Dovitinib (TKI-258, CHIR-258)

Catalog No.S1018

Dovitinib (TKI-258, CHIR-258) Chemical Structure

Molecular Weight(MW): 392.43

Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.

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Cited by 19 Publications

Purity & Quality Control

Choose Selective FLT3 Inhibitors

Biological Activity

Description Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.
Targets
FLT3 [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
FGFR1 [1]
(Cell-free assay)
VEGFR3/FLT4 [1]
(Cell-free assay)
FGFR3 [1]
(Cell-free assay)
1 nM 2 nM 8 nM 8 nM 9 nM
In vitro

Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50 of 25 nM. In addition, Dovitinib inhibits proliferation of B9 cells expressing each of the various activated mutants of FGFR3. Interestingly, there are minimal observed differences in the sensitivity of the different FGFR3 mutations to Dovitinib, with the IC50 ranging from 70 to 90 nM for each of the various mutations. IL-6-dependent B9 cells containing vector only (B9-MINV cells are resistant to the inhibitory activity of Dovitinib at concentrations up to 1 μM. Dovitinib inhibits cell proliferation of KMS11 (FGFR3-Y373C), OPM2 (FGFR3-K650E), and KMS18 (FGFR3-G384D) cells with IC50 of 90 nM (KMS11 and OPM2) and 550 nM, respectively. Dovitinib inhibits FGF-mediated ERK1/2 phosphorylation and induces cytotoxicity in FGFR3-expressing primary MM cells. BMSCs does confer a modest degree of resistance with 44.6% growth inhibition for cells treated with 500 nM Dovitinib and cultured on stroma compared with 71.6% growth inhibition for cells grown without BMSCs. Dovitinib inhibits proliferation of M-NFS-60, an M-CSF growth-driven mouse myeloblastic cell line with a median effective concentration (EC50) of 220 nM. [1] Treatment of SK-HEP1 cells with Dovitinib results in a dose-dependent reduction in cell number and G2/M phase arrest with reduction in the G0/G1 and S phases, inhibition of anchorage-independent growth and blockage of bFGF-induced cell motility. The IC50 for Dovitinib in SK-HEP1 cells is approximately 1.7 μM. Dovitinib also significantly reduces the basal phosphorylation levels of FGFR-1, FGFR substrate 2α (FRS2-α) and ERK1/2 but not Akt in both SK-HEP1 and 21-0208 cells. In 21-0208 HCC cells, Dovitinib significantly inhibits bFGF-induced phosphorylation of FGFR-1, FRS2-α, ERK1/2 but not Akt. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SupB15 NG\Yd4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjkWIpZUUN3ME2wMlQ1QSEQvF2= NYXPbJNNOjV{MEKwO|M>
SupB15-R M33R[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYK1VGdxUUN3ME2wMlU2QCEQvF2= NUHLWXFmOjV{MEKwO|M>
BaF3-pSRα NV\uUolCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwNk[4JO69VQ>? NGm1c4szPTJyMkC3Ny=>
BaF3-p210Bcr-Abl M4\6Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHFTWM2OD1yLk[5NkDPxE1? MYGyOVIxOjB5Mx?=
BaF3-p210Bcr-Abl-T315I MonGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\zWIVKSzVyPUKuOlI3KM7:TR?= MYGyOVIxOjB5Mx?=
CCRF-CEM NX;NZZViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTBwM{m4JO69VQ>? NYLlbm1xOjV{MEKwO|I>
CEM/C2 NFf5VGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fDWmlEPTB;MT6xNlUh|ryP MoLvNlUzODJyN{K=
Nalm-6 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLv[3lKSzVyPUCuN|gzKM7:TR?= NE\uUGUzPTJyMkC3Ni=>
SEM-K2 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUj3eY9LUUN3ME2wMlAzOiEQvF2= NF76dWUzPTJyMkC3Ni=>
HB-1119 NV\i[|Z3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTBwMEK4JO69VQ>? NH;yPIszPTJyMkC3Ni=>
RS4:11 NYrpbIg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjyTWM2OD1{LkixJO69VQ>? NGW0eWszPTJyMkC3Ni=>
Nalm-6 MX\BdI9xfG:|aYOgRZN{[Xl? NGWwRXYzKM7:TR?= MX:yOE81QCCq M3HSXIlv\HWlZYOgZZBweHSxc3nzJJJme3WudHnu[{BqdiCjYn;1eEA4OiVib3[gZ4VtdCCmZXH0bEBi\nSncjCyOEBpKHS{ZXH0cYVvfCCjbnSgPFEmKGGodHXyJFQ5KGh? NULTWY1COjV{MEKwO|I>
SEM-K2 NFnxWGFCeG:ydH;zbZMhSXO|YYm= MlGzNE4yNzFizszN NYrlWZE3OjRiaB?= Mln2bY5lfWOnczDlZZJtgSCjcH;weI9{cXNib3[gV2VONUt{IHPlcIx{KGG2IECuNUDPxE1iYX\0[ZIhOjRiaB?= M1z4cFI2OjB{MEey
HCT-116 NGi0NI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvCTWM2OD1|LkC1NE42QCEQvF2= MWiyOFQ6PTd3MB?=
HT-29 M1jtN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTVwMkGuPVMh|ryP M4H3clI1PDl3N{Ww
SW-480 NYXmRXIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vqS2lEPTB;ND6zN|AvPDdizszN MVyyOFQ6PTd3MB?=
CaCO2 NGn3dWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPZcmZKSzVyPUOuNlMxNjZ2IN88US=> M1T0WVI1PDl3N{Ww
LS174T M1To[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{f5VmlEPTB;ND6zN|AvPDdizszN MXyyOFQ6PTd3MB?=
HEC-1A NVexZZpvTnWwY4Tpc44hSXO|YYm= NGPiNJIxNjB3L{CuNU8xNjVizszN M{W2flczKGh? MlXCZ4F2e2W|IHGg[IVkemWjc3WgbY4hW1SDVEOsJGVTUyxiYX7kJGFMXCCyaH;zdIhwenmuYYTpc44> MmLFNlQ1QTV5NUC=
AN3CA M3HKUmZ2dmO2aX;uJGF{e2G7 NHjkPYsxNjB3L{CuNU8xNjVizszN NYXzd3o6PzJiaB?= M1;xToNifXOnczDhJIRm[3KnYYPlJIlvKFOWQWSzMEBGWktuIHHu[EBCU1RicHjvd5Bpd3K7bHH0bY9v M1zxUVI1PDl3N{Ww
MFE-296  MnfISpVv[3Srb36gRZN{[Xl? NF;4WWIxNjB3L{CuNU8xNjVizszN NETtSos4OiCq MnzpZ4F2e2W|IHGg[IVkemWjc3WgbY4hW1SDVEOsJGVTUyxiYX7kJGFMXCCyaH;zdIhwenmuYYTpc44> NULldpRGOjR2OUW3OVA>
UMC3 MoXmR4VtdCCYaXHibYxqfHliQYPzZZk> M3fqeFEuOTBizszN M4C3Z|czKGh? MXvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NFjs[YYzPDN{NUS2NS=>
5637 MVzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHPqRVEyNTFyIN88US=> NVzyOopCPzJiaB?= NUDQWFI5cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M{XSNFI1OzJ3NE[x
HU456 NU\0Z|ZNS2WubDDWbYFjcWyrdImgRZN{[Xl? M37sNFEuOTBizszN M1LMS|czKGh? MV;pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MoqzNlQ{OjV2NkG=
MGHU4 MnTqR4VtdCCYaXHibYxqfHliQYPzZZk> NIe1VVgyNTFyIN88US=> MWS3NkBp NUjxeWxKcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MYmyOFMzPTR4MR?=
HT1376 M{foRWNmdGxiVnnhZoltcXS7IFHzd4F6 M33vNVEuOTBizszN NF3qc2Q4OiCq MVrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M3rmcVI1OzJ3NE[x
RT112 NYPOW2ZjS2WubDDWbYFjcWyrdImgRZN{[Xl? MYWxMVExKM7:TR?= MlrXO|IhcA>? MUDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M{\NTFI1OzJ3NE[x
T24 Mo[4R4VtdCCYaXHibYxqfHliQYPzZZk> M2Xw[VEuOTBizszN MWG3NkBp NULHXHFDcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MoTpNlQ{OjV2NkG=
BFTC905 MWXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFOwbXEyNTFyIN88US=> NULEN4NFPzJiaB?= MljUbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MYWyOFMzPTR4MR?=
TCC-SUP MYPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWexMVExKM7:TR?= MXq3NkBp M4jyT4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NWflWGM3OjR|MkW0OlE>
RT4 MkGyR4VtdCCYaXHibYxqfHliQYPzZZk> NEfGVm0yNTFyIN88US=> M{HNVFczKGh? Mnv5bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MkDUNlQ{OjV2NkG=
HONE1 NGfnfmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjjfoIxNjFvMUCg{txO Moq1OFjDqGh? NEDtR25qdmS3Y3XzJGczN01iZHXsZZkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MkDkNlQzOzhyOUS=
HNE1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnH3NE4yNTFyIN88US=> M3rteFQ5yqCq MkTWbY5lfWOnczDHNk9OKGSnbHH5JIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy MX[yOFI{QDB7NB?=
CNE2  MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmCwNE4yNTFyIN88US=> NX;ye4VZPDkEoHi= M1W5e4lv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> MVeyOFI{QDB7NB?=
C666-1 MmC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX73bpVLOC5zLUGwJO69VQ>? NWPKVIduPDkEoHi= MX\pcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= NILVS5AzPDJ|OEC5OC=>
HeLa MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUewMlEuOTBizszN NH3GPWozPCCq MXXpcoR2[2W|IFeyM20h[XK{ZYP0JIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy MXGyOFI{QDB7NB?=
Hep3B MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzEWHhqOC5zLUGwJO69VQ>? MnXGNlQhcA>? NUnBTo16cW6mdXPld{BIOsLiYYLy[ZN1yqB? MUmyOFI{QDB7NB?=
HepG2 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHL1enU1QCCq M1;GdmlEPTB;Mj63NlchyrFiMD60Nlkh|ryP NVPG[GZsOjN3NE[1PVE>
Hep3B NG\GPWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXvOFghcA>? M3KzcWlEPTB;ND6yNlMhyrFiMD64N|kh|ryP Mn3SNlM2PDZ3OUG=
PLC/PRF5 NHLEUHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2qxS|Q5KGh? NEK0cXlKSzVyPUG2MlEzOCEEsTC0MlAxOSEQvF2= NYHo[GVZOjN3NE[1PVE>
Huh7 NUPmU2psT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVW0PEBp NVv1T|lyUUN3ME2xOU4xODdiwsGgO{4{OzRizszN M4\MRVI{PTR4NUmx
HepG2 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXK3NkBp MkjvTWM2OD1zLkKwNEDDuSByLkKyOkDPxE1? M{ju[lI{PTR4NUmx
Hep3B M{LzXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWW3T|dUPzJiaB?= M4DTTGlEPTB;MD64PVIhyrFiMD6wOFQh|ryP NGPmU2kzOzV2NkW5NS=>
PLC/PRF5 NFWy[o9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfsO|IhcA>? NYnScItWUUN3ME2zMlEyOCEEsTCwMlM{PyEQvF2= M3jI[|I{PTR4NUmx
Huh7 NIDXXmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPNfpFmPzJiaB?= M1HSeWlEPTB;Mz65PFAhyrFiMD64NFMh|ryP NX3KSHJPOjN3NE[1PVE>
MFE280 M122emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF61RpFKSzVyPUCuOFIhyrFiMD6wOkDPxE1? MXmyN|Q1OzhyNR?=
AN3CA NGD3O4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nYR2lEPTB;MD61NEDDuSByLkGwJO69VQ>? MWqyN|Q1OzhyNR?=
HEC155 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fnV2lEPTB;MD62OkDDuSByLkC5JO69VQ>? NVLkeY51OjN2NEO4NFU>
MFE296 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTBwNk[gxtEhOC5zOTFOwG0> NFS4fpYzOzR2M{iwOS=>
SPAC1S M3O1bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnCWVNKSzVyPUCuO|chyrFiMD6wPEDPxE1? MYCyN|Q1OzhyNR?=
RL952 M4[wSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjlZ25KSzVyPUCuPVMhyrFiMD6wNUDPxE1? M4fENFI{PDR|OEC1
EN1 MmfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUP5U|E6UUN3ME2xMlAzKMLzIECuNlUh|ryP Ml;aNlM1PDN6MEW=
SNGII NVf4VFhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fqZWlEPTB;MT6yOEDDuSByLkK4JO69VQ>? NFHvU2ozOzR2M{iwOS=>
ISHIKAWA MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7VTWM2OD1zLkOwJOKyKDBwMUGg{txO Ml\lNlM1PDN6MEW=
HEC1A MlPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfq[pRKSzVyPUGuN|QhyrFiMD6zNEDPxE1? NHf5Z28zOzR2M{iwOS=>
KLE MmfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTFwM{egxtEhOC5yMjFOwG0> NHzXOIwzOzR2M{iwOS=>
SNGM M3PwSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTFwNEKgxtEhOC5zMzFOwG0> MoLiNlM1PDN6MEW=
USPC2 NI\O[otIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUO3T44{UUN3ME2xMlYzKMLzIECuNFEh|ryP NHjKXVkzOzR2M{iwOS=>
EN MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLOTWM2OD1zLk[2JOKyKDBwMEGg{txO NXnqNGlCOjN2NEO4NFU>
MFE319 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3GxRWlEPTB;MT64O{DDuSByLkS1JO69VQ>? Ml3KNlM1PDN6MEW=
EFE184 NIHUR|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7zTWM2OD1{LkC0JOKyKDBwMUOg{txO MYKyN|Q1OzhyNR?=
ECC1 NYXUW2RbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4f0XWlEPTB;Mj6wO{DDuSByLkCxJO69VQ>? MonDNlM1PDN6MEW=
HEC1B M3XIfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTJwNUegxtEhOC5{MzFOwG0> NEnXTVczOzR2M{iwOS=>
USPC1 MnvXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fy[GlEPTB;Mj62NEDDuSByLkGzJO69VQ>? MVOyN|Q1OzhyNR?=
SPAC1L Ml;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rod2lEPTB;Mz6wOkDDuSBzLkG0JO69VQ>? MXeyN|Q1OzhyNR?=
HUVEC NWjuWGRrS2WubDDWbYFjcWyrdImgRZN{[Xl? NY[3UXZ7OC1{NTFOwG0> M3HQelczKGh? NUDmdFk{TE2VTx?= MWjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M4jXbFI{OjJ6MEG3
HMVEC NEjpW5dE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MX[wMVI2KM7:TR?= M2TWbVczKGh? NYHDeph3TE2VTx?= MmTEbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MUCyN|IzQDBzNx?=
MHCC-97H M3PYNGNmdGxiVnnhZoltcXS7IFHzd4F6 M1LCRlAuOjVizszN M3nWXlczKGh? NEnLVY1FVVOR NF\LdG1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MWeyN|IzQDBzNx?=
SMMC7721 M1fsZmNmdGxiVnnhZoltcXS7IFHzd4F6 Mn7KNE0zPSEQvF2= MkDEO|IhcA>? NXfHWodOTE2VTx?= MUfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MnfMNlMzOjhyMUe=
Huh-7 MmHYRZBweHSxc3nzJGF{e2G7 NYnZ[I1xOC1zMj61JO69VQ>? MVyyOEBp MmPLSG1UV8Li MkHyd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFjocY8zOjJ|MES3PS=>
Sk-Hep1 MWLBdI9xfG:|aYOgRZN{[Xl? MojlNE0yOi53IN88US=> MYCyOEBp NV;DbW03TE2VT9Mg M{LuSpNmdnOrdHn6[ZMhUEOFIHPlcIx{KHSxIGTSRWlNNSCjbnSgeIlo[XS3eoXtZYIucW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3LWSlIzOjNyNEe5
Hep3B NETnd|RCeG:ydH;zbZMhSXO|YYm= MYiwMVEzNjVizszN NX\FdoZyOjRiaB?= NUfjR3VlTE2VT9Mg MUDz[Y5{cXSrenXzJGhESyClZXzsd{B1dyCWUlHJUE0h[W6mIITp[4F1fXq3bXHiMYlv\HWlZXSgZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M3zpOVIzOjNyNEe5
PLC5 MWXBdI9xfG:|aYOgRZN{[Xl? M3XsVFAuOTJwNTFOwG0> NYrhOFZjOjRiaB?= MYTEUXNQyqB? M{nWZZNmdnOrdHn6[ZMhUEOFIHPlcIx{KHSxIGTSRWlNNSCjbnSgeIlo[XS3eoXtZYIucW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NXjQUnRrOjJ{M{C0O|k>
PLC5 NVnrUmNrS2WubDDWbYFjcWyrdImgRZN{[Xl? M3viSlAuOTVizszN NHm2XIs4OiCq M{SybJJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NHHTSZczOjF6MEOwPC=>
Hep3B NIi4foRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGXUWIYxNTF3IN88US=> NEjzdJc4OiCq NUS5dlBxemWmdXPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg MY[yNlE5ODNyOB?=
Sk-Hep1 NHn3[2hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGe2XFUxNTF3IN88US=> NYD5[pZ{PzJiaB?= M2\TXpJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NVu2XmI2OjJzOECzNFg>
Huh-7 NF;FXFBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MnfHNE0yPSEQvF2= MnzhO|IhcA>? NH75dFJz\WS3Y3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M2PtOFIzOThyM{C4
PLC5 NWnIW|FHSXCxcITvd4l{KEG|c3H5 M2HsfFAuOTVizszN MXuyOEBp NEjHRnNqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MoDCNlIyQDB|MEi=
Hep3B M3fDVWFxd3C2b4Ppd{BCe3OjeR?= NUjienE3OC1zNTFOwG0> Mo\mNlQhcA>? MYHpcoNz\WG|ZYOgZZBweHSxdHnjJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZLDqA>? NULaeFVuOjJzOECzNFg>
Sk-Hep1 NGT1cYhCeG:ydH;zbZMhSXO|YYm= NVrz[llFOC1zNTFOwG0> NFrhOmozPCCq NITiPZZqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= Ml7KNlIyQDB|MEi=
Huh-7 NYrmUXlrSXCxcITvd4l{KEG|c3H5 MYKwMVE2KM7:TR?= M1PYVVI1KGh? NVjy[oFJcW6lcnXhd4V{KGGyb4D0c5Rq[yClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M4DzdVIzOThyM{C4
PLC5 M{Pq[mZ2dmO2aX;uJGF{e2G7 NY\SS3Z[OC1zMDFOwG0> NEDYOoIzPCCq NYLEW5F5[2G3c3XzJIRwe2VvZHXw[Y5l\W62IFTORUBnemGpbXXueIF1cW:w M2D6[VIzOThyM{C4
Hep3B MXvGeY5kfGmxbjDBd5NigQ>? MV[wMVExKM7:TR?= NFTTblEzPCCq Mmr1Z4F2e2W|IHTvd4Uu\GWyZX7k[Y51KESQQTDmdoFodWWwdHH0bY9v NH3ufIIzOjF6MEOwPC=>
Sk-Hep1 Mn;aSpVv[3Srb36gRZN{[Xl? NVTjXWtFOC1zMDFOwG0> M1ftS|I1KGh? MkTqZ4F2e2W|IHTvd4Uu\GWyZX7k[Y51KESQQTDmdoFodWWwdHH0bY9v MV[yNlE5ODNyOB?=
Huh-7 NWHuNGNuTnWwY4Tpc44hSXO|YYm= MnzoNE0yOCEQvF2= MYKyOEBp Mn;DZ4F2e2W|IHTvd4Uu\GWyZX7k[Y51KESQQTDmdoFodWWwdHH0bY9v M33PflIzOThyM{C4
SW780 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLSOUBl NFLSOYZKSzVyPUWwJI5O M3\YPFIyOTF7Nk[x
RT112 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWWzdnB{PSCm NVfJNpRWUUN3ME2xOUBvVQ>? M1XKZVIyOTF7Nk[x
RT4 NHj6d5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUm1JIQ> NHjC[nlKSzVyPUWgcm0> NGH3PZgzOTFzOU[2NS=>
JMSU1 MlHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvBRZU2KGR? MnS1TWM2OD13MDDuUS=> MnG0NlEyOTl4NkG=
J82 NYjzWVhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PsZ|Uh\A>? M1H3S2lEPTB;MUSwNEBvVQ>? MX[yNVEyQTZ4MR?=
97-7 NF\VSmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjkU4Q6PSCm M1m2cmlEPTB;MUCwNEBvVQ>? M3HTO|IyOTF7Nk[x
RT112 MlHPSpVv[3Srb36gRZN{[Xl? NHTRcYQ2ODBibl2= M4fPRVI1KGh? MV7pcoNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gS|HDqGGlY3;tdIFvcWWmIHL5JIEh\GWlcnXhd4UhcW5iUzDhcoQhTzJxTTDwbIF{\XN? NE[xVYQzOTFzOU[2NS=>
RT4 MkG3SpVv[3Srb36gRZN{[Xl? NWniU254PTByIH7N M2LmelI1KGh? MnHSbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| M1XIWVIyOTF7Nk[x
MGH-U3 NYTWfllkTnWwY4Tpc44hSXO|YYm= MnPpOVAxKG6P MmPsNlQhcA>? NGfQSZlqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= MUiyNVEyQTZ4MR?=
SW780 NIPlNFhHfW6ldHnvckBCe3OjeR?= MmrDOVAxKG6P M3XXbFI1KGh? NHfNdphqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= MnHDNlEyOTl4NkG=
97-7 MX\GeY5kfGmxbjDBd5NigQ>? MlXuOVAxKG6P M1i0S|I1KGh? NIDqTlVqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= M1TiSVIyOTF7Nk[x
 J807C MkX5R4VtdCCYaXHibYxqfHliQYPzZZk> MkDGNE01ODBibl2= MmP5OFghcA>? M2XRUolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M3z0OFE2PTl6OEG0
Y373C MVzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MV6wMVQxOCCwTR?= M2TQWVQ5KGh? Mn7lbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> Ml23NVU2QTh6MUS=
K650E M4C2NWNmdGxiVnnhZoltcXS7IFHzd4F6 NVH0NGNGOC12MECgcm0> MY[0PEBp MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NXfGRY57OTV3OUi4NVQ>
G384D NFOxZYhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXqyU5FqOC12MECgcm0> M135NlQ5KGh? M2rQPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MlvqNVU2QTh6MUS=
F384L M2KyemNmdGxiVnnhZoltcXS7IFHzd4F6 M4LHVlAuPDByIH7N M1zr[VQ5KGh? NE\vcodqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M2HDRVE2PTl6OEG0
KMS11 MliwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPQOmw4OiCq M2K2cGlEPTB;OUCgcm0> NHi2Z|MyPTV7OEixOC=>
KMS18 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTsbJdxPzJiaB?= NIHwfGZKSzVyPUW1NEBvVQ>? NV7rbZA2OTV3OUi4NVQ>
OPM2 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFf6PJc4OiCq M{HHZ2lEPTB;OUCgcm0> MofFNVU2QTh6MUS=
H929 Mn7QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHvO|IhcA>? MmDzTWM2OD5iMkWwNEBvVQ>? NXrWem9tOTV3OUi4NVQ>
8226 Mn7mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWe3NkBp MYPJR|UxRiB{NUCwJI5O M3q0b|E2PTl6OEG0
U266 NH6yVmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TPTFczKGh? MnzOTWM2OD5iMkWwNEBvVQ>? M3WxdVE2PTl6OEG0

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CDK1 / p-CDK1 / p53 / p21 ; 

PubMed: 24238094     


(A) Dovitinib induces phosphorylation of CDK1(Tyr15) in nasopharyngeal carcinoma cells. HONE1 cells were incubated with Dovitinib (5 μM) and harvested at the indicated time-points. Lysates were prepared and the indicated proteins were detected with immunoblotting. Equal loading of lysates was confirmed by immunoblotting for actin. (B) Dovitinib induces phosphorylation of CDK1Tyr15 in HeLa cells. HeLa cells were exposed to the indicated concentrations of Dovitinib for 24 hrs. Lysates were prepared and analysed with immunoblotting. Equal loading of extracts was accessed by immunoblotting of actin. (C) Dovitinib induces phosphorylation of CDK1Tyr15 in Hep3B cells. Hep3B cells were treated with the indicated concentrations of Dovitinib for 24 hrs. Lysates were prepared for immunoblotting analysis. Actin was probed to confirm equal loading. 

p-PDGFR-β / PDGFR-β / p-ERK / ERK ; 

PubMed: 23228017     


Phosphorylation of p-PDGFR-β and p-ERK were inhibited by dovitinib at pharmacologically relevant concentrations in MHCC-97H and SMMC7721 cells.

p-VEGFR-2 / VEGFR-2 / p-FGFR-1 / FGFR-1 ; 

PubMed: 23228017     


Dovitinib inhibited the phosphorylation of FGFG-1, VEGFR-2, and downstream ERK in HMVEC and HUVEC endothelial cells at pharmacologically relevant concentrations.

p-STAT3 / STAT3 / Mcl-1 / LC3 / Beclin 1 / p62 ; 

PubMed: 31485222     


The protein extracts from dovitinib-treated were subjected to immunoblot analysis for p-STAT3, STAT3, Mcl-1, beclin1, LC3B, p62, and actin.

24238094 23228017 31485222
Growth inhibition assay
Cell viability; 

PubMed: 28467797     


Cell viability of peripheral blood mononuclear cells (PBMCs) and RPMI8226 cells treated with dovitinib in RPMI1640 medium containing 5% FBS for 24 h. Data are presented as mean±SD. Experiments were performed in triplicate.* P < 0.01, **P < 0.001 versus control.

28467797
In vivo Dovitinib induces both cytostatic and cytotoxic responses in vivo resulting in regression of FGFR3-expressing tumors.[1] Dovitinib shows a dose- and exposure-dependent inhibition of target receptor tyrosine kinases (RTKs) expressed in tumor xenografts. Dovitinib potently inhibits tumor growth of six HCC lines. Inhibition of angiogenesis correlated with inactivation of FGFR/PDGFRβ/VEGFR2 signaling pathways. In an orthotopic model, Dovitinib potently inhibits primary tumor growth and lung metastasis and significantly prolonged mouse survival. [2] Administration of Dovitinib results in significant tumor growth inhibition and tumor regressions, including large, established tumors (500-1,000 mm3). [3]

Protocol

Kinase Assay:[1]
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In vitro kinase assays:

The inhibitory concentration of 50% (IC50) values for the inhibition of RTKs by Dovitinib are determined in a time-resolved fluorescence (TRF) or radioactive format, measuring the inhibition by Dovitinib of phosphate transfer to a substrate by the respective enzyme. The kinase domains of FGFR3, FGFR1, PDGFRβ, and VEGFR1-3 are assayed in 50 mM HEPES (N-2-hydroxyethylpiperazine-N-2-ethanesulfonic acid), pH 7.0, 2 mM MgCl2, 10 mM MnCl2 1 mM NaF, 1 mM dithiothreitol (DTT), 1 mg/mL bovine serum albumin (BSA), 0.25 μM biotinylated peptide substrate (GGGGQDGKDYIVLPI), and 1 to 30 μM adenosine triphosphate (ATP) depending on the Km for the respective enzyme. ATP concentrations are at or just below Km. For c-KIT and FLT3 reactions the pH is raised to 7.5 with 0.2 to 8 μM ATP in the presence of 0.25 to 1 μM biotinylated peptide substrate (GGLFDDPSYVNVQNL). Reactions are incubated at room temperature for 1 to 4 hours and the phosphorylated peptide captured on streptavidin-coated microtiter plates containing stop reaction buffer (25 mM EDTA [ethylenediaminetetraacetic acid], 50 mM HEPES, pH 7.5). Phosphorylated peptide is measured with the DELFIA TRF system using a Europium-labeled antiphosphotyrosine antibody PT66. The concentration of Dovitinib for IC50 is calculated using nonlinear regression with XL-Fit data analysis software version 4.1 (IDBS). Inhibition of colony-stimulating factor-1 receptor (CSF-1R), PDGFRα, insulin receptor (InsR), and insulin-like growth factor receptor 1 (IGFR1) kinase activity is determined at ATP concentrations close the Km for ATP.
Cell Research:[1]
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  • Cell lines: B9 cells, MM cell lines
  • Concentrations: 100 nM
  • Incubation Time: 48-96 hours
  • Method: Cell viability is assessed by 3-(4,5-dimethylthiazol)-2,5-diphenyl tetrazolium (MTT) dye absorbance. Cells are seeded in 96-well plates at a density of 5 × 103 (B9 cells) or 2 × 104 (MM cell lines) cells per well. Cells are incubated with 30 ng/mL aFGF and 100 μg/mL heparin or 1% IL-6 where indicated and increasing concentrations of Dovitinib. For each concentration of Dovitinib, 10 μL aliquots of drug or DMSO diluted in culture medium is added. For drug combination studies, cells are incubated with 0.5 μM dexamethasone, 100 nM Dovitinib, or both simultaneously where indicated. To evaluate the effect of Dovitinib on growth of MM cells adherent to BMSCs, 104 KMS11 cells are cultured on BMSC-coated 96-well plates in the presence or absence of Dovitinib. Plates are incubated for 48 to 96 hours. For assessment of macrophage colony-stimulating factor (M-CSF)-mediated growth, 5 × 103 M-NFS-60 cells/well are incubated with serial dilutions of Dovitinib with 10 ng/mL M-CSF and without granulocyte-macrophage colony-stimulating factor (GM-CSF). After 72 hours cell viability is determined using Cell Titer-Glo Assay. Each experimental condition is performed in triplicate.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: 8-week-old female BNX mice bearing KMS11 cells
  • Formulation: 5 mM citrate buffer
  • Dosages: 10, 30, or 60 mg/kg
  • Administration: Gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 30 mg/mL (76.44 mM)
Water Insoluble
Ethanol 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 392.43
Formula

C21H21FN6O

CAS No. 405169-16-6
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02268435 Withdrawn Drug: dovitinib plus imatinib Gastrointestinal Stromal Tumors Asan Medical Center March 2015 Phase 1
NCT01700270 Completed Drug: dovitinib (TKI258)|Drug: fluvoxamine Advanced Solid Tumors Excluding Breast Cancer Novartis Pharmaceuticals|Novartis May 2013 Phase 1
NCT01680796 Withdrawn Drug: Dovitinib|Drug: Bortezomib|Drug: Dexamethasone Multiple Myeloma University of Florida|Novartis Pharmaceuticals February 2013 Phase 1
NCT01266070 Terminated Drug: Dovitinib Von Hippel-Lindau Syndrome M.D. Anderson Cancer Center|Novartis November 2012 Phase 2
NCT01515969 Terminated Drug: Erlotinib hydrochloride|Drug: Dovitinib lactate Non-small Cell Lung Cancer (NSCLC) Recurrent|Non-small Cell Lung Cancer (NSCLC) Stage IV Heather Wakelee|Genentech Inc.|Novartis|Stanford University July 2012 Phase 1
NCT01030055 Completed Drug: TKI258 (dovitinib) Neoplasms|Cancer|Tumors Novartis Pharmaceuticals|Novartis February 2010 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID