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.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock

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4 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.

    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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 MkHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTIEsUCuNFMh|ryP NUHxc|NKOjV3OUe3OVQ>
HL60/VCR NVPlZlA3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHCcZRKSzVyPU[uPVPDuTBwMEOg{txO NUHtWJFnOjV3OUe3OVQ>
K562 M{LPN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTFwM9MxNE4xOyEQvF2= NF3uR4QzPTV7N{e1OC=>
K562/ABCB1 MlflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTRwNkhCtVAvODFizszN NHvCeVkzPTV7N{e1OC=>
K562/ABCG2 M4jnXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTFwNUVCtVAvODNizszN MkP6NlU2QTd5NUS=
HL60 NFPw[5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfVdo1KSzVyPUGuOFbDuTBwMESg{txO MXyyOVU6Pzd3NB?=
HL60/ADR NUnm[2lQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHe1NnBKSzVyPUGuO|LDuTBwME[g{txO NUPBPJlyOjV3OUe3OVQ>
HL60 NYG1TodsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHBdVZ1UUN3ME2wMlg3yrFyLkCyJO69VQ>? MXKyOVU6Pzd3NB?=
HL60+PSC-833 MkDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnP[WdKSzVyPUGuN|LDuTBwME[g{txO M{LheFI2PTl5N{W0
HL60/VCR MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;mWnlKSzVyPU[uNlfDuTBwMEKg{txO MYWyOVU6Pzd3NB?=
HL60/VCR+PSC-833 Mn;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojvTWM2OD1yLki0xtExNjB2IN88US=> Mnm5NlU2QTd5NUS=
K562 NFzhcJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV31fZNMUUN3ME2yMlAzyrFyLkC1JO69VQ>? Ml\LNlU2QTd5NUS=
K562+PSC-833 NWjISWYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVGzWZFMUUN3ME2yMlAzyrFyLkC4JO69VQ>? MkLnNlU2QTd5NUS=
K562/ABCB1 MkKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nhOmlEPTB;ND60PeKyOC5yNDFOwG0> NF7lXWYzPTV7N{e1OC=>
K562/ABCB1+PSC-833 M122Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTJwMEdCtVAvODhizszN NFnjZnMzPTV7N{e1OC=>
A549  NVPMbVZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGwMVExODBibl2= Ml34NlQwPDhxN{KgbC=> NH3GWmVqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIFv\CC2aX3lJIRmeGWwZHXueIx6 M4HoeVI2OzJ6NEC5
A549 NFjyPGZCeG:ydH;zbZMhSXO|YYm= MmX0OVAxKG6P M2freFQ5KGh? NI\rbm5qdmS3Y3XzJINmdGxiYYDvdJRwe2m| NWC5R|dHOjV|Mki0NFk>
A549 NGTuflJHfW6ldHnvckBCe3OjeR?= NH;1U4UyOi53L{K1M|UxKG6P NXrvbVBTOTBiaB?= NGLlcYRqdmirYnn0d{Bk\WyuIH3p[5JifGmxbh?= MX:yOVMzQDRyOR?=
M21 NWS1W3lpSXCxcITvd4l{KEG|c3H5 NU\6WYpbOSEQvF2= Ml;pNlQhcA>? MkLNbY5lfWOnczDj[YxtKGGyb4D0c5NqeyC|aXfubYZq[2GwdHz5JINwdWKrbnXkJJdqfGhidnXteZJi\mWwaXK= NGi3b3ozPDd|MkG3Ni=>
M21R Ml64RZBweHSxc3nzJGF{e2G7 NHvyUmwyKM7:TR?= MmX6NlQhcA>? M{f1bIlv\HWlZYOgZ4VtdCCjcH;weI9{cXNic3nncolncWOjboTsfUBkd22kaX7l[EB4cXSqII\lcZVz[W[nbnni NYTiNY5bOjR5M{KxO|I>
TPF-10-741 NFf3O4VCeG:ydH;zbZMhSXO|YYm= MUexJO69VQ>? MnTZNlQhcA>? NXrYXJpVcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzbYdvcW[rY3HueIx6KGOxbXLpcoVlKHerdHigeoVufXKjZnXubYI> NUjBSoZWOjR5M{KxO|I>
Ba/F3 ITD M3LVVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\CTWM2OD1zLkOg{txO NUDsRm1rOjR{Mke4NlA>
Ba/F3 ITD/D835Y NVPRZY1FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRThwNzFOwG0> MYmyOFIzPzh{MB?=
Ba/F3 WT D835Y MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\BfW5KSzVyPU[uPUDPxE1? NF[x[4MzPDJ{N{iyNC=>
Ba/F3 WT D835F Mmj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NID3WXpKSzVyPU[uOUDPxE1? MW[yOFIzPzh{MB?=
Ba/F3 WT D835H NGfldmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3n4cGlEPTB;MUmuPEDPxE1? NVrZVZhFOjR{Mke4NlA>
Ba/F3 WT D835N NXHE[5VuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETjdnlKSzVyPUSuN{DPxE1? M{L4TlI1OjJ5OEKw
Ba/F3 WT D835V NV3vXo4xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrlTWM2OD1{LkOg{txO NE\hOoMzPDJ{N{iyNC=>
Ba/F3 ITD/F691L NYL1SYt2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTiNGpVUUN3ME22O{45KM7:TR?= MmOxNlQzOjd6MkC=
MV4-11 NFO3fW9E\WyuIG\pZYJtcXS7IFHzd4F6 MmXWNE0yKM7:TR?= NY\iPFlPPzJiaB?= MXfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NY\RPIp{OjRyNE[wNVQ>
MOLM-13 MXTD[YxtKF[rYXLsbZR6KEG|c3H5 MVuwMVEh|ryP Mki0O|IhcA>? MnG4bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NE\WRm4zPDB2NkCxOC=>
PL21 NHXETHRE\WyuIG\pZYJtcXS7IFHzd4F6 Mn;wNE0yODBizszN NF\tSmI4OiCq Mof5bY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MlzLNlQxPDZyMUS=
OCI-AML3 NVryW2xGS2WubDDWbYFjdGm2eTDBd5NigQ>? MmT5NE0yODBizszN NIW1S4k4OiCq NFzNdI9qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M2POc|I1ODR4MEG0
THP-1 M3S0cWNmdGxiVnnhZoxqfHliQYPzZZk> NXPHSI9rOC1zMECg{txO M1vW[|czKGh? M4TRe4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M{ezR|I1ODR4MEG0
U937 NIqwVYJE\WyuIG\pZYJtcXS7IFHzd4F6 MYKwMVExOCEQvF2= NX\VcFZMPzJiaB?= NXvlPJg4cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MonwNlQxPDZyMUS=

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay
+ 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
+ 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 (200.65 mM) warming
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