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.
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 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXK3OpJjUUN3ME2xxtExNjB|IN88US=> Ml3jNlU2QTd5NUS=
HL60/VCR NFfzT4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGm3clFKSzVyPU[uPVPDuTBwMEOg{txO NIqxZWUzPTV7N{e1OC=>
K562 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTkTWM2OD1zLkRCtVAvODNizszN NILkfW0zPTV7N{e1OC=>
K562/ABCB1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\UdlRKSzVyPUSuOlfDuTBwMEGg{txO NFXCbFkzPTV7N{e1OC=>
K562/ABCG2 MlHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnHTWM2OD1zLkW0xtExNjB|IN88US=> M2jCUVI2PTl5N{W0
HL60 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTFwNEdCtVAvODRizszN NXTHVWhFOjV3OUe3OVQ>
HL60/ADR M1;uU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTCTWM2OD1zLkeyxtExNjB4IN88US=> MkPlNlU2QTd5NUS=
HL60 NGG0V21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjlZWdTUUN3ME2wMlg3yrFyLkCyJO69VQ>? NUHnbYFiOjV3OUe3OVQ>
HL60+PSC-833 NV3MNIZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojaTWM2OD1zLkOyxtExNjB4IN88US=> MlLsNlU2QTd5NUS=
HL60/VCR NX7pRY1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HNZ2lEPTB;Nj6yO:KyOC5yMjFOwG0> MnvMNlU2QTd5NUS=
HL60/VCR+PSC-833 NVLleXl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjRTFBRUUN3ME2wMlg1yrFyLkC0JO69VQ>? M2HDelI2PTl5N{W0
K562 MoDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDaTWM2OD1{LkCyxtExNjB3IN88US=> NXzWVZgzOjV3OUe3OVQ>
K562+PSC-833 NIC5eINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTJwMENCtVAvODhizszN MV:yOVU6Pzd3NB?=
K562/ABCB1 M1rQSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPMTW1KSzVyPUSuOFnDuTBwMESg{txO NVzEdHY3OjV3OUe3OVQ>
K562/ABCB1+PSC-833 NG\iU3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTJwMEdCtVAvODhizszN M1Po[|I2PTl5N{W0
A549  MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYOwMVExODBibl2= MVKyOE81QC95MjDo NXyxUW1scW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBidmRidHnt[UBl\XCnbnTlcpRtgQ>? NWnBN5VROjV|Mki0NFk>
A549 NXqwOld4SXCxcITvd4l{KEG|c3H5 NXr6NGNlPTByIH7N NITDdo01QCCq NVHjdmh1cW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MVKyOVMzQDRyOR?=
A549 NV;RRlJiTnWwY4Tpc44hSXO|YYm= MV2xNk42NzJ3L{WwJI5O NYS1bXlZOTBiaB?= MX3pcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? NYPqfYoyOjV|Mki0NFk>
M21 NV3XRpFKSXCxcITvd4l{KEG|c3H5 MYCxJO69VQ>? M3HoflI1KGh? NIrnXnNqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IIPp[45q\mmlYX70cJkh[2:vYnnu[YQhf2m2aDD2[Y12emGoZX7pZi=> NVe1U5BLOjR5M{KxO|I>
M21R NIXrZ25CeG:ydH;zbZMhSXO|YYm= MnrkNUDPxE1? MlHtNlQhcA>? NW[5WmdtcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigeoVufXKjZnXubYI> NInJTVUzPDd|MkG3Ni=>
TPF-10-741 MnzKRZBweHSxc3nzJGF{e2G7 MWmxJO69VQ>? MmXtNlQhcA>? NVXqcIs1cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigeoVufXKjZnXubYI> M3q4RlI1PzN{MUey
Ba/F3 ITD NHPsU3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkWzTWM2OD1zLkOg{txO M1nkbVI1OjJ5OEKw
Ba/F3 ITD/D835Y MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jBdmlEPTB;OD63JO69VQ>? NX3DcVhyOjR{Mke4NlA>
Ba/F3 WT D835Y NHX6VIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DTe2lEPTB;Nj65JO69VQ>? NGfoXFczPDJ{N{iyNC=>
Ba/F3 WT D835F M{TFXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TRemlEPTB;Nj61JO69VQ>? NGDFXHgzPDJ{N{iyNC=>
Ba/F3 WT D835H MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTF7Lkig{txO NX7YSJRkOjR{Mke4NlA>
Ba/F3 WT D835N MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmL6TWM2OD12LkOg{txO NIi0bIozPDJ{N{iyNC=>
Ba/F3 WT D835V NWmxdGNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M374VWlEPTB;Mj6zJO69VQ>? NVTzdXlvOjR{Mke4NlA>
Ba/F3 ITD/F691L MlfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHIOIkxUUN3ME22O{45KM7:TR?= NEPGe3EzPDJ{N{iyNC=>
MV4-11 MUDD[YxtKF[rYXLsbZR6KEG|c3H5 Mn3lNE0yKM7:TR?= MnrMO|IhcA>? MkfVbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M{fRNFI1ODR4MEG0
MOLM-13 NW\MZWlTS2WubDDWbYFjdGm2eTDBd5NigQ>? MmfZNE0yKM7:TR?= MmLaO|IhcA>? NHfFUHFqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NVrGeGt7OjRyNE[wNVQ>
PL21 M2LIemNmdGxiVnnhZoxqfHliQYPzZZk> NX\HNZNzOC1zMECg{txO M{f1WlczKGh? NGTqVnVqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MY[yOFA1PjBzNB?=
OCI-AML3 M3r3WmNmdGxiVnnhZoxqfHliQYPzZZk> M3\zPVAuOTByIN88US=> MWG3NkBp NHPsNYtqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M2DHfVI1ODR4MEG0
THP-1 NY\GV5U4S2WubDDWbYFjdGm2eTDBd5NigQ>? NVTQS|hsOC1zMECg{txO Mn2zO|IhcA>? MYLpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M4L4WVI1ODR4MEG0
U937 M{\lW2NmdGxiVnnhZoxqfHliQYPzZZk> M{\0V|AuOTByIN88US=> MXi3NkBp NHzvZ2VqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NHP4VmQzPDB2NkCxOC=>

... 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
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