Dovitinib (TKI-258)

For research use only.

Catalog No.S1018 Synonyms: CHIR-258

35 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 35 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 NFjCVVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorwTWM2OD1yLkS0PUDPxE1? NWS1OmZyOjV{MEKwO|M>
SupB15-R NGnTZWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTBwNUW4JO69VQ>? M2npclI2OjB{MEez
BaF3-pSRα NGrIeI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUOzWZBrUUN3ME2wMlY3QCEQvF2= MnWxNlUzODJyN{O=
BaF3-p210Bcr-Abl NE\ObnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLucI5KSzVyPUCuOlkzKM7:TR?= Mlu0NlUzODJyN{O=
BaF3-p210Bcr-Abl-T315I MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1e5PWlEPTB;Mj62NlYh|ryP M4f4WVI2OjB{MEez
CCRF-CEM MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWj0OJZVUUN3ME2wMlM6QCEQvF2= MYKyOVIxOjB5Mh?=
CEM/C2 M4raTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LXZWlEPTB;MT6xNlUh|ryP M1u0TFI2OjB{MEey
Nalm-6 M3rU[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLZTWM2OD1yLkO4NkDPxE1? Mn;PNlUzODJyN{K=
SEM-K2 MnXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEH0SpZKSzVyPUCuNFIzKM7:TR?= M2rOTFI2OjB{MEey
HB-1119 NFTWTG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vZTWlEPTB;MD6wNlgh|ryP NHrVS5czPTJyMkC3Ni=>
RS4:11 MmXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJwOEGg{txO NHzEdZUzPTJyMkC3Ni=>
Nalm-6 MVnBdI9xfG:|aYOgRZN{[Xl? M4G0Z|Ih|ryP NYPjRWdxOjRxNEigbC=> MoX5bY5lfWOnczDhdI9xfG:|aYOgdoV{fWy2aX7nJIlvKGGkb4X0JFczLSCxZjDj[YxtKGSnYYToJIFnfGW{IEK0JIghfHKnYYTt[Y51KGGwZDC4NUUh[W[2ZYKgOFghcA>? NV7ETmdzOjV{MEKwO|I>
SEM-K2 NHPCfFNCeG:ydH;zbZMhSXO|YYm= MlnYNE4yNzFizszN M3PvWlI1KGh? MmnobY5lfWOnczDlZZJtgSCjcH;weI9{cXNib3[gV2VONUt{IHPlcIx{KGG2IECuNUDPxE1iYX\0[ZIhOjRiaB?= MkHoNlUzODJyN{K=
HCT-116 NHzjSHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnLTWM2OD1|LkC1NE42QCEQvF2= NU\ZdHZWOjR2OUW3OVA>
HT-29 NV\qNnNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3f1fmlEPTB;NT6yNU46OyEQvF2= M1TVW|I1PDl3N{Ww
SW-480 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\wTWM2OD12LkOzNE41PyEQvF2= NFjMZnMzPDR7NUe1NC=>
CaCO2 NG\0WHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULIe3FJUUN3ME2zMlI{OC54NDFOwG0> MnfRNlQ1QTV5NUC=
LS174T NV:1UXBxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnL4TWM2OD12LkOzNE41PyEQvF2= NXLifGo5OjR2OUW3OVA>
HEC-1A MVXGeY5kfGmxbjDBd5NigQ>? NXfobGlkOC5yNT:wMlEwOC53IN88US=> NXXDOphHPzJiaB?= NGrqPXdk[XW|ZYOgZUBl\WO{ZXHz[UBqdiCVVFHUN{whTVKNLDDhcoQhSUuWIIDoc5NxcG:{eXzheIlwdg>? MkXFNlQ1QTV5NUC=
AN3CA M4rp[WZ2dmO2aX;uJGF{e2G7 MoK1NE4xPS9yLkGvNE42KM7:TR?= NXPpOVFjPzJiaB?= Mm\5Z4F2e2W|IHGg[IVkemWjc3WgbY4hW1SDVEOsJGVTUyxiYX7kJGFMXCCyaH;zdIhwenmuYYTpc44> M3WxO|I1PDl3N{Ww
MFE-296  MV\GeY5kfGmxbjDBd5NigQ>? NYXBRXk2OC5yNT:wMlEwOC53IN88US=> M{fiOlczKGh? NIT5Z3Bk[XW|ZYOgZUBl\WO{ZXHz[UBqdiCVVFHUN{whTVKNLDDhcoQhSUuWIIDoc5NxcG:{eXzheIlwdg>? NEL1fYczPDR7NUe1NC=>
UMC3 NGD0TIxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXSxMVExKM7:TR?= M3zaNlczKGh? M3rYdYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NVe4WZc6OjR|MkW0OlE>
5637 NITX[4hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M33sWVEuOTBizszN MXS3NkBp NE\KboVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NIX4SJgzPDN{NUS2NS=>
HU456 NInKUXBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHzpd2MyNTFyIN88US=> NYXiR5RmPzJiaB?= MmrWbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NXLEbJBEOjR|MkW0OlE>
MGHU4 M3rIPWNmdGxiVnnhZoltcXS7IFHzd4F6 NW\KWGk3OS1zMDFOwG0> MYS3NkBp M{XSUYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NVHjV4x4OjR|MkW0OlE>
HT1376 MmXkR4VtdCCYaXHibYxqfHliQYPzZZk> M13jdVEuOTBizszN NIHDOJY4OiCq MVnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NHX6[5QzPDN{NUS2NS=>
RT112 MoTtR4VtdCCYaXHibYxqfHliQYPzZZk> MWSxMVExKM7:TR?= NX2zXolsPzJiaB?= MnnibY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MU[yOFMzPTR4MR?=
T24 MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3fNcVEuOTBizszN Ml2xO|IhcA>? M2G2VolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NYnaTXF3OjR|MkW0OlE>
BFTC905 NUW1em5GS2WubDDWbYFjcWyrdImgRZN{[Xl? MnXmNU0yOCEQvF2= NYTZSplnPzJiaB?= NH;z[GtqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MUSyOFMzPTR4MR?=
TCC-SUP M2DqVmNmdGxiVnnhZoltcXS7IFHzd4F6 MYCxMVExKM7:TR?= NWThNnY1PzJiaB?= NWnoSmVzcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MX[yOFMzPTR4MR?=
RT4 M1z4T2NmdGxiVnnhZoltcXS7IFHzd4F6 M1XKVFEuOTBizszN MUi3NkBp M1fVPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M1z3RlI1OzJ3NE[x
HONE1 NHLUdWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLqUZQyOC5zLUGwJO69VQ>? NX\5RnZLPDkEoHi= MUDpcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= M4WwTFI1OjN6MEm0
HNE1 M1rXRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LaVlAvOS1zMDFOwG0> Mn\yOFjDqGh? MUDpcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= NXjtNJV1OjR{M{iwPVQ>
CNE2  MkHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\NNE4yNTFyIN88US=> M1nVNFQ5yqCq MW\pcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= MXmyOFI{QDB7NB?=
C666-1 MkX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFruNXcxNjFvMUCg{txO NF;rTIU1QMLiaB?= MXzpcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= MVeyOFI{QDB7NB?=
HeLa MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHewTYsxNjFvMUCg{txO M1rne|I1KGh? MU\pcoR2[2W|IFeyM20h[XK{ZYP0JIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy MUOyOFI{QDB7NB?=
Hep3B NWHaeHplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWCwMlEuOTBizszN M3jVSlI1KGh? NH\RfJVqdmS3Y3XzJGczyqCjcoLld5TDqA>? NFfUcIMzPDJ|OEC5OC=>
HepG2 M3P4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlz1OFghcA>? NWL4WXU{UUN3ME2yMlczPyEEsTCwMlQzQSEQvF2= NGDoWm8zOzV2NkW5NS=>
Hep3B M4nmcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[0PEBp MXPJR|UxRTRwMkKzJOKyKDBwOEO5JO69VQ>? MV2yN|U1PjV7MR?=
PLC/PRF5 NVWwZW9JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3wfGZMPDhiaB?= NIeyOY5KSzVyPUG2MlEzOCEEsTC0MlAxOSEQvF2= NWPq[Gl3OjN3NE[1PVE>
Huh7 Mn3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7ZXXI1QCCq NELrNZpKSzVyPUG1MlAxPyEEsTC3MlM{PCEQvF2= NVXQeYN7OjN3NE[1PVE>
HepG2 M1yy[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfzW2R4PzJiaB?= NVvGPWhZUUN3ME2xMlIxOCEEsTCwMlIzPiEQvF2= M1nSdFI{PTR4NUmx
Hep3B NX\xeVdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXO3NkBp M{HYOmlEPTB;MD64PVIhyrFiMD6wOFQh|ryP NGLyNXYzOzV2NkW5NS=>
PLC/PRF5 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rTc|czKGh? NHzvTY9KSzVyPUOuNVExKMLzIECuN|M4KM7:TR?= MUeyN|U1PjV7MR?=
Huh7 M3HPVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXm5d|hXPzJiaB?= M1PzOWlEPTB;Mz65PFAhyrFiMD64NFMh|ryP NIq1UIMzOzV2NkW5NS=>
MFE280 MnTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTBwNEKgxtEhOC5yNjFOwG0> NWfXSndoOjN2NEO4NFU>
AN3CA NHm5dZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVf5UodSUUN3ME2wMlUxKMLzIECuNVAh|ryP NWfucXJpOjN2NEO4NFU>
HEC155 NEC4V2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLEOYt3UUN3ME2wMlY3KMLzIECuNFkh|ryP MWmyN|Q1OzhyNR?=
MFE296 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnxTWhKSzVyPUCuOlYhyrFiMD6xPUDPxE1? MkXRNlM1PDN6MEW=
SPAC1S MlH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYraNJY3UUN3ME2wMlc4KMLzIECuNFgh|ryP M2rTSFI{PDR|OEC1
RL952 M2HWOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{O1dWlEPTB;MD65N{DDuSByLkCxJO69VQ>? NITFS4szOzR2M{iwOS=>
EN1 NILnOoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTFwMEKgxtEhOC5{NTFOwG0> M3e4S|I{PDR|OEC1
SNGII MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojqTWM2OD1zLkK0JOKyKDBwMkig{txO NVTQUJB1OjN2NEO4NFU>
ISHIKAWA M4jTXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jU[GlEPTB;MT6zNEDDuSByLkGxJO69VQ>? MlzXNlM1PDN6MEW=
HEC1A NET1PGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{GyfWlEPTB;MT6zOEDDuSByLkOwJO69VQ>? NGfwbIozOzR2M{iwOS=>
KLE MlPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHnTWM2OD1zLkO3JOKyKDBwMEKg{txO MmTENlM1PDN6MEW=
SNGM NUn2Z|hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rodWlEPTB;MT60NkDDuSByLkGzJO69VQ>? NUTaUGxlOjN2NEO4NFU>
USPC2 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPSTWM2OD1zLk[yJOKyKDBwMEGg{txO NGX1[XMzOzR2M{iwOS=>
EN M{HpWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUmyZWI{UUN3ME2xMlY3KMLzIECuNFEh|ryP M2DDZ|I{PDR|OEC1
MFE319 Mn;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILUWJBKSzVyPUGuPFchyrFiMD60OUDPxE1? NVXPZlMyOjN2NEO4NFU>
EFE184 NXvNb4NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml2yTWM2OD1{LkC0JOKyKDBwMUOg{txO NHr6VWwzOzR2M{iwOS=>
ECC1 NVHOUmJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfrRWVwUUN3ME2yMlA4KMLzIECuNFEh|ryP M2CweVI{PDR|OEC1
HEC1B NVn1SWFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nzcmlEPTB;Mj61O{DDuSByLkKzJO69VQ>? NXfuVmRIOjN2NEO4NFU>
USPC1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3tW3lKSzVyPUKuOlAhyrFiMD6xN{DPxE1? MVSyN|Q1OzhyNR?=
SPAC1L NIfacJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;OSFhKSzVyPUOuNFYhyrFiMT6xOEDPxE1? MoG4NlM1PDN6MEW=
HUVEC M4PQeGNmdGxiVnnhZoltcXS7IFHzd4F6 M1;vflAuOjVizszN NWnwcplCPzJiaB?= M3T6fWROW09? MVTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M3PZV|I{OjJ6MEG3
HMVEC M1W4TGNmdGxiVnnhZoltcXS7IFHzd4F6 NF\sXlgxNTJ3IN88US=> MWW3NkBp MXjEUXNQ NX61Omh[cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MoryNlMzOjhyMUe=
MHCC-97H MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEH0UGgxNTJ3IN88US=> MW[3NkBp NGjpd4FFVVOR MVvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NH;3[FYzOzJ{OECxOy=>
SMMC7721 M1;CeGNmdGxiVnnhZoltcXS7IFHzd4F6 NFi4PYIxNTJ3IN88US=> NIftfVY4OiCq NV3VNGRTTE2VTx?= NVjKR4ZMcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MmjINlMzOjhyMUe=
Huh-7 MUTBdI9xfG:|aYOgRZN{[Xl? MVGwMVEzNjVizszN NUTud4x4OjRiaB?= NHjJOIRFVVORwrC= MlTNd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MoLUNlIzOzB2N{m=
Sk-Hep1 MUTBdI9xfG:|aYOgRZN{[Xl? NEnOXWcxNTF{LkWg{txO NXvqZ3AxOjRiaB?= MoTQSG1UV8Li M13wOpNmdnOrdHn6[ZMhUEOFIHPlcIx{KHSxIGTSRWlNNSCjbnSgeIlo[XS3eoXtZYIucW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MY[yNlI{ODR5OR?=
Hep3B M1:yXGFxd3C2b4Ppd{BCe3OjeR?= NE[wZ48xNTF{LkWg{txO MnrLNlQhcA>? NHPBUYdFVVORwrC= MkXZd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFu3W4gzOjJ|MES3PS=>
PLC5 Mln2RZBweHSxc3nzJGF{e2G7 MU[wMVEzNjVizszN M{TX[lI1KGh? MUTEUXNQyqB? NHSzNG1{\W6|aYTpfoV{KEiFQzDj[YxteyC2bzDUVmFKVC1iYX7kJJRq\2G2dYr1cYFjNWmwZIXj[YQh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M1:2bFIzOjNyNEe5
PLC5 MWTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MonVNE0yPSEQvF2= NI\qNoM4OiCq NWn3d|l5emWmdXPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg MY[yNlE5ODNyOB?=
Hep3B MkPCR4VtdCCYaXHibYxqfHliQYPzZZk> MoO3NE0yPSEQvF2= Mnj3O|IhcA>? MXvy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? NGfvW|IzOjF6MEOwPC=>
Sk-Hep1 NIe2NFFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Ml\yNE0yPSEQvF2= NXL5d3RvPzJiaB?= NGLaWnFz\WS3Y3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M{D2OFIzOThyM{C4
Huh-7 MljzR4VtdCCYaXHibYxqfHliQYPzZZk> MXewMVE2KM7:TR?= NHXSe5c4OiCq MknkdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi MVuyNlE5ODNyOB?=
PLC5 M1nM[WFxd3C2b4Ppd{BCe3OjeR?= MXSwMVE2KM7:TR?= Mkj5NlQhcA>? NIi5N|ZqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NFv6RY0zOjF6MEOwPC=>
Hep3B M1zhfGFxd3C2b4Ppd{BCe3OjeR?= NYPXXmZ4OC1zNTFOwG0> NULG[5lROjRiaB?= NIDlS5VqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NH;yT3EzOjF6MEOwPC=>
Sk-Hep1 MXXBdI9xfG:|aYOgRZN{[Xl? NIflXmkxNTF3IN88US=> NEDncFIzPCCq NEmyb2lqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= M1TGd|IzOThyM{C4
Huh-7 NHrjZ2dCeG:ydH;zbZMhSXO|YYm= MUGwMVE2KM7:TR?= MlPyNlQhcA>? M3XPeYlv[3KnYYPld{BieG:ydH;0bYMh[2WubDDk[YF1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi M1TXTlIzOThyM{C4
PLC5 NIrZRYdHfW6ldHnvckBCe3OjeR?= M{nhXFAuOTBizszN M{fGPVI1KGh? M3vTV4NifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? NGPjSXQzOjF6MEOwPC=>
Hep3B M2TzRWZ2dmO2aX;uJGF{e2G7 NHHzdFIxNTFyIN88US=> Mnr3NlQhcA>? NGHF[JVk[XW|ZYOg[I9{\S2mZYDlcoRmdnRiRF7BJIZz[WevZX70ZZRqd25? NYHQSZNPOjJzOECzNFg>
Sk-Hep1 M1fGfmZ2dmO2aX;uJGF{e2G7 NHvCTHYxNTFyIN88US=> NXuzOHZjOjRiaB?= MXXjZZV{\XNiZH;z[U1l\XCnbnTlcpQhTE6DIH\yZYdu\W62YYTpc44> MXGyNlE5ODNyOB?=
Huh-7 MXPGeY5kfGmxbjDBd5NigQ>? NFW5V5YxNTFyIN88US=> MUCyOEBp MWTjZZV{\XNiZH;z[U1l\XCnbnTlcpQhTE6DIH\yZYdu\W62YYTpc44> MorUNlIyQDB|MEi=
SW780 M1jveGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPVOUBl M4HQemlEPTB;NUCgcm0> NGTO[YUzOTFzOU[2NS=>
RT112 NEn1blJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLBOUBl M4KzXGlEPTB;MUWgcm0> M{S3SVIyOTF7Nk[x
RT4 NVvX[3RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nESFUh\A>? MnXWTWM2OD13IH7N NXm5WWNOOjFzMUm2OlE>
JMSU1 NUHMdZZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1H5N|Uh\A>? MkP0TWM2OD13MDDuUS=> NH\6c5YzOTFzOU[2NS=>
J82 NVjIWlZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zyO|Uh\A>? Ml3VTWM2OD1zNECwJI5O MluwNlEyOTl4NkG=
97-7 M2X3[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\qUYg2KGR? NIfKS2ZKSzVyPUGwNFAhdk1? MmLKNlEyOTl4NkG=
RT112 M13FZ2Z2dmO2aX;uJGF{e2G7 MUC1NFAhdk1? NXPWSHVOOjRiaB?= MojYbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| NGHsSHYzOTFzOU[2NS=>
RT4 NH;KWmZHfW6ldHnvckBCe3OjeR?= MUC1NFAhdk1? NWjRTJprOjRiaB?= NWTMb45icW6lcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKEdzwrDhZ4NwdXCjbnnl[EBjgSCjIHTlZ5Jm[XOnIHnuJHMh[W6mIFeyM20heGijc3Xz M4nsV|IyOTF7Nk[x
MGH-U3 NHLNUJNHfW6ldHnvckBCe3OjeR?= M1vVelUxOCCwTR?= NFrTUVEzPCCq NIG1ZYRqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= NXPxO3pZOjFzMUm2OlE>
SW780 MmLhSpVv[3Srb36gRZN{[Xl? MVm1NFAhdk1? MVqyOEBp NVz5TJBvcW6lcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKEdzwrDhZ4NwdXCjbnnl[EBjgSCjIHTlZ5Jm[XOnIHnuJHMh[W6mIFeyM20heGijc3Xz MkfhNlEyOTl4NkG=
97-7 NXL5cGk4TnWwY4Tpc44hSXO|YYm= MnvFOVAxKG6P NF;YfoozPCCq M2q5PYlv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= NF\nSZIzOTFzOU[2NS=>
 J807C MoruR4VtdCCYaXHibYxqfHliQYPzZZk> MXqwMVQxOCCwTR?= NEPiU5o1QCCq MVTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NET4UWUyPTV7OEixOC=>
Y373C NXfBPGpzS2WubDDWbYFjcWyrdImgRZN{[Xl? Mn36NE01ODBibl2= NHrxcWg1QCCq MULpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MmLQNVU2QTh6MUS=
K650E MU\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MV:wMVQxOCCwTR?= MlrlOFghcA>? NWnkWmhNcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M1:xclE2PTl6OEG0
G384D M{SzUmNmdGxiVnnhZoltcXS7IFHzd4F6 MUKwMVQxOCCwTR?= NIPIUJU1QCCq MkCybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> Ml3ENVU2QTh6MUS=
F384L MorFR4VtdCCYaXHibYxqfHliQYPzZZk> MkjKNE01ODBibl2= MVm0PEBp MUPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MVmxOVU6QDhzNB?=
KMS11 NXG2R4hNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXe3NkBp NH\DU2NKSzVyPUmwJI5O MWWxOVU6QDhzNB?=
KMS18 M3fY[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVT3WHFKPzJiaB?= Mnm1TWM2OD13NUCgcm0> NHK2co8yPTV7OEixOC=>
OPM2 NF;jcolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvNbYc4OiCq Mle4TWM2OD17MDDuUS=> M{m3PFE2PTl6OEG0
H929 M37ycWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYK3NkBp MXXJR|UxRiB{NUCwJI5O NVXISVEzOTV3OUi4NVQ>
8226 NUL0S4RVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLnZVE4OiCq MWTJR|UxRiB{NUCwJI5O NInSdGkyPTV7OEixOC=>
U266 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTwfIw4OiCq M3HTOmlEPTB-IEK1NFAhdk1? NFHCdGgyPTV7OEixOC=>

... 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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    V2

* 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