Dovitinib (TKI-258)

For research use only.

Catalog No.S1018 Synonyms: CHIR-258

24 publications

Dovitinib (TKI-258) Chemical Structure

CAS No. 405169-16-6

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 24 publications

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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 NVjucmRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mni4TWM2OD1yLkS0PUDPxE1? Mn32NlUzODJyN{O=
SupB15-R MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlv0TWM2OD1yLkW1PEDPxE1? Mke3NlUzODJyN{O=
BaF3-pSRα Mle2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvOVWZ5UUN3ME2wMlY3QCEQvF2= NY\oOmMxOjV{MEKwO|M>
BaF3-p210Bcr-Abl NEXkb5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PDd2lEPTB;MD62PVIh|ryP M1\STlI2OjB{MEez
BaF3-p210Bcr-Abl-T315I NHrQfGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HYRWlEPTB;Mj62NlYh|ryP M3nGSFI2OjB{MEez
CCRF-CEM NFHSfXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwM{m4JO69VQ>? NIHQO|kzPTJyMkC3Ni=>
CEM/C2 M37HPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2T3bWlEPTB;MT6xNlUh|ryP Mon1NlUzODJyN{K=
Nalm-6 NGjQbWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoWzTWM2OD1yLkO4NkDPxE1? NYHISJVmOjV{MEKwO|I>
SEM-K2 M{XVVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTBwMEKyJO69VQ>? MYSyOVIxOjB5Mh?=
HB-1119 M1HT[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTBwMEK4JO69VQ>? MmL0NlUzODJyN{K=
RS4:11 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\PRphMUUN3ME2yMlgyKM7:TR?= M2PIV|I2OjB{MEey
Nalm-6 M4S3SmFxd3C2b4Ppd{BCe3OjeR?= MXeyJO69VQ>? M1WzTFI1NzR6IHi= NWnDO|U3cW6mdXPld{BieG:ydH;zbZMhemW|dXz0bY5oKGmwIHHic5V1KDd{JTDv[kBk\WyuIHTlZZRpKGGodHXyJFI1KGhidILlZZRu\W62IHHu[EA5OSViYX\0[ZIhPDhiaB?= NV7UNWFJOjV{MEKwO|I>
SEM-K2 NYWzN3IxSXCxcITvd4l{KEG|c3H5 NIO4V5cxNjFxMTFOwG0> NELH[FYzPCCq MnjabY5lfWOnczDlZZJtgSCjcH;weI9{cXNib3[gV2VONUt{IHPlcIx{KGG2IECuNUDPxE1iYX\0[ZIhOjRiaB?= MoSwNlUzODJyN{K=
HCT-116 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjRXJBKSzVyPUOuNFUxNjV6IN88US=> MYeyOFQ6PTd3MB?=
HT-29 MnHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rGb2lEPTB;NT6yNU46OyEQvF2= MVWyOFQ6PTd3MB?=
SW-480 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTRwM{OwMlQ4KM7:TR?= NGDYUGIzPDR7NUe1NC=>
CaCO2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\BW2VKSzVyPUOuNlMxNjZ2IN88US=> M3TYSVI1PDl3N{Ww
LS174T NUDsUVNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTGUXJKSzVyPUSuN|MxNjR5IN88US=> NVrwV4tuOjR2OUW3OVA>
HEC-1A M3vVRmZ2dmO2aX;uJGF{e2G7 MoLTNE4xPS9yLkGvNE42KM7:TR?= NHvDRlQ4OiCq Mn3JZ4F2e2W|IHGg[IVkemWjc3WgbY4hW1SDVEOsJGVTUyxiYX7kJGFMXCCyaH;zdIhwenmuYYTpc44> M3XLPFI1PDl3N{Ww
AN3CA M4\QNGZ2dmO2aX;uJGF{e2G7 NHvvZ|YxNjB3L{CuNU8xNjVizszN NX20eFVJPzJiaB?= M1fpWINifXOnczDhJIRm[3KnYYPlJIlvKFOWQWSzMEBGWktuIHHu[EBCU1RicHjvd5Bpd3K7bHH0bY9v NVf3SWQ3OjR2OUW3OVA>
MFE-296  M3TRV2Z2dmO2aX;uJGF{e2G7 NHTkbJExNjB3L{CuNU8xNjVizszN Mnv1O|IhcA>? MkLZZ4F2e2W|IHGg[IVkemWjc3WgbY4hW1SDVEOsJGVTUyxiYX7kJGFMXCCyaH;zdIhwenmuYYTpc44> MkXqNlQ1QTV5NUC=
UMC3 M3nmTmNmdGxiVnnhZoltcXS7IFHzd4F6 MmGzNU0yOCEQvF2= M1TO[|czKGh? NEXMZm9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHLuO4MzPDN{NUS2NS=>
5637 MkfsR4VtdCCYaXHibYxqfHliQYPzZZk> NWDvR3ZSOS1zMDFOwG0> MkHzO|IhcA>? NH\JbG1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M4K0UFI1OzJ3NE[x
HU456 NYfiPJFRS2WubDDWbYFjcWyrdImgRZN{[Xl? MonlNU0yOCEQvF2= Ml3tO|IhcA>? MnOybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NUHnUGtUOjR|MkW0OlE>
MGHU4 NYLqR5pGS2WubDDWbYFjcWyrdImgRZN{[Xl? NXe3Z3ZuOS1zMDFOwG0> NUjjZ2xXPzJiaB?= MUDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NF;LW2czPDN{NUS2NS=>
HT1376 M1PQSWNmdGxiVnnhZoltcXS7IFHzd4F6 NYewb4JVOS1zMDFOwG0> MXm3NkBp NYfjZ4lxcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NX;mc5pYOjR|MkW0OlE>
RT112 NVrRWGMzS2WubDDWbYFjcWyrdImgRZN{[Xl? MWqxMVExKM7:TR?= NHPJb3o4OiCq NEXlb5dqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MlGzNlQ{OjV2NkG=
T24 NXjTO2dnS2WubDDWbYFjcWyrdImgRZN{[Xl? MoDFNU0yOCEQvF2= NYHB[W8xPzJiaB?= MmnTbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> Mn\FNlQ{OjV2NkG=
BFTC905 MUXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVexMVExKM7:TR?= M2XDeVczKGh? M{T5PYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M{O0OFI1OzJ3NE[x
TCC-SUP NITydZNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3KyV|EuOTBizszN MoXQO|IhcA>? NYCwZld6cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NVHKTmVDOjR|MkW0OlE>
RT4 M4XIdGNmdGxiVnnhZoltcXS7IFHzd4F6 M2nh[FEuOTBizszN Ml\hO|IhcA>? MW\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M1vYR|I1OzJ3NE[x
HONE1 M4W4NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[wMlEuOTBizszN M2jVOFQ5yqCq MoXBbY5lfWOnczDHNk9OKGSnbHH5JIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy NIrPR|QzPDJ|OEC5OC=>
HNE1 NH\wUGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWewMlEuOTBizszN M3rqUVQ5yqCq M3uyWIlv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> M1rhcFI1OjN6MEm0
CNE2  NHXsfGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nsS|AvOS1zMDFOwG0> M2DDbFQ5yqCq MWnpcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= MmXONlQzOzhyOUS=
C666-1 NIrZRWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjKNE4yNTFyIN88US=> MX:0POKhcA>? MnXGbY5lfWOnczDHNk9OKGSnbHH5JIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy M13pZVI1OjN6MEm0
HeLa MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mme0NE4yNTFyIN88US=> MlGwNlQhcA>? M3O2NIlv\HWlZYOgS|IwVSCjcoLld5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> M1PIOlI1OjN6MEm0
Hep3B NFHtSYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7KNE4yNTFyIN88US=> NHm5OWozPCCq MWPpcoR2[2W|IFeyxsBienKnc4VCpC=> NEPWe|czPDJ|OEC5OC=>
HepG2 NELBdoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWS0PEBp MUPJR|UxRTJwN{K3JOKyKDBwNEK5JO69VQ>? M4XP[FI{PTR4NUmx
Hep3B NWfmOm8xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYG0PEBp MWfJR|UxRTRwMkKzJOKyKDBwOEO5JO69VQ>? NVHKb4NJOjN3NE[1PVE>
PLC/PRF5 MmLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7BOFghcA>? NFXBO29KSzVyPUG2MlEzOCEEsTC0MlAxOSEQvF2= NYPSR2xQOjN3NE[1PVE>
Huh7 NH7oRmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2T3TVQ5KGh? MmTmTWM2OD1zNT6wNFchyrFiNz6zN|Qh|ryP NWH0NWJKOjN3NE[1PVE>
HepG2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4ezU|czKGh? M3LaT2lEPTB;MT6yNFAhyrFiMD6yNlYh|ryP MUiyN|U1PjV7MR?=
Hep3B MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HDdFczKGh? NXnZPYNoUUN3ME2wMlg6OiEEsTCwMlA1PCEQvF2= MXeyN|U1PjV7MR?=
PLC/PRF5 MlHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorpO|IhcA>? MUPJR|UxRTNwMUGwJOKyKDBwM{O3JO69VQ>? NVLF[olVOjN3NE[1PVE>
Huh7 M2XzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zsT|czKGh? NWG3VYp1UUN3ME2zMlk5OCEEsTCwMlgxOyEQvF2= MV[yN|U1PjV7MR?=
MFE280 NVzvOHc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWm1V2MyUUN3ME2wMlQzKMLzIECuNFYh|ryP MX[yN|Q1OzhyNR?=
AN3CA NFLuZnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvSW5FWUUN3ME2wMlUxKMLzIECuNVAh|ryP Mo\pNlM1PDN6MEW=
HEC155 NHi3WpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorsTWM2OD1yLk[2JOKyKDBwMEmg{txO MVOyN|Q1OzhyNR?=
MFE296 MnPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moi3TWM2OD1yLk[2JOKyKDBwMUmg{txO NYH6TVBLOjN2NEO4NFU>
SPAC1S MmjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3CTWM2OD1yLke3JOKyKDBwMEig{txO MoLYNlM1PDN6MEW=
RL952 M1vSSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fNVGlEPTB;MD65N{DDuSByLkCxJO69VQ>? MmTCNlM1PDN6MEW=
EN1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzaN|F6UUN3ME2xMlAzKMLzIECuNlUh|ryP NXqwPWllOjN2NEO4NFU>
SNGII MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvJV|BtUUN3ME2xMlI1KMLzIECuNlgh|ryP NH3QR|EzOzR2M{iwOS=>
ISHIKAWA NWjBcGRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jwNGlEPTB;MT6zNEDDuSByLkGxJO69VQ>? NYLkcXhbOjN2NEO4NFU>
HEC1A MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3nTWM2OD1zLkO0JOKyKDBwM{Cg{txO MVOyN|Q1OzhyNR?=
KLE NEDRfVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXGTWM2OD1zLkO3JOKyKDBwMEKg{txO MlHoNlM1PDN6MEW=
SNGM NECwfXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHewXVFKSzVyPUGuOFIhyrFiMD6xN{DPxE1? MlzTNlM1PDN6MEW=
USPC2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoGxTWM2OD1zLk[yJOKyKDBwMEGg{txO MYSyN|Q1OzhyNR?=
EN NVT2ZnpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPpTWM2OD1zLk[2JOKyKDBwMEGg{txO MoGxNlM1PDN6MEW=
MFE319 NXHXNolbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYq3UFhNUUN3ME2xMlg4KMLzIECuOFUh|ryP NETNV3AzOzR2M{iwOS=>
EFE184 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XaTmlEPTB;Mj6wOEDDuSByLkGzJO69VQ>? MmrXNlM1PDN6MEW=
ECC1 M3fCcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PtR2lEPTB;Mj6wO{DDuSByLkCxJO69VQ>? NVTWWItLOjN2NEO4NFU>
HEC1B MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTDfJl5UUN3ME2yMlU4KMLzIECuNlMh|ryP NHz2XWczOzR2M{iwOS=>
USPC1 NIq0S3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHi5W2xKSzVyPUKuOlAhyrFiMD6xN{DPxE1? NXvnSJhbOjN2NEO4NFU>
SPAC1L MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXOe2RSUUN3ME2zMlA3KMLzIEGuNVQh|ryP NYDpUm52OjN2NEO4NFU>
HUVEC NGL1PXlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MV:wMVI2KM7:TR?= MUO3NkBp MmqzSG1UVw>? MoLMbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M4TzTFI{OjJ6MEG3
HMVEC MX3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MoTYNE0zPSEQvF2= MYi3NkBp MXvEUXNQ MWLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NVrzToVUOjN{MkiwNVc>
MHCC-97H NVnQbnFDS2WubDDWbYFjcWyrdImgRZN{[Xl? MnftNE0zPSEQvF2= NXPnR3VGPzJiaB?= M2XWTmROW09? NInHXJdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NUTFN3UxOjN{MkiwNVc>
SMMC7721 MoK2R4VtdCCYaXHibYxqfHliQYPzZZk> NW[ybHpqOC1{NTFOwG0> NEe0Z|I4OiCq M3\NbGROW09? M1\GSIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz Mlm3NlMzOjhyMUe=
Huh-7 NX;DOoNRSXCxcITvd4l{KEG|c3H5 M4izWVAuOTJwNTFOwG0> M1vsRVI1KGh? Mm\4SG1UV8Li NXm1RlFbe2Wwc3n0bZpmeyCKQ1OgZ4VtdHNidH:gWHJCUUxvIHHu[EB1cWejdIX6eY1i[i2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NV3JWZhuOjJ{M{C0O|k>
Sk-Hep1 Mlf1RZBweHSxc3nzJGF{e2G7 NHi5eo4xNTF{LkWg{txO MX[yOEBp MlTiSG1UV8Li M{LRNJNmdnOrdHn6[ZMhUEOFIHPlcIx{KHSxIGTSRWlNNSCjbnSgeIlo[XS3eoXtZYIucW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MV2yNlI{ODR5OR?=
Hep3B NHfKb4VCeG:ydH;zbZMhSXO|YYm= NXvmOmlmOC1zMj61JO69VQ>? M37DNVI1KGh? NX;XTWJjTE2VT9Mg MWDz[Y5{cXSrenXzJGhESyClZXzsd{B1dyCWUlHJUE0h[W6mIITp[4F1fXq3bXHiMYlv\HWlZXSgZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NVLNVYVMOjJ{M{C0O|k>
PLC5 MoKwRZBweHSxc3nzJGF{e2G7 NYfLPIM{OC1zMj61JO69VQ>? MXSyOEBp NGDQblJFVVORwrC= Mlr2d4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NX7zOXlbOjJ{M{C0O|k>
PLC5 M3u0OmNmdGxiVnnhZoltcXS7IFHzd4F6 M3TnSVAuOTVizszN MWm3NkBp MVny[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? Ml:5NlIyQDB|MEi=
Hep3B NIXvVpNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGHiSVExNTF3IN88US=> NXXBZY06PzJiaB?= M3;jcZJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= Mn;BNlIyQDB|MEi=
Sk-Hep1 M{XqTWNmdGxiVnnhZoltcXS7IFHzd4F6 MVWwMVE2KM7:TR?= M1XnbFczKGh? NILX[2Zz\WS3Y3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= NF3GOFIzOjF6MEOwPC=>
Huh-7 NETveXpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXiwMVE2KM7:TR?= NHrQZ2k4OiCq M2PqeZJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NHzofGIzOjF6MEOwPC=>
PLC5 NWjXSINxSXCxcITvd4l{KEG|c3H5 NFXoW2oxNTF3IN88US=> M37PfVI1KGh? M1jEZYlv[3KnYYPld{BieG:ydH;0bYMh[2WubDDk[YF1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi Ml;PNlIyQDB|MEi=
Hep3B NHWyRYVCeG:ydH;zbZMhSXO|YYm= M1;JT|AuOTVizszN MVKyOEBp NF\ZdVJqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MVOyNlE5ODNyOB?=
Sk-Hep1 NULFXY1bSXCxcITvd4l{KEG|c3H5 MonUNE0yPSEQvF2= MnLPNlQhcA>? MXnpcoNz\WG|ZYOgZZBweHSxdHnjJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZLDqA>? MYmyNlE5ODNyOB?=
Huh-7 MlTlRZBweHSxc3nzJGF{e2G7 MWOwMVE2KM7:TR?= NWLIXIg5OjRiaB?= MUjpcoNz\WG|ZYOgZZBweHSxdHnjJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZLDqA>? MYeyNlE5ODNyOB?=
PLC5 NH\yWlJHfW6ldHnvckBCe3OjeR?= MkTFNE0yOCEQvF2= NGD0XVUzPCCq M1fZTYNifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? NH[yPYwzOjF6MEOwPC=>
Hep3B NHWyPHdHfW6ldHnvckBCe3OjeR?= NX2zPW9iOC1zMDFOwG0> M4DtZVI1KGh? MYjjZZV{\XNiZH;z[U1l\XCnbnTlcpQhTE6DIH\yZYdu\W62YYTpc44> NV\nVXJuOjJzOECzNFg>
Sk-Hep1 NIXNboFHfW6ldHnvckBCe3OjeR?= NVqxNHJGOC1zMDFOwG0> NUXhfINXOjRiaB?= MVrjZZV{\XNiZH;z[U1l\XCnbnTlcpQhTE6DIH\yZYdu\W62YYTpc44> MVOyNlE5ODNyOB?=
Huh-7 NV:4boNVTnWwY4Tpc44hSXO|YYm= MkLVNE0yOCEQvF2= NYK0RXFFOjRiaB?= M1;yWoNifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? NIfrb4czOjF6MEOwPC=>
SW780 MoLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rNcFUh\A>? NXrSbWI3UUN3ME21NEBvVQ>? MViyNVEyQTZ4MR?=
RT112 NHPBUHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnzTmJjPSCm NX;M[4dOUUN3ME2xOUBvVQ>? MUKyNVEyQTZ4MR?=
RT4 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUe1JIQ> NXfZSpVbUUN3ME21JI5O NIPHSo4zOTFzOU[2NS=>
JMSU1 MojNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPy[nJQPSCm NXjmSYQyUUN3ME21NEBvVQ>? M2\sdFIyOTF7Nk[x
J82 M2G2N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTBN4w2KGR? NXrlVllSUUN3ME2xOFAxKG6P M1v2TVIyOTF7Nk[x
97-7 MkizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVz1NGg1PSCm MoTFTWM2OD1zMECwJI5O MnHyNlEyOTl4NkG=
RT112 Mle0SpVv[3Srb36gRZN{[Xl? MkjPOVAxKG6P NVXmZ2RROjRiaB?= MnLobY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| NGG3XGozOTFzOU[2NS=>
RT4 MUfGeY5kfGmxbjDBd5NigQ>? NFj1bZc2ODBibl2= MnLVNlQhcA>? Ml3rbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| NW\oVYxTOjFzMUm2OlE>
MGH-U3 NVezO4dYTnWwY4Tpc44hSXO|YYm= M2Syb|UxOCCwTR?= M4DxeFI1KGh? MofqbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| Ml;lNlEyOTl4NkG=
SW780 MUXGeY5kfGmxbjDBd5NigQ>? NFLZToQ2ODBibl2= M3;xfVI1KGh? NX\qcXRzcW6lcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKEdzwrDhZ4NwdXCjbnnl[EBjgSCjIHTlZ5Jm[XOnIHnuJHMh[W6mIFeyM20heGijc3Xz MnfyNlEyOTl4NkG=
97-7 NYD3V|R{TnWwY4Tpc44hSXO|YYm= M1GwOlUxOCCwTR?= NXX6d49wOjRiaB?= M1Xy[Ylv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= MkDhNlEyOTl4NkG=
 J807C NHHpTItE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MX6wMVQxOCCwTR?= M3ztdlQ5KGh? NY\rOmNicW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NEjobpkyPTV7OEixOC=>
Y373C NFW1ZnZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYGwMVQxOCCwTR?= NWHMS|IyPDhiaB?= M3LCUolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MU[xOVU6QDhzNB?=
K650E M1fPRWNmdGxiVnnhZoltcXS7IFHzd4F6 MkDtNE01ODBibl2= MnnzOFghcA>? MnTEbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MVyxOVU6QDhzNB?=
G384D MWrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGrzb5oxNTRyMDDuUS=> MX60PEBp NWS1ZXFucW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M4\CfVE2PTl6OEG0
F384L MoO2R4VtdCCYaXHibYxqfHliQYPzZZk> M2\mN|AuPDByIH7N MkXuOFghcA>? MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> Ml3kNVU2QTh6MUS=
KMS11 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nUSlczKGh? NGfwfHVKSzVyPUmwJI5O M3vDeFE2PTl6OEG0
KMS18 MoDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWC3NkBp MlG2TWM2OD13NUCgcm0> M4XOclE2PTl6OEG0
OPM2 NUT5OFRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\SO|IhcA>? MlPhTWM2OD17MDDuUS=> NF65PJkyPTV7OEixOC=>
H929 NX74dohtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkT0O|IhcA>? NIDoUY9KSzVyPjCyOVAxKG6P Mm[4NVU2QTh6MUS=
8226 M2LxRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXy3NkBp NHH4cYFKSzVyPjCyOVAxKG6P MojrNVU2QTh6MUS=
U266 Mnf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELVcIo4OiCq NUjXPIdEUUN3ME6gNlUxOCCwTR?= NIPRR|EyPTV7OEixOC=>

... 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(N3)C4=C(C5=C(C=CC=C5F)NC4=O)N

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 ()
% 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 )

  • C1
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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

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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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