Dovitinib (TKI-258, CHIR-258)

Catalog No.S1018

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

Molecular Weight(MW): 392.43

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

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In DMSO USD 191 In stock
USD 170 In stock
USD 270 In stock
USD 470 In stock

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7 Customer Reviews

  • In vitro assays on CUX1-FGFR1-expressing Ba/F3 cells. a. IL-3 deprivation of Ba/F3 cells transduced with CUX1-FGFR1 resulted in transformation to growth factor independent growth. The mean growth ±SEM of three separate measurements over four consecutive days is presented. b. The dose-response curves of CUX1-FGFR1-transduced Ba/F3 cells, treated with TKI258 and PKC412 for 48 hours in the absence or presence of IL-3 (2 ng/ml) are presented. Points represent the average results of two experiments done in triplicate plotted with the curve-fitting GraphPad Prism 5 software; bars, SD. The calculated IC50 for each inhibitor is indicated. c. Western blot analyses of CUX1-FGFR1-transformed Ba/F3 cells after treatment with PKC412 and TKI258. Phosphorylation of CUX1-FGFR1 and its downstream effectors STAT5 and RPS6K decreased with increasing inhibitor concentrations. Expression of total CUX1-FGFR1, STAT5 and RPS6K remained unaffected. d. Effect of PKC412 and TKI258 on apoptosis of CUX1-FGFR1-expressing Ba/F3 cells after treatment for 48 hours. The percentage of apoptotic plus necrotic CUX1-FGFR1-transduced Ba/F3 cells is indicated.

    haematologica 2011 96, 922-926. Dovitinib (TKI-258, CHIR-258) purchased from Selleck.

    RT112 cells were exposed to PD173074 (PD) (500 nM) for 0-24 h, TKI-258 (TK) (500 nM) or SU5402 (SU) (5 nM) for 1 h. Cells were lysed, FGFR3 was immunoprecipitated (immunoprecipitated, IP) and blots (immunoblot, IB) were probed for phospho-tyrosine and reprobed for FGFR3 or probed for phospho-ERK and reprobed for total ERK.

    Brit J Cancer 2010 104, 75-82. Dovitinib (TKI-258, CHIR-258) purchased from Selleck.

  • Cells were exposed to PD173074 or TKI-258 (500 nM) for 24 h. Cell cycle profile was analysed using the Guava Easycyte Plus flow cytometry system.

    Brit J Cancer 2010 104, 75-82. Dovitinib (TKI-258, CHIR-258) purchased from Selleck.


    Orthotopic xenografts of HNSCC cell lines (A) SCC-1 and (B) OSC-19 were treated with dovitinib (20 mg/kg/day). In addition, the OSC-19 xenografts were treated with +/ radiation therapy. Marker, mean for triplicate; bars, SE. Statistical significance by unpaired t-test, p < 0.05.

    Oral Oncol 2012 48, 1242-9. Dovitinib (TKI-258, CHIR-258) purchased from Selleck.

  • Treatments were initiated at time of orthotopic implantation. Growth stabilization was seen by day 8 of treatment (Fig. B). On day 17, tumors were har-vested and histological analysis was performed (Fig. C). Following Ki67 staining, tumors from control xenografts were found to have a higher percentage of proliferating cells (62%) compared to those treated with dovitinib (14%; p = 0.005). The incidence of lymph nodes metastasis was greater in the control cohort ( n = 15) com-pared to those treated with dovitinib (n = 5).

    Oral Oncol 2012 48, 1242-9. Dovitinib (TKI-258, CHIR-258) purchased from Selleck.

    Dose–response curves for HNSCC cells and fibroblasts treated in vitro with dovitinib (0–1000 nM). Boxes, mean for triplicate; bars, SE

    Oral Oncol 2012 48, 1242-9. Dovitinib (TKI-258, CHIR-258) purchased from Selleck.

  • Ba/F3 cell lines expressing the recombinant TEL/kinase domain fusion protein for FGFR1-4 .Cells were grown in RPMI 1640 containing 10% FBS and 500 ng/mL puromycin. The parental Ba/F3 cell line transduced with an empty vector was grown in 10 ng/mL IL-3 (R & D systems). Cell viability was assessed at 72 hours using the Cell Titer 96 Aqueous One Solution (Promega). Data were plotted as percent viability relative to vehicle-treated cells and are shown as mean (±SD) from 3 experiments.

    AACR 2011 Dovitinib (TKI-258, CHIR-258) purchased from Selleck.

Purity & Quality Control

Choose Selective FLT3 Inhibitors

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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.
FLT3 [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
FGFR1 [1]
(Cell-free assay)
(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 NIjwbIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fa[2lEPTB;MD60OFkh|ryP M3KzSlI2OjB{MEez
SupB15-R MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzObWFKSzVyPUCuOVU5KM7:TR?= MUOyOVIxOjB5Mx?=
BaF3-pSRα NWjUdXU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFO0W4hKSzVyPUCuOlY5KM7:TR?= M1TNVVI2OjB{MEez
BaF3-p210Bcr-Abl MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWToRmdPUUN3ME2wMlY6OiEQvF2= MkPXNlUzODJyN{O=
BaF3-p210Bcr-Abl-T315I MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjubI9KSzVyPUKuOlI3KM7:TR?= Mnj6NlUzODJyN{O=
CCRF-CEM M3fzU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH24So1KSzVyPUCuN|k5KM7:TR?= NUXncm1wOjV{MEKwO|I>
CEM/C2 NGHldHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW[4bWg5UUN3ME2xMlEzPSEQvF2= Ml;BNlUzODJyN{K=
Nalm-6 MknaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPWc|lKSzVyPUCuN|gzKM7:TR?= MnLYNlUzODJyN{K=
SEM-K2 NWfE[nRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWCxVlhiUUN3ME2wMlAzOiEQvF2= M17KOVI2OjB{MEey
HB-1119 NUPtNFNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PHSWlEPTB;MD6wNlgh|ryP NXrON5FnOjV{MEKwO|I>
RS4:11 Mn6zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPETWM2OD1{LkixJO69VQ>? M2DLZlI2OjB{MEey
Nalm-6 MmnlRZBweHSxc3nzJGF{e2G7 MontNkDPxE1? M1m0[VI1NzR6IHi= MWLpcoR2[2W|IHHwc5B1d3OrczDy[ZN2dHSrbnegbY4h[WKxdYSgO|ImKG:oIHPlcIwh\GWjdHigZYZ1\XJiMkSgbEB1emWjdH3lcpQh[W6mIEixKUBi\nSncjC0PEBp MmLUNlUzODJyN{K=
HT-29 NFHON|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nlXmlEPTB;NT6yNU46OyEQvF2= MnLHNlQ1QTV5NUC=
SW-480 NEP6ZXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfRfpNKSzVyPUSuN|MxNjR5IN88US=> M4W4ZVI1PDl3N{Ww
CaCO2 NF\STFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:wV2lEPTB;Mz6yN|AvPjRizszN MWKyOFQ6PTd3MB?=
LS174T M2HoV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLjTWM2OD12LkOzNE41PyEQvF2= NYDsRlFPOjR2OUW3OVA>
AN3CA MoW4SpVv[3Srb36gRZN{[Xl? Mni2NE4xPS9yLkGvNE42KM7:TR?= NGfi[3Q4OiCq NVm3dpVr[2G3c3XzJIEh\GWlcnXhd4UhcW5iU2TBWFMtKEWUSzygZY5lKEGNVDDwbI9{eGixconsZZRqd25? Ml;ONlQ1QTV5NUC=
MFE-296  MYPGeY5kfGmxbjDBd5NigQ>? NWnIe|hsOC5yNT:wMlEwOC53IN88US=> MkLnO|IhcA>? MXHjZZV{\XNiYTDk[YNz\WG|ZTDpckBUXEGWMzygSXJMNCCjbnSgRWtVKHCqb4PwbI9zgWyjdHnvci=> MlPUNlQ1QTV5NUC=
UMC3 NYTZV4V3S2WubDDWbYFjcWyrdImgRZN{[Xl? M1XEd|EuOTBizszN NFjFWlY4OiCq MVjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NHryZ4ozPDN{NUS2NS=>
5637 NInndZVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Ml;qNU0yOCEQvF2= NGLUelE4OiCq NXPRSGZHcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MXOyOFMzPTR4MR?=
HU456 M3uyfGNmdGxiVnnhZoltcXS7IFHzd4F6 NI[2Ro0yNTFyIN88US=> NEPBcVA4OiCq M3LqTIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MVuyOFMzPTR4MR?=
MGHU4 NELHZZZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFO0cIkyNTFyIN88US=> Mof5O|IhcA>? NGXjPJNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MlSwNlQ{OjV2NkG=
HT1376 NHvaNVhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4m2NlEuOTBizszN MXy3NkBp MmