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 NGDlRnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTIEsUCuNFMh|ryP MkfjNlU2QTd5NUS=
HL60/VCR NVv3TGlDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV20[GZjUUN3ME22Mlk{yrFyLkCzJO69VQ>? M1;DZ|I2PTl5N{W0
K562 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;UTWM2OD1zLkRCtVAvODNizszN MYmyOVU6Pzd3NB?=
K562/ABCB1 Mny0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTRwNkhCtVAvODFizszN NGXqe2wzPTV7N{e1OC=>
K562/ABCG2 NEO5cIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\iemxKSzVyPUGuOVTDuTBwMEOg{txO MVqyOVU6Pzd3NB?=
HL60 M4\6T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DnO2lEPTB;MT60OuKyOC5yNDFOwG0> M{e2[VI2PTl5N{W0
HL60/ADR NETvb2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HuO2lEPTB;MT63NuKyOC5yNjFOwG0> M2K3[lI2PTl5N{W0
HL60 NHHJeY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TwSmlEPTB;MD64OuKyOC5yMjFOwG0> MmHaNlU2QTd5NUS=
HL60+PSC-833 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnO3TWM2OD1zLkOyxtExNjB4IN88US=> M2j5UFI2PTl5N{W0
HL60/VCR MnrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PvXGlEPTB;Nj6yO:KyOC5yMjFOwG0> NWjiZY41OjV3OUe3OVQ>
HL60/VCR+PSC-833 M3PPVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17hVWlEPTB;MD64OOKyOC5yNDFOwG0> M3O0S|I2PTl5N{W0
K562 MnzQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfQTWM2OD1{LkCyxtExNjB3IN88US=> NV72WmZuOjV3OUe3OVQ>
K562+PSC-833 NFfJNHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX[yb4ZGUUN3ME2yMlAzyrFyLkC4JO69VQ>? MUSyOVU6Pzd3NB?=
K562/ABCB1 M{PkZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHXTWM2OD12LkS5xtExNjB2IN88US=> M{XITlI2PTl5N{W0
K562/ABCB1+PSC-833 Mmj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlL4TWM2OD1{LkC2xtExNjB6IN88US=> M3\ESVI2PTl5N{W0
A549  MmnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGwMVExODBibl2= MVWyOE81QC95MjDo MlPPbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> NXLOb492OjV|Mki0NFk>
A549 Mn;qRZBweHSxc3nzJGF{e2G7 MUK1NFAhdk1? Ml24OFghcA>? M2jnXYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MlzsNlU{Ojh2MEm=
A549 NH\LXIFHfW6ldHnvckBCe3OjeR?= NWKxfJdQOTJwNT:yOU82OCCwTR?= NFzrd|gyOCCq MXPpcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? MkHQNlU{Ojh2MEm=
M21 NFHVTpFCeG:ydH;zbZMhSXO|YYm= M1na[|Eh|ryP NW\4fXNpOjRiaB?= M2TEZ4lv\HWlZYOgZ4VtdCCjcH;weI9{cXNic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\lcZVz[W[nbnni MYeyOFc{OjF5Mh?=
M21R MYrBdI9xfG:|aYOgRZN{[Xl? M1PQRVEh|ryP M3HHZVI1KGh? NGjNZXZqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IIPp[45q\mmlYX70cJkh[2:vYnnu[YQhf2m2aDD2[Y12emGoZX7pZi=> MX6yOFc{OjF5Mh?=
TPF-10-741 NF3aVYhCeG:ydH;zbZMhSXO|YYm= NHGyU3QyKM7:TR?= MmjlNlQhcA>? NWPpVmRwcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigeoVufXKjZnXubYI> MUSyOFc{OjF5Mh?=
Ba/F3 ITD MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnNTWM2OD1zLkOg{txO MWGyOFIzPzh{MB?=
Ba/F3 ITD/D835Y NWLwXWdDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXX1SW9KUUN3ME24Mlch|ryP M{Dhc|I1OjJ5OEKw
Ba/F3 WT D835Y M4TpSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTZwOTFOwG0> NXX3clJvOjR{Mke4NlA>
Ba/F3 WT D835F NHf1cJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1j4OGlEPTB;Nj61JO69VQ>? NFTWZYszPDJ{N{iyNC=>
Ba/F3 WT D835H MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTF7Lkig{txO MYOyOFIzPzh{MB?=
Ba/F3 WT D835N MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELQc3JKSzVyPUSuN{DPxE1? MVmyOFIzPzh{MB?=
Ba/F3 WT D835V NUXHNY9TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTJwMzFOwG0> M3P4XVI1OjJ5OEKw
Ba/F3 ITD/F691L MoPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn6T21oUUN3ME22O{45KM7:TR?= NFOwOJozPDJ{N{iyNC=>
MV4-11 MnGwR4VtdCCYaXHicIl1gSCDc4PhfS=> NVrnfldQOC1zIN88US=> MkKzO|IhcA>? MYHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MmfiNlQxPDZyMUS=
MOLM-13 Mn\MR4VtdCCYaXHicIl1gSCDc4PhfS=> NGXubFExNTFizszN Mmf1O|IhcA>? MVfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MkG2NlQxPDZyMUS=
PL21 MoqwR4VtdCCYaXHicIl1gSCDc4PhfS=> MlnzNE0yODBizszN NXLVe|h{PzJiaB?= MX3pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 Ml2xNlQxPDZyMUS=
OCI-AML3 MVHD[YxtKF[rYXLsbZR6KEG|c3H5 MmL5NE0yODBizszN NH64Npo4OiCq M3fRUolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NV;MemlZOjRyNE[wNVQ>
THP-1 MonER4VtdCCYaXHicIl1gSCDc4PhfS=> Mn3BNE0yODBizszN M4PK[VczKGh? NY\QUY9VcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M3LZW|I1ODR4MEG0
U937 NXzJXVlPS2WubDDWbYFjdGm2eTDBd5NigQ>? NFT6PJkxNTFyMDFOwG0> M{izO|czKGh? NYrv[W1qcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NHHxRm4zPDB2NkCxOC=>

... 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