMhSXO|YYm= NWS2WVRMOSEQvF2= MUCyOEBp MYLpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHOrZ37p[olk[W62bImgZ49u[mmwZXSge4l1cCC4ZX31doFn\W6rYh?= NWnQT5lpOjR5M{KxO|I>
Ba/F3 ITD MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTFwMzFOwG0> MmLPNlQzOjd6MkC=
Ba/F3 ITD/D835Y NYTLeXV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRThwNzFOwG0> MV6yOFIzPzh{MB?=
Ba/F3 WT D835Y NGTSdoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWH5c|NbUUN3ME22Mlkh|ryP M13XS|I1OjJ5OEKw
Ba/F3 WT D835F MoTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zobGlEPTB;Nj61JO69VQ>? M3z3V|I1OjJ5OEKw
Ba/F3 WT D835H NHzCWpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TyO2lEPTB;MUmuPEDPxE1? MXOyOFIzPzh{MB?=
Ba/F3 WT D835N MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LpXmlEPTB;ND6zJO69VQ>? M3;yeFI1OjJ5OEKw
Ba/F3 WT D835V NWPRTIMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnyTWM2OD1{LkOg{txO NGHIZo8zPDJ{N{iyNC=>
Ba/F3 ITD/F691L NXLybpB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zOVmlEPTB;NkeuPEDPxE1? MX2yOFIzPzh{MB?=
MV4-11 MV3D[YxtKF[rYXLsbZR6KEG|c3H5 NY\4fWFrOC1zIN88US=> Mom5O|IhcA>? MlfqbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NUTtVmlPOjRyNE[wNVQ>
MOLM-13 NFvZcY1E\WyuIG\pZYJtcXS7IFHzd4F6 MlnWNE0yKM7:TR?= M17JR|czKGh? NF7EWZFqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MWOyOFA1PjBzNB?=
PL21 Mm\qR4VtdCCYaXHicIl1gSCDc4PhfS=> MXywMVExOCEQvF2= Mn7RO|IhcA>? NYP0UHQ{cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M{jo[lI1ODR4MEG0
OCI-AML3 NUftS3N3S2WubDDWbYFjdGm2eTDBd5NigQ>? MYqwMVExOCEQvF2= M13r[|czKGh? NV7yN5JycW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M4f5Z|I1ODR4MEG0
THP-1 M4S2S2NmdGxiVnnhZoxqfHliQYPzZZk> NGLLWnIxNTFyMDFOwG0> Ml;NO|IhcA>? M{fhbIlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MorQNlQxPDZyMUS=
U937 M{PRe2NmdGxiVnnhZoxqfHliQYPzZZk> NIDuOIMxNTFyMDFOwG0> MmTBO|IhcA>? MWHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MmHpNlQxPDZyMUS=

... 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 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
Formula

C26H29N5O2

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
NCT01522469 Completed Relapsed or Refractory Acute Myeloid Leukemia With FLT3 Activating Mutations Arog Pharmaceuticals Inc. July 2012 Phase 2
NCT01243346 Completed D842-related Mutant GIST Arog Pharmaceuticals Inc. April 2011 Phase 2
NCT01229644 Terminated Glioma Arog Pharmaceuticals Inc. April 2011 Phase 2
NCT00386555 Withdrawn Carcinoma Non-Small-Cell Lung Arog Pharmaceuticals Inc. May 2007 Phase 2
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