Dovitinib (TKI-258)

For research use only.

Catalog No.S1018 Synonyms: CHIR-258

22 publications

Dovitinib (TKI-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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Selleck's Dovitinib (TKI-258) has been cited by 22 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 NHnPR2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\kV5NUUUN3ME2wMlQ1QSEQvF2= M3HXdlI2OjB{MEez
SupB15-R MmnLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTBZpgxUUN3ME2wMlU2QCEQvF2= MV6yOVIxOjB5Mx?=
BaF3-pSRα MnLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfITWM2OD1yLk[2PEDPxE1? MX:yOVIxOjB5Mx?=
BaF3-p210Bcr-Abl M17GXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:3cGdVUUN3ME2wMlY6OiEQvF2= MXKyOVIxOjB5Mx?=
BaF3-p210Bcr-Abl-T315I MmrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTV[VRKSzVyPUKuOlI3KM7:TR?= M2noUFI2OjB{MEez
CCRF-CEM MkfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTBwM{m4JO69VQ>? NX;DUWJmOjV{MEKwO|I>
CEM/C2 M3fNSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTFwMUK1JO69VQ>? MXmyOVIxOjB5Mh?=
Nalm-6 MoLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEWyNI5KSzVyPUCuN|gzKM7:TR?= M37qXlI2OjB{MEey
SEM-K2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwMEKyJO69VQ>? NGnSTGwzPTJyMkC3Ni=>
HB-1119 NIfPfXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jEVGlEPTB;MD6wNlgh|ryP MYmyOVIxOjB5Mh?=
RS4:11 M1O3O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDzTWM2OD1{LkixJO69VQ>? MlzrNlUzODJyN{K=
Nalm-6 NX21ZYF{SXCxcITvd4l{KEG|c3H5 M4jpNlIh|ryP MXSyOE81QCCq MVPpcoR2[2W|IHHwc5B1d3OrczDy[ZN2dHSrbnegbY4h[WKxdYSgO|ImKG:oIHPlcIwh\GWjdHigZYZ1\XJiMkSgbEB1emWjdH3lcpQh[W6mIEixKUBi\nSncjC0PEBp NFq2V5gzPTJyMkC3Ni=>
SEM-K2 MmezRZBweHSxc3nzJGF{e2G7 NXHUZWZkOC5zL{Gg{txO NGKxVVQzPCCq M1[yR4lv\HWlZYOg[YFzdHliYYDvdJRwe2m|IH;mJHNGVS2NMjDj[YxteyCjdDCwMlEh|ryPIHHmeIVzKDJ2IHi= NEjlZ2MzPTJyMkC3Ni=>
HCT-116 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTNwMEWwMlU5KM7:TR?= MWWyOFQ6PTd3MB?=
HT-29 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnLdIhbUUN3ME21MlIyNjl|IN88US=> NH74UpYzPDR7NUe1NC=>
SW-480 NHLON4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LmcmlEPTB;ND6zN|AvPDdizszN MWSyOFQ6PTd3MB?=
CaCO2 MnnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PIbWlEPTB;Mz6yN|AvPjRizszN MlTpNlQ1QTV5NUC=
LS174T M2LrXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzCU2drUUN3ME20MlM{OC52NzFOwG0> NX:wd|VGOjR2OUW3OVA>
HEC-1A MWLGeY5kfGmxbjDBd5NigQ>? NGmySmIxNjB3L{CuNU8xNjVizszN MojKO|IhcA>? MVTjZZV{\XNiYTDk[YNz\WG|ZTDpckBUXEGWMzygSXJMNCCjbnSgRWtVKHCqb4PwbI9zgWyjdHnvci=> NHvnUZozPDR7NUe1NC=>
AN3CA MYnGeY5kfGmxbjDBd5NigQ>? MUCwMlA2NzBwMT:wMlUh|ryP MYi3NkBp Mli3Z4F2e2W|IHGg[IVkemWjc3WgbY4hW1SDVEOsJGVTUyxiYX7kJGFMXCCyaH;zdIhwenmuYYTpc44> MVGyOFQ6PTd3MB?=
MFE-296  M{fHeGZ2dmO2aX;uJGF{e2G7 M2nzbVAvODVxMD6xM|AvPSEQvF2= MlLPO|IhcA>? NX3aRZpN[2G3c3XzJIEh\GWlcnXhd4UhcW5iU2TBWFMtKEWUSzygZY5lKEGNVDDwbI9{eGixconsZZRqd25? MXOyOFQ6PTd3MB?=
UMC3 NXrwblVsS2WubDDWbYFjcWyrdImgRZN{[Xl? MXSxMVExKM7:TR?= NXrscI46PzJiaB?= Mmq5bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NIDWbmgzPDN{NUS2NS=>
5637 MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mln0NU0yOCEQvF2= MXK3NkBp NUfoRZN7cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M1jJT|I1OzJ3NE[x
HU456 Mn\5R4VtdCCYaXHibYxqfHliQYPzZZk> NE\5SFMyNTFyIN88US=> MWG3NkBp MonQbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NGK2W2EzPDN{NUS2NS=>
MGHU4 MXHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnrqNU0yOCEQvF2= NV72eZRtPzJiaB?= NX\RRWl2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M4jCPFI1OzJ3NE[x
HT1376 M4TN[GNmdGxiVnnhZoltcXS7IFHzd4F6 Mn[wNU0yOCEQvF2= M4LRZlczKGh? M{H0eolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MYCyOFMzPTR4MR?=
RT112 NFnGUmZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlH6NU0yOCEQvF2= NV7BOZd2PzJiaB?= MWjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MWmyOFMzPTR4MR?=
T24 NXHr[2lqS2WubDDWbYFjcWyrdImgRZN{[Xl? NXn4Wm1lOS1zMDFOwG0> MXm3NkBp MnX3bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MXiyOFMzPTR4MR?=
BFTC905 M37nUmNmdGxiVnnhZoltcXS7IFHzd4F6 MmDZNU0yOCEQvF2= MX63NkBp MXrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NXPjS3ExOjR|MkW0OlE>
TCC-SUP NXjUbYwzS2WubDDWbYFjcWyrdImgRZN{[Xl? MmnFNU0yOCEQvF2= NG\yVWo4OiCq M3n5OolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NGn0U3AzPDN{NUS2NS=>
RT4 MkToR4VtdCCYaXHibYxqfHliQYPzZZk> MVWxMVExKM7:TR?= MkXvO|IhcA>? MWPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NFfLbmUzPDN{NUS2NS=>
HONE1 NEf4R5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXGSI4xNjFvMUCg{txO MVy0POKhcA>? NUSzemxPcW6mdXPld{BIOi:PIHTlcIF6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MXKyOFI{QDB7NB?=
HNE1 NYXURWh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[4cZZDOC5zLUGwJO69VQ>? MYO0POKhcA>? NHzsS5hqdmS3Y3XzJGczN01iZHXsZZkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MVmyOFI{QDB7NB?=
CNE2  NELac|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rZ[FAvOS1zMDFOwG0> M174d|Q5yqCq M1z5TIlv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> MWmyOFI{QDB7NB?=
C666-1 MoW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLZNE4yNTFyIN88US=> M2j2N|Q5yqCq NYnwW5FMcW6mdXPld{BIOi:PIHTlcIF6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NFXaVIEzPDJ|OEC5OC=>
HeLa NYTheGsxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUmwMlEuOTBizszN M173OlI1KGh? NIXiSIFqdmS3Y3XzJGczN01iYYLy[ZN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NXfHd2RMOjR{M{iwPVQ>
Hep3B NETEfpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPaUIsxNjFvMUCg{txO MlXyNlQhcA>? MnjnbY5lfWOnczDHNuKh[XK{ZYP0xsA> NUOwUVhPOjR{M{iwPVQ>
HepG2 MoLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3n6T|Q5KGh? MYDJR|UxRTJwN{K3JOKyKDBwNEK5JO69VQ>? NU\yOo9FOjN3NE[1PVE>
Hep3B MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXO0PEBp NVf3OpJnUUN3ME20MlIzOyEEsTCwMlg{QSEQvF2= M{DIdFI{PTR4NUmx
PLC/PRF5 NG\z[nZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7ONnlDPDhiaB?= MVTJR|UxRTF4LkGyNEDDuSB2LkCwNUDPxE1? NV7N[|FDOjN3NE[1PVE>
Huh7 MkTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{D6NlQ5KGh? NV35OoVqUUN3ME2xOU4xODdiwsGgO{4{OzRizszN NXzKdI5MOjN3NE[1PVE>
HepG2 MlSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnEPXJnPzJiaB?= MY\JR|UxRTFwMkCwJOKyKDBwMkK2JO69VQ>? MXqyN|U1PjV7MR?=
Hep3B MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkP5O|IhcA>? MVTJR|UxRTBwOEmyJOKyKDBwMES0JO69VQ>? M3PuclI{PTR4NUmx
PLC/PRF5 MlOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXm3NkBp MnL4TWM2OD1|LkGxNEDDuSByLkOzO{DPxE1? MljiNlM2PDZ3OUG=
Huh7 NE\SPJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjGcmM4OiCq M3HDfWlEPTB;Mz65PFAhyrFiMD64NFMh|ryP MWeyN|U1PjV7MR?=
MFE280 NGXaTpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfJTWM2OD1yLkSyJOKyKDBwME[g{txO M4THSVI{PDR|OEC1
AN3CA NUewU5c3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfHT3NKSzVyPUCuOVAhyrFiMD6xNEDPxE1? NWDSZmpCOjN2NEO4NFU>
HEC155 NYrJfIxNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnsTXhKSzVyPUCuOlYhyrFiMD6wPUDPxE1? M2Tmb|I{PDR|OEC1
MFE296 NIiwOnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[3W4dKSzVyPUCuOlYhyrFiMD6xPUDPxE1? NFXNfJQzOzR2M{iwOS=>
SPAC1S M3;WZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFv1OVJKSzVyPUCuO|chyrFiMD6wPEDPxE1? Ml;lNlM1PDN6MEW=
RL952 M13sfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\EdGlEPTB;MD65N{DDuSByLkCxJO69VQ>? MX:yN|Q1OzhyNR?=
EN1 NYSzfml1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLaTWM2OD1zLkCyJOKyKDBwMkWg{txO M1;Sb|I{PDR|OEC1
SNGII NUOzSm1kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjaXG9KSzVyPUGuNlQhyrFiMD6yPEDPxE1? MViyN|Q1OzhyNR?=
ISHIKAWA M1vp[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYO0bINMUUN3ME2xMlMxKMLzIECuNVEh|ryP M3vYb|I{PDR|OEC1
HEC1A NHHhU5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEKxT|JKSzVyPUGuN|QhyrFiMD6zNEDPxE1? NYKz[W9oOjN2NEO4NFU>
KLE M3P3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;yTWM2OD1zLkO3JOKyKDBwMEKg{txO M{j3N|I{PDR|OEC1
SNGM NFXpW2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfQVXRKSzVyPUGuOFIhyrFiMD6xN{DPxE1? M1HrblI{PDR|OEC1
USPC2 NGTD[4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HEZmlEPTB;MT62NkDDuSByLkCxJO69VQ>? MWCyN|Q1OzhyNR?=
EN NXvnWFFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\ZcVhKSzVyPUGuOlYhyrFiMD6wNUDPxE1? M4eyflI{PDR|OEC1
MFE319 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVn4WlBnUUN3ME2xMlg4KMLzIECuOFUh|ryP M3TEPVI{PDR|OEC1
EFE184 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELKPHJKSzVyPUKuNFQhyrFiMD6xN{DPxE1? NV\mbY1QOjN2NEO4NFU>
ECC1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfkdYlKSzVyPUKuNFchyrFiMD6wNUDPxE1? M2X2VVI{PDR|OEC1
HEC1B NXLMTnZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LHO2lEPTB;Mj61O{DDuSByLkKzJO69VQ>? M4TUWVI{PDR|OEC1
USPC1 NF7yVVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHiTWM2OD1{Lk[wJOKyKDBwMUOg{txO M1[2V|I{PDR|OEC1
SPAC1L NF6xdYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlW5TWM2OD1|LkC2JOKyKDFwMUSg{txO MnS5NlM1PDN6MEW=
HUVEC NVqzO3gyS2WubDDWbYFjcWyrdImgRZN{[Xl? NXywcFExOC1{NTFOwG0> NIfoSZg4OiCq NYnEeoJ2TE2VTx?= MoXpbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MofJNlMzOjhyMUe=
HMVEC MnjhR4VtdCCYaXHibYxqfHliQYPzZZk> MVWwMVI2KM7:TR?= M1jKO|czKGh? MX3EUXNQ NI\EV|VqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NWDnNnR4OjN{MkiwNVc>
