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
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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 M2\hWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\rXmlEPTB;MdMxNE4xOyEQvF2= MmT2NlU2QTd5NUS=
HL60/VCR M1LQU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojTTWM2OD14LkmzxtExNjB|IN88US=> NU\JV4VROjV3OUe3OVQ>
K562 M3\YTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzKe4ZKSzVyPUGuN:KyOC5yMzFOwG0> NHXpXXAzPTV7N{e1OC=>
K562/ABCB1 MlLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFz5[4ZKSzVyPUSuOlfDuTBwMEGg{txO M4HvcFI2PTl5N{W0
K562/ABCG2 NWW2TlZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTuTWM2OD1zLkW0xtExNjB|IN88US=> Mlr3NlU2QTd5NUS=
HL60 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vEfGlEPTB;MT60OuKyOC5yNDFOwG0> NYGxU|R1OjV3OUe3OVQ>
HL60/ADR M336XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTFwN{NCtVAvODZizszN NEnwfXUzPTV7N{e1OC=>
HL60 Mmf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M333OWlEPTB;MD64OuKyOC5yMjFOwG0> MYGyOVU6Pzd3NB?=
HL60+PSC-833 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjuV5JKSzVyPUGuN|LDuTBwME[g{txO MWWyOVU6Pzd3NB?=
HL60/VCR MlPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHz2eZhKSzVyPU[uNlfDuTBwMEKg{txO M1\mTVI2PTl5N{W0
HL60/VCR+PSC-833 MkjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTBwOEVCtVAvODRizszN M4XXPVI2PTl5N{W0
K562 M36yWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJwMENCtVAvODVizszN MkftNlU2QTd5NUS=
K562+PSC-833 M4riZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jRRmlEPTB;Mj6wNuKyOC5yODFOwG0> MmP4NlU2QTd5NUS=
K562/ABCB1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fZU2lEPTB;ND60PeKyOC5yNDFOwG0> MV2yOVU6Pzd3NB?=
K562/ABCB1+PSC-833 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzYNIVqUUN3ME2yMlA3yrFyLkC4JO69VQ>? NIrObXAzPTV7N{e1OC=>
A549  NYjQN5MyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV:wMVExODBibl2= MUOyOE81QC95MjDo NH\4Z3pqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MUSyOVMzQDRyOR?=
A549 M4POXGFxd3C2b4Ppd{BCe3OjeR?= MV61NFAhdk1? M2rMc|Q5KGh? M2rnOolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MUWyOVMzQDRyOR?=
A549 MontSpVv[3Srb36gRZN{[Xl? NILZT2IyOi53L{K1M|UxKG6P MXyxNEBp NYHkd3Y5cW6qaXLpeJMh[2WubDDtbYdz[XSrb36= MmP2NlU{Ojh2MEm=
M21 NGjEWVNCeG:ydH;zbZMhSXO|YYm= Ml3nNUDPxE1? NWLCUpZROjRiaB?= MkLUbY5lfWOnczDj[YxtKGGyb4D0c5NqeyC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnXteZJi\mWwaXK= M4Tm[lI1PzN{MUey
M21R NU\TU4trSXCxcITvd4l{KEG|c3H5 MmLYNUDPxE1? NYfkRZRzOjRiaB?= M3iycIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\lcZVz[W[nbnni M3zp[|I1PzN{MUey
TPF-10-741 NITiRWJCeG:ydH;zbZMhSXO|YYm= MXyxJO69VQ>? NUjqVplzOjRiaB?= NYC5OGFjcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigeoVufXKjZnXubYI> NIPNUlAzPDd|MkG3Ni=>
Ba/F3 ITD MnmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTFwMzFOwG0> MUeyOFIzPzh{MB?=
Ba/F3 ITD/D835Y MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXy[lduUUN3ME24Mlch|ryP M3XURVI1OjJ5OEKw
Ba/F3 WT D835Y MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTZwOTFOwG0> MliwNlQzOjd6MkC=
Ba/F3 WT D835F M16zd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\hTWM2OD14LkWg{txO NYHxPGV1OjR{Mke4NlA>
Ba/F3 WT D835H Mlr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\5TYY1UUN3ME2xPU45KM7:TR?= NGrqdZEzPDJ{N{iyNC=>
Ba/F3 WT D835N NGPyVY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPXcIlKSzVyPUSuN{DPxE1? MXmyOFIzPzh{MB?=
Ba/F3 WT D835V MoLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTJwMzFOwG0> NEnofZIzPDJ{N{iyNC=>
Ba/F3 ITD/F691L NV7md203T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDUTWM2OD14Nz64JO69VQ>? M2TtWFI1OjJ5OEKw
MV4-11 MlezR4VtdCCYaXHicIl1gSCDc4PhfS=> MYWwMVEh|ryP NVzqSXJCPzJiaB?= NYT5SHNrcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVfCOnJTOjRyNE[wNVQ>
MOLM-13 M1;SXmNmdGxiVnnhZoxqfHliQYPzZZk> NFfsdGsxNTFizszN NIHZfY44OiCq NIfOVGNqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MmPVNlQxPDZyMUS=
PL21 MVTD[YxtKF[rYXLsbZR6KEG|c3H5 M{HWdFAuOTByIN88US=> NIntbZk4OiCq NUD0XmtocW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NXPLWIJwOjRyNE[wNVQ>
OCI-AML3 M2S5O2NmdGxiVnnhZoxqfHliQYPzZZk> MnzFNE0yODBizszN NH3lTJo4OiCq MXHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MWSyOFA1PjBzNB?=
THP-1 NYDHWJoyS2WubDDWbYFjdGm2eTDBd5NigQ>? NFPUc28xNTFyMDFOwG0> NWPE[W9KPzJiaB?= NEjHfmhqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NYDaS4tHOjRyNE[wNVQ>
U937 NVqxb5FuS2WubDDWbYFjdGm2eTDBd5NigQ>? NGnBbYcxNTFyMDFOwG0> M4TpdFczKGh? NXXJOHZNcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M13PdlI1ODR4MEG0

... 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:
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID