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

  • 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 NEfXU|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1uxU2lEPTB;MdMxNE4xOyEQvF2= MkLYNlU2QTd5NUS=
HL60/VCR MmfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2j4bGlEPTB;Nj65N:KyOC5yMzFOwG0> NEPSWGQzPTV7N{e1OC=>
K562 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MniyTWM2OD1zLkRCtVAvODNizszN NYDZUlZzOjV3OUe3OVQ>
K562/ABCB1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2D6bWlEPTB;ND62O:KyOC5yMTFOwG0> MWGyOVU6Pzd3NB?=
K562/ABCG2 NXPpOllGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XCPWlEPTB;MT61OOKyOC5yMzFOwG0> NVnycWd4OjV3OUe3OVQ>
HL60 MmnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TnZ2lEPTB;MT60OuKyOC5yNDFOwG0> M4TNelI2PTl5N{W0
HL60/ADR MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:yUnFKSzVyPUGuO|LDuTBwME[g{txO MlHENlU2QTd5NUS=
HL60 NHO0ZVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7rfnJKSzVyPUCuPFbDuTBwMEKg{txO M4fSS|I2PTl5N{W0
HL60+PSC-833 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nYZ2lEPTB;MT6zNuKyOC5yNjFOwG0> NYDp[pdROjV3OUe3OVQ>
HL60/VCR NXPGVY9WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTZwMkhCtVAvODJizszN MXuyOVU6Pzd3NB?=
HL60/VCR+PSC-833 NXHPOIpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4D1S2lEPTB;MD64OOKyOC5yNDFOwG0> MmWyNlU2QTd5NUS=
K562 MnjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF23OHhKSzVyPUKuNFLDuTBwMEWg{txO MnnjNlU2QTd5NUS=
K562+PSC-833 NI\KWZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHtcHZKSzVyPUKuNFLDuTBwMEig{txO NVe4NnJIOjV3OUe3OVQ>
K562/ABCB1 MmD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTRwNEpCtVAvODRizszN NWHRfHZHOjV3OUe3OVQ>
K562/ABCB1+PSC-833 NGjVWm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTJwMEdCtVAvODhizszN NVnIfHJmOjV3OUe3OVQ>
A549  MoPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUCwMVExODBibl2= M3XYe|I1NzR6L{eyJIg> NEHn[pRqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 MnLhNlU{Ojh2MEm=
A549 M2fh[WFxd3C2b4Ppd{BCe3OjeR?= M1G2VlUxOCCwTR?= MYS0PEBp M4PkXYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NV6xVo5pOjV|Mki0NFk>
A549 MnzlSpVv[3Srb36gRZN{[Xl? M3zHNFEzNjVxMkWvOVAhdk1? NY\DU2NDOTBiaB?= NU\xXIdncW6qaXLpeJMh[2WubDDtbYdz[XSrb36= M2P4flI2OzJ6NEC5
M21 NWjjPVN7SXCxcITvd4l{KEG|c3H5 NYLYZo9XOSEQvF2= NUXkbopSOjRiaB?= NH\OR2xqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IIPp[45q\mmlYX70cJkh[2:vYnnu[YQhf2m2aDD2[Y12emGoZX7pZi=> M{ezNlI1PzN{MUey
M21R NXLUcWVSSXCxcITvd4l{KEG|c3H5 MmjFNUDPxE1? NGX1UmEzPCCq MonpbY5lfWOnczDj[YxtKGGyb4D0c5NqeyC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnXteZJi\mWwaXK= NUHZSpdTOjR5M{KxO|I>
TPF-10-741 Mny0RZBweHSxc3nzJGF{e2G7 MUexJO69VQ>? M{LVPVI1KGh? NXvKN5dIcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigeoVufXKjZnXubYI> Mkj6NlQ4OzJzN{K=
Ba/F3 ITD NVvzVJk5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLRWopsUUN3ME2xMlMh|ryP Ml3ENlQzOjd6MkC=
Ba/F3 ITD/D835Y NY\kSmh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33pb2lEPTB;OD63JO69VQ>? MVWyOFIzPzh{MB?=
Ba/F3 WT D835Y NUTHVlA2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HLW2lEPTB;Nj65JO69VQ>? MlLsNlQzOjd6MkC=
Ba/F3 WT D835F MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTZwNTFOwG0> MUKyOFIzPzh{MB?=
Ba/F3 WT D835H MkW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTF7Lkig{txO NVHSUG1OOjR{Mke4NlA>
Ba/F3 WT D835N NXPVV2FbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLJVFhHUUN3ME20MlMh|ryP MUGyOFIzPzh{MB?=
Ba/F3 WT D835V NEO3N5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mof3TWM2OD1{LkOg{txO MkDlNlQzOjd6MkC=
Ba/F3 ITD/F691L MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTZ5Lkig{txO NF3H[3EzPDJ{N{iyNC=>
MV4-11 NVzjW4tbS2WubDDWbYFjdGm2eTDBd5NigQ>? NVL6d40{OC1zIN88US=> MV[3NkBp NEjHN5BqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NWK5VY5EOjRyNE[wNVQ>
MOLM-13 MkHqR4VtdCCYaXHicIl1gSCDc4PhfS=> M3O3flAuOSEQvF2= MUO3NkBp MofXbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? Mn7hNlQxPDZyMUS=
PL21 M2HuUGNmdGxiVnnhZoxqfHliQYPzZZk> NGH1cFUxNTFyMDFOwG0> NG[0Ook4OiCq NXjYTJltcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M{XJT|I1ODR4MEG0
OCI-AML3 MnrzR4VtdCCYaXHicIl1gSCDc4PhfS=> MlvoNE0yODBizszN M{XFc|czKGh? NH:yWVFqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NEXxS2EzPDB2NkCxOC=>
THP-1 M4L1SGNmdGxiVnnhZoxqfHliQYPzZZk> M3rYRlAuOTByIN88US=> NF[4OXo4OiCq MXPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MmT4NlQxPDZyMUS=
U937 M1fy[2NmdGxiVnnhZoxqfHliQYPzZZk> NF[4VnkxNTFyMDFOwG0> M2fSO|czKGh? NWfuTHE3cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= Ml35NlQxPDZyMUS=

... 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 89 mg/mL warmed (200.65 mM)
Ethanol 7 mg/mL (15.78 mM)
Water <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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