MHCC-97H NVPUUFlDS2WubDDWbYFjcWyrdImgRZN{[Xl? NUDBXWVQOC1{NTFOwG0> NFiyT2g4OiCq M1fyOGROW09? NHPtV|RqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M4PLdlI{OjJ6MEG3
SMMC7721 MoDGR4VtdCCYaXHibYxqfHliQYPzZZk> NYm4N2liOC1{NTFOwG0> MmXQO|IhcA>? M2jtbGROW09? MX\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M1PSPFI{OjJ6MEG3
Huh-7 NXXtWWF3SXCxcITvd4l{KEG|c3H5 M1m2flAuOTJwNTFOwG0> MnLiNlQhcA>? MlXaSG1UV8Li Mk\Xd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MX[yNlI{ODR5OR?=
Sk-Hep1 NFjHNYxCeG:ydH;zbZMhSXO|YYm= NV[wUXhCOC1zMj61JO69VQ>? Ml\MNlQhcA>? MoTnSG1UV8Li MYnz[Y5{cXSrenXzJGhESyClZXzsd{B1dyCWUlHJUE0h[W6mIITp[4F1fXq3bXHiMYlv\HWlZXSgZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NXG1W5pzOjJ{M{C0O|k>
Hep3B NGq1ZlRCeG:ydH;zbZMhSXO|YYm= MWGwMVEzNjVizszN MnLINlQhcA>? MVLEUXNQyqB? M1O5R5NmdnOrdHn6[ZMhUEOFIHPlcIx{KHSxIGTSRWlNNSCjbnSgeIlo[XS3eoXtZYIucW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NX:ySVFIOjJ{M{C0O|k>
PLC5 NUTNUHJnSXCxcITvd4l{KEG|c3H5 MV6wMVEzNjVizszN NXnJc4JROjRiaB?= MlruSG1UV8Li MkGyd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NWjhZ5JoOjJ{M{C0O|k>
PLC5 MWnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4DY[|AuOTVizszN NHfy[II4OiCq MWry[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? MV6yNlE5ODNyOB?=
Hep3B M2O5emNmdGxiVnnhZoltcXS7IFHzd4F6 NF;tVHgxNTF3IN88US=> MkCyO|IhcA>? M1;1bJJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= M4HHUFIzOThyM{C4
Sk-Hep1 NU\DRoh6S2WubDDWbYFjcWyrdImgRZN{[Xl? MoDnNE0yPSEQvF2= M2Xa[FczKGh? M4fOU5Jm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MWOyNlE5ODNyOB?=
Huh-7 M3z5dmNmdGxiVnnhZoltcXS7IFHzd4F6 MUGwMVE2KM7:TR?= M3PzeFczKGh? MWny[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? MW[yNlE5ODNyOB?=
PLC5 MYrBdI9xfG:|aYOgRZN{[Xl? NGLxeIgxNTF3IN88US=> MUOyOEBp MlfxbY5kemWjc3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? NYDEfItQOjJzOECzNFg>
Hep3B Mo\1RZBweHSxc3nzJGF{e2G7 M2Dn[|AuOTVizszN NGqxPFIzPCCq NYPkbVhVcW6lcnXhd4V{KGGyb4D0c5Rq[yClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M4TUO|IzOThyM{C4
Sk-Hep1 MWDBdI9xfG:|aYOgRZN{[Xl? NW\me|lKOC1zNTFOwG0> MUOyOEBp M3T5N4lv[3KnYYPld{BieG:ydH;0bYMh[2WubDDk[YF1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi MmjmNlIyQDB|MEi=
Huh-7 Mn7MRZBweHSxc3nzJGF{e2G7 MmDnNE0yPSEQvF2= MmPPNlQhcA>? NEXM[nNqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MkLuNlIyQDB|MEi=
PLC5 NVPqPHlsTnWwY4Tpc44hSXO|YYm= NHi4XoIxNTFyIN88US=> Ml[wNlQhcA>? M3zPVoNifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? M3nXeFIzOThyM{C4
Hep3B MXnGeY5kfGmxbjDBd5NigQ>? MmjKNE0yOCEQvF2= MoTjNlQhcA>? MXjjZZV{\XNiZH;z[U1l\XCnbnTlcpQhTE6DIH\yZYdu\W62YYTpc44> MlP6NlIyQDB|MEi=
Sk-Hep1 MWnGeY5kfGmxbjDBd5NigQ>? NHXWdFMxNTFyIN88US=> M3LXbVI1KGh? M{fiR4NifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? NUPueXN{OjJzOECzNFg>
Huh-7 Mnf3SpVv[3Srb36gRZN{[Xl? MYWwMVExKM7:TR?= MWmyOEBp NHW2SpZk[XW|ZYOg[I9{\S2mZYDlcoRmdnRiRF7BJIZz[WevZX70ZZRqd25? MYWyNlE5ODNyOB?=
SW780 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LKWVUh\A>? MXrJR|UxRTVyIH7N NF22WIgzOTFzOU[2NS=>
RT112 NIDhPXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TCUlUh\A>? MkjBTWM2OD1zNTDuUS=> MV2yNVEyQTZ4MR?=
RT4 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DGdVUh\A>? MYnJR|UxRTVibl2= NUfubZVnOjFzMUm2OlE>
JMSU1 M2rzZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVW1JIQ> NYHxcphiUUN3ME21NEBvVQ>? NUGxTpdCOjFzMUm2OlE>
J82 NID6eopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjMU4c2KGR? NF7mdFdKSzVyPUG0NFAhdk1? M3;GOlIyOTF7Nk[x
97-7 NF;kcVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXy1JIQ> Mk\1TWM2OD1zMECwJI5O MYqyNVEyQTZ4MR?=
RT112 NF3ZdZJHfW6ldHnvckBCe3OjeR?= NF23NWo2ODBibl2= M2rMclI1KGh? M1vobolv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= NU\2[2hTOjFzMUm2OlE>
RT4 M3z6O2Z2dmO2aX;uJGF{e2G7 NI\0fmQ2ODBibl2= M2fMTlI1KGh? M3jT[Ylv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= M2\RTlIyOTF7Nk[x
MGH-U3 MVLGeY5kfGmxbjDBd5NigQ>? NG\PT5U2ODBibl2= MmC5NlQhcA>? NYCxc2V2cW6lcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKEdzwrDhZ4NwdXCjbnnl[EBjgSCjIHTlZ5Jm[XOnIHnuJHMh[W6mIFeyM20heGijc3Xz MX[yNVEyQTZ4MR?=
SW780 M1TSemZ2dmO2aX;uJGF{e2G7 MYi1NFAhdk1? M4[yWFI1KGh? NGn3NJFqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= NFjrNW8zOTFzOU[2NS=>
97-7 NF\6bHpHfW6ldHnvckBCe3OjeR?= NGTaUog2ODBibl2= MkO5NlQhcA>? MnLDbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| M4\UZVIyOTF7Nk[x
 J807C M2G4OWNmdGxiVnnhZoltcXS7IFHzd4F6 M3rhdFAuPDByIH7N MnjGOFghcA>? MVjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NGTQXY0yPTV7OEixOC=>
Y373C NULFXm56S2WubDDWbYFjcWyrdImgRZN{[Xl? MXWwMVQxOCCwTR?= MVS0PEBp NEmwZlJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M4fzUlE2PTl6OEG0
K650E NXHGPG81S2WubDDWbYFjcWyrdImgRZN{[Xl? MUewMVQxOCCwTR?= NWPCTnpNPDhiaB?= Ml7PbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MVqxOVU6QDhzNB?=
G384D NHnjd4NE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1XMe|AuPDByIH7N NX30d4JIPDhiaB?= M4TySolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NV3yfHJSOTV3OUi4NVQ>
F384L NUf2RohxS2WubDDWbYFjcWyrdImgRZN{[Xl? NVmyNoVjOC12MECgcm0> NXT3UmVZPDhiaB?= MlzCbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> Mnf0NVU2QTh6MUS=
KMS11 MnzIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3ZSZlQPzJiaB?= NWTPWZRkUUN3ME25NEBvVQ>? MY[xOVU6QDhzNB?=
KMS18 M3qxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3LO|IhcA>? MWTJR|UxRTV3MDDuUS=> NI[5WYkyPTV7OEixOC=>
OPM2 NFLqTJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13pOlczKGh? NVP0[Wd3UUN3ME25NEBvVQ>? NXnVTZpxOTV3OUi4NVQ>
H929 MnLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\1SlczKGh? MmrwTWM2OD5iMkWwNEBvVQ>? MUOxOVU6QDhzNB?=
8226 NYDNcHp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TzdVczKGh? NXzPRnVoUUN3ME6gNlUxOCCwTR?= MoKyNVU2QTh6MUS=
U266 NWSyUmJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;rSIk4OiCq Ml33TWM2OD5iMkWwNEBvVQ>? MWOxOVU6QDhzNB?=

... 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
  • 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 CHIR-258
Smiles CN1CCN(CC1)C2=CC3=C(C=C2)N=C([NH]3)C4=C(N)C5=C(NC4=O)C=CC=C5F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

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  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID