Dovitinib (TKI-258)

For research use only.

Catalog No.S1018 Synonyms: CHIR-258

19 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 19 publications

Purity & Quality Control

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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 NXTGbXdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELWfY5KSzVyPUCuOFQ6KM7:TR?= MX[yOVIxOjB5Mx?=
SupB15-R NYXqeIt7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwNUW4JO69VQ>? M33YN|I2OjB{MEez
BaF3-pSRα M2Xp[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfaTWM2OD1yLk[2PEDPxE1? NEPnVZQzPTJyMkC3Ny=>
BaF3-p210Bcr-Abl NIXmfGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTBwNkmyJO69VQ>? MonLNlUzODJyN{O=
BaF3-p210Bcr-Abl-T315I Mn7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHrS2tXUUN3ME2yMlYzPiEQvF2= NHywSFYzPTJyMkC3Ny=>
CCRF-CEM NYHhWpk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2C0dWlEPTB;MD6zPVgh|ryP MkfBNlUzODJyN{K=
CEM/C2 NHvifndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3kZpRKSzVyPUGuNVI2KM7:TR?= NXH4em1yOjV{MEKwO|I>
Nalm-6 M1nGd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULNWplKUUN3ME2wMlM5OiEQvF2= NY\qV|c1OjV{MEKwO|I>
SEM-K2 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTBwMEKyJO69VQ>? MVyyOVIxOjB5Mh?=
HB-1119 M1X6bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjTb5NpUUN3ME2wMlAzQCEQvF2= MX6yOVIxOjB5Mh?=
RS4:11 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLyTWYzUUN3ME2yMlgyKM7:TR?= MWSyOVIxOjB5Mh?=
Nalm-6 M3PvTmFxd3C2b4Ppd{BCe3OjeR?= NVy0T41VOiEQvF2= Mo\PNlQwPDhiaB?= M1PCPYlv\HWlZYOgZZBweHSxc3nzJJJme3WudHnu[{BqdiCjYn;1eEA4OiVib3[gZ4VtdCCmZXH0bEBi\nSncjCyOEBpKHS{ZXH0cYVvfCCjbnSgPFEmKGGodHXyJFQ5KGh? Ml7FNlUzODJyN{K=
SEM-K2 MXPBdI9xfG:|aYOgRZN{[Xl? NH7hfocxNjFxMTFOwG0> NXK0ZpVkOjRiaB?= M4n6[Ilv\HWlZYOg[YFzdHliYYDvdJRwe2m|IH;mJHNGVS2NMjDj[YxteyCjdDCwMlEh|ryPIHHmeIVzKDJ2IHi= NW\CWol[OjV{MEKwO|I>
HCT-116 Mn\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTNwMEWwMlU5KM7:TR?= MnHJNlQ1QTV5NUC=
HT-29 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfZTWM2OD13LkKxMlk{KM7:TR?= NYrhNY1rOjR2OUW3OVA>
SW-480 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjFVYZKSzVyPUSuN|MxNjR5IN88US=> M3S4bVI1PDl3N{Ww
CaCO2 M2joSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELITpVKSzVyPUOuNlMxNjZ2IN88US=> Mkm4NlQ1QTV5NUC=
LS174T NYi1UpcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITLO|VKSzVyPUSuN|MxNjR5IN88US=> MmLxNlQ1QTV5NUC=
HEC-1A MlfuSpVv[3Srb36gRZN{[Xl? MmfCNE4xPS9yLkGvNE42KM7:TR?= NFnXZZU4OiCq NV3m[WxN[2G3c3XzJIEh\GWlcnXhd4UhcW5iU2TBWFMtKEWUSzygZY5lKEGNVDDwbI9{eGixconsZZRqd25? NFnmeXYzPDR7NUe1NC=>
AN3CA NXjDRWNWTnWwY4Tpc44hSXO|YYm= NVnrcoN4OC5yNT:wMlEwOC53IN88US=> M4XxflczKGh? NIrrXpBk[XW|ZYOgZUBl\WO{ZXHz[UBqdiCVVFHUN{whTVKNLDDhcoQhSUuWIIDoc5NxcG:{eXzheIlwdg>? NFn6PZgzPDR7NUe1NC=>
MFE-296  NYDM[HpjTnWwY4Tpc44hSXO|YYm= MonPNE4xPS9yLkGvNE42KM7:TR?= NHfwN2k4OiCq NX6wNnRS[2G3c3XzJIEh\GWlcnXhd4UhcW5iU2TBWFMtKEWUSzygZY5lKEGNVDDwbI9{eGixconsZZRqd25? MYGyOFQ6PTd3MB?=
UMC3 NX\6NGxLS2WubDDWbYFjcWyrdImgRZN{[Xl? MWCxMVExKM7:TR?= M{PjXlczKGh? MUjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NH71W3YzPDN{NUS2NS=>
5637 NFe3UG1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlK3NU0yOCEQvF2= MXK3NkBp NGW5ZVdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MmDRNlQ{OjV2NkG=
HU456 MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHu2ZY4yNTFyIN88US=> MYm3NkBp NWX1XXFScW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MknjNlQ{OjV2NkG=
MGHU4 NHfxO2VE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M330eFEuOTBizszN MV:3NkBp NILieY5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MX:yOFMzPTR4MR?=
HT1376 NXzN[FR3S2WubDDWbYFjcWyrdImgRZN{[Xl? Mn7LNU0yOCEQvF2= NXLYc2xqPzJiaB?= Mn3obY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MWmyOFMzPTR4MR?=
RT112 M3[wd2NmdGxiVnnhZoltcXS7IFHzd4F6 MXmxMVExKM7:TR?= MXO3NkBp NY\re3VwcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? Mmi4NlQ{OjV2NkG=
T24 MnvwR4VtdCCYaXHibYxqfHliQYPzZZk> NYTnfldYOS1zMDFOwG0> MXK3NkBp M2H5ZolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M4TlU|I1OzJ3NE[x
BFTC905 MVPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmrYNU0yOCEQvF2= MYG3NkBp MXrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NV\SblNnOjR|MkW0OlE>
TCC-SUP MU\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NIPIbVYyNTFyIN88US=> NEfGOmI4OiCq MX7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NXn1dHFxOjR|MkW0OlE>
RT4 NGnNUnhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWKxMVExKM7:TR?= MWS3NkBp NF\SdmJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M2PxcFI1OzJ3NE[x
HONE1 MoLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVGwMlEuOTBizszN NX7WXYdSPDkEoHi= MXLpcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= MlrnNlQzOzhyOUS=
HNE1 MnPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\T[5JmOC5zLUGwJO69VQ>? Ml;jOFjDqGh? NEXteYpqdmS3Y3XzJGczN01iZHXsZZkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NXLoWIo4OjR{M{iwPVQ>
CNE2  MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nCVlAvOS1zMDFOwG0> NXHNSIZ{PDkEoHi= NYTFN5MycW6mdXPld{BIOi:PIHTlcIF6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MUiyOFI{QDB7NB?=
C666-1 M335[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXiwMlEuOTBizszN NHjqe|I1QMLiaB?= NEKyS2ZqdmS3Y3XzJGczN01iZHXsZZkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> NUjxXZNrOjR{M{iwPVQ>
HeLa NHPld4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXGwMlEuOTBizszN MoqyNlQhcA>? MnLhbY5lfWOnczDHNk9OKGG{cnXzeEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NGfJbnYzPDJ|OEC5OC=>
Hep3B MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvQeVZVOC5zLUGwJO69VQ>? NXPqWFBmOjRiaB?= MnvSbY5lfWOnczDHNuKh[XK{ZYP0xsA> MUCyOFI{QDB7NB?=
HepG2 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDuN5A1QCCq NFjYOZVKSzVyPUKuO|I4KMLzIECuOFI6KM7:TR?= MmW1NlM2PDZ3OUG=
Hep3B MlHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrJcWQyPDhiaB?= NUL1bmNFUUN3ME20MlIzOyEEsTCwMlg{QSEQvF2= M3;zPFI{PTR4NUmx
PLC/PRF5 NF7sPZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfTfJI1QCCq M{TVfWlEPTB;MU[uNVIxKMLzIESuNFAyKM7:TR?= MX2yN|U1PjV7MR?=
Huh7 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjtNIM1QCCq M4TkXGlEPTB;MUWuNFA4KMLzIEeuN|M1KM7:TR?= NW\GN2FuOjN3NE[1PVE>
HepG2 NVPjb2JXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFy2TFE4OiCq MXPJR|UxRTFwMkCwJOKyKDBwMkK2JO69VQ>? MYmyN|U1PjV7MR?=
Hep3B NF\WcYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2m1RlczKGh? M4HvUWlEPTB;MD64PVIhyrFiMD6wOFQh|ryP MWiyN|U1PjV7MR?=
PLC/PRF5 MmLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvEO|IhcA>? MVTJR|UxRTNwMUGwJOKyKDBwM{O3JO69VQ>? MmnJNlM2PDZ3OUG=
Huh7 NH\5O2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTqW|Q2PzJiaB?= NUfzWWtZUUN3ME2zMlk5OCEEsTCwMlgxOyEQvF2= NYS4d4tvOjN3NE[1PVE>
MFE280 MlfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzzNFJpUUN3ME2wMlQzKMLzIECuNFYh|ryP MkHPNlM1PDN6MEW=
AN3CA NIjHSpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPsNnBKSzVyPUCuOVAhyrFiMD6xNEDPxE1? MlrtNlM1PDN6MEW=
HEC155 MnHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXXTWM2OD1yLk[2JOKyKDBwMEmg{txO MVqyN|Q1OzhyNR?=
MFE296 NW[4NHI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4P3dGlEPTB;MD62OkDDuSByLkG5JO69VQ>? Mn;PNlM1PDN6MEW=
SPAC1S M{\J[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTBwN{egxtEhOC5yODFOwG0> MWGyN|Q1OzhyNR?=
RL952 MnruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfVTWM2OD1yLkmzJOKyKDBwMEGg{txO MV:yN|Q1OzhyNR?=
EN1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfyNJFKSzVyPUGuNFIhyrFiMD6yOUDPxE1? NYi4[VExOjN2NEO4NFU>
SNGII M1rmNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXJZnpXUUN3ME2xMlI1KMLzIECuNlgh|ryP NHX0[WUzOzR2M{iwOS=>
ISHIKAWA NYfmS|l2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nZWGlEPTB;MT6zNEDDuSByLkGxJO69VQ>? NYjTZ3B7OjN2NEO4NFU>
HEC1A MmrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnRXXZDUUN3ME2xMlM1KMLzIECuN|Ah|ryP NVHRdI9EOjN2NEO4NFU>
KLE NVrBO25QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHTTWM2OD1zLkO3JOKyKDBwMEKg{txO M1\CWVI{PDR|OEC1
SNGM NWfZNoJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3ywNGlEPTB;MT60NkDDuSByLkGzJO69VQ>? MWSyN|Q1OzhyNR?=
USPC2 MonBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jZRWlEPTB;MT62NkDDuSByLkCxJO69VQ>? NVjOfIE5OjN2NEO4NFU>
EN NHLUWGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfaTWM2OD1zLk[2JOKyKDBwMEGg{txO NGXlXXIzOzR2M{iwOS=>
MFE319 NV3pRW9ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7rTWM2OD1zLki3JOKyKDBwNEWg{txO MVKyN|Q1OzhyNR?=
EFE184 NIjHS2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjIbmlKSzVyPUKuNFQhyrFiMD6xN{DPxE1? NWjEUYZqOjN2NEO4NFU>
ECC1 MnLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3K4WGlEPTB;Mj6wO{DDuSByLkCxJO69VQ>? MoX0NlM1PDN6MEW=
HEC1B NUm1WZRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTJwNUegxtEhOC5{MzFOwG0> NE[0U3kzOzR2M{iwOS=>
USPC1 NGTzR5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnq2TWM2OD1{Lk[wJOKyKDBwMUOg{txO MkX4NlM1PDN6MEW=
SPAC1L Mmn5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3ZTWM2OD1|LkC2JOKyKDFwMUSg{txO MYCyN|Q1OzhyNR?=
HUVEC MXTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXftRZdLOC1{NTFOwG0> NX\sc4lmPzJiaB?= NH21UmlFVVOR NIn1UZRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MV:yN|IzQDBzNx?=
HMVEC NFm3cnVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NVHLbVBEOC1{NTFOwG0> NHTPSYQ4OiCq M1n3TGROW09? NIPtc|ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MUeyN|IzQDBzNx?=
MHCC-97H MoXSR4VtdCCYaXHibYxqfHliQYPzZZk> MUiwMVI2KM7:TR?= NEjYd2I4OiCq M{XS[2ROW09? M{nZ[olvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NI[0UVMzOzJ{OECxOy=>
SMMC7721 MVrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NW[1ZlZpOC1{NTFOwG0> MX23NkBp M2fUVGROW09? M1PUbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M121dFI{OjJ6MEG3
Huh-7 NFT0[ppCeG:ydH;zbZMhSXO|YYm= MWiwMVEzNjVizszN NVPmUYVWOjRiaB?= M1;jRWROW00EoB?= MmPHd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NEDzbIEzOjJ|MES3PS=>
Sk-Hep1 NXrvdmFZSXCxcITvd4l{KEG|c3H5 MmjxNE0yOi53IN88US=> NGHIb|UzPCCq NGXxcWpFVVORwrC= NEPEclZ{\W6|aYTpfoV{KEiFQzDj[YxteyC2bzDUVmFKVC1iYX7kJJRq\2G2dYr1cYFjNWmwZIXj[YQh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIDE[5AzOjJ|MES3PS=>
Hep3B NFLUWFdCeG:ydH;zbZMhSXO|YYm= MYKwMVEzNjVizszN MXKyOEBp NYrncFVCTE2VT9Mg NYO0Topye2Wwc3n0bZpmeyCKQ1OgZ4VtdHNidH:gWHJCUUxvIHHu[EB1cWejdIX6eY1i[i2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1T5cFIzOjNyNEe5
PLC5 MlLQRZBweHSxc3nzJGF{e2G7 NY\YT2lHOC1zMj61JO69VQ>? MVWyOEBp NITHS4dFVVORwrC= MnjXd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFrsOZozOjJ|MES3PS=>
PLC5 M1LUSmNmdGxiVnnhZoltcXS7IFHzd4F6 MkjCNE0yPSEQvF2= MoHYO|IhcA>? NXXIUGwzemWmdXPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg NHfxcZczOjF6MEOwPC=>
Hep3B M1XpbGNmdGxiVnnhZoltcXS7IFHzd4F6 MmLaNE0yPSEQvF2= NUOzOHhzPzJiaB?= M1PKfJJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NHz5WnIzOjF6MEOwPC=>
Sk-Hep1 MmfjR4VtdCCYaXHibYxqfHliQYPzZZk> MnH5NE0yPSEQvF2= MkLkO|IhcA>? MVry[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? MnrQNlIyQDB|MEi=
Huh-7 NEGxNXRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mn\4NE0yPSEQvF2= MlS3O|IhcA>? MmfWdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi NHXKboYzOjF6MEOwPC=>
PLC5 MljuRZBweHSxc3nzJGF{e2G7 NGTXN|YxNTF3IN88US=> M{PPUVI1KGh? M2XC[Ylv[3KnYYPld{BieG:ydH;0bYMh[2WubDDk[YF1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi Ml;ZNlIyQDB|MEi=
Hep3B M37GfWFxd3C2b4Ppd{BCe3OjeR?= MlS2NE0yPSEQvF2= MkLMNlQhcA>? MYXpcoNz\WG|ZYOgZZBweHSxdHnjJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZLDqA>? MX:yNlE5ODNyOB?=
Sk-Hep1 NUOxe2pOSXCxcITvd4l{KEG|c3H5 NGDyNmMxNTF3IN88US=> M4DkdFI1KGh? NEPydpFqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MnPNNlIyQDB|MEi=
Huh-7 MknKRZBweHSxc3nzJGF{e2G7 M4TwW|AuOTVizszN NVT1RnQ1OjRiaB?= MnLZbY5kemWjc3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? NF;VW4IzOjF6MEOwPC=>
PLC5 MmrWSpVv[3Srb36gRZN{[Xl? Mk\UNE0yOCEQvF2= NHzTcGIzPCCq M{jjWYNifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? NG\vXXAzOjF6MEOwPC=>
Hep3B MXPGeY5kfGmxbjDBd5NigQ>? MVqwMVExKM7:TR?= NWDqUmRvOjRiaB?= NFr3dmFk[XW|ZYOg[I9{\S2mZYDlcoRmdnRiRF7BJIZz[WevZX70ZZRqd25? NWDI[IR2OjJzOECzNFg>
Sk-Hep1 NI\mWnRHfW6ldHnvckBCe3OjeR?= MkHBNE0yOCEQvF2= NIXIUFEzPCCq MofDZ4F2e2W|IHTvd4Uu\GWyZX7k[Y51KESQQTDmdoFodWWwdHH0bY9v NH\OdIUzOjF6MEOwPC=>
Huh-7 MnjQSpVv[3Srb36gRZN{[Xl? MUGwMVExKM7:TR?= NWC2e|FkOjRiaB?= NXv4S3F6[2G3c3XzJIRwe2VvZHXw[Y5l\W62IFTORUBnemGpbXXueIF1cW:w M4Dh[VIzOThyM{C4
SW780 M2rzPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPWOUBl MnTnTWM2OD13MDDuUS=> M1r0d|IyOTF7Nk[x
RT112 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[1JIQ> Mlf0TWM2OD1zNTDuUS=> NXnTeZF1OjFzMUm2OlE>
RT4 MljMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXy1JIQ> NXTTZVNlUUN3ME21JI5O NUfUOpZkOjFzMUm2OlE>
JMSU1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVm1JIQ> NWfBeWJUUUN3ME21NEBvVQ>? MV[yNVEyQTZ4MR?=
J82 NYO0WHU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXi1JIQ> MlXMTWM2OD1zNECwJI5O NWnaeYFpOjFzMUm2OlE>
97-7 M12zNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYe1dJQ3PSCm MUHJR|UxRTFyMECgcm0> MVGyNVEyQTZ4MR?=
RT112 M2G2SWZ2dmO2aX;uJGF{e2G7 MlLIOVAxKG6P NXnq[ZlpOjRiaB?= MWjpcoNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gS|HDqGGlY3;tdIFvcWWmIHL5JIEh\GWlcnXhd4UhcW5iUzDhcoQhTzJxTTDwbIF{\XN? NYrVdmp[OjFzMUm2OlE>
RT4 NYnONFJWTnWwY4Tpc44hSXO|YYm= MUO1NFAhdk1? MUGyOEBp M{HWOYlv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= MX[yNVEyQTZ4MR?=
MGH-U3 M{PXPGZ2dmO2aX;uJGF{e2G7 NWDMOnlXPTByIH7N NELiToozPCCq Mm\PbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| MnHNNlEyOTl4NkG=
SW780 MWDGeY5kfGmxbjDBd5NigQ>? MYG1NFAhdk1? NX3IRo9TOjRiaB?= MVLpcoNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gS|HDqGGlY3;tdIFvcWWmIHL5JIEh\GWlcnXhd4UhcW5iUzDhcoQhTzJxTTDwbIF{\XN? M{[wNVIyOTF7Nk[x
97-7 MXnGeY5kfGmxbjDBd5NigQ>? NYDJfVBDPTByIH7N NWDrS49IOjRiaB?= M4W3W4lv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= Mmf1NlEyOTl4NkG=
 J807C MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGm0[HExNTRyMDDuUS=> NYPiXnBpPDhiaB?= MnjNbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MX:xOVU6QDhzNB?=
Y373C M{TwfGNmdGxiVnnhZoltcXS7IFHzd4F6 MUewMVQxOCCwTR?= MlfhOFghcA>? MV3pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M{jPVVE2PTl6OEG0
K650E NYnqWo12S2WubDDWbYFjcWyrdImgRZN{[Xl? Ml70NE01ODBibl2= Ml7DOFghcA>? NHrT[IpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M4WxfVE2PTl6OEG0
G384D M33KbGNmdGxiVnnhZoltcXS7IFHzd4F6 M4nFPFAuPDByIH7N NVrkXYlkPDhiaB?= NEfqVpVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MkHuNVU2QTh6MUS=
F384L NHLFNlZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUGwMVQxOCCwTR?= MVK0PEBp MlHjbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NGn2[3YyPTV7OEixOC=>
KMS11 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3S1V|czKGh? NH;HUYRKSzVyPUmwJI5O NH\zd2oyPTV7OEixOC=>
KMS18 NGDGWIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fZXlczKGh? MmnLTWM2OD13NUCgcm0> M3rLelE2PTl6OEG0
OPM2 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2izNFczKGh? NXHzR45uUUN3ME25NEBvVQ>? M2TDOlE2PTl6OEG0
H929 M1TDSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrNO|IhcA>? M3qzVGlEPTB-IEK1NFAhdk1? MlW5NVU2QTh6MUS=
8226 MojuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVW3NkBp NWLuXVlQUUN3ME6gNlUxOCCwTR?= M2jSfFE2PTl6OEG0
U266 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7YbJA4OiCq MVzJR|UxRiB{NUCwJI5O Ml3lNVU2QTh6MUS=

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

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

  • 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):
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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

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

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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
NCT01030055 Completed Drug: TKI258 (dovitinib) Neoplasms|Cancer|Tumors Novartis Pharmaceuticals|Novartis February 2010 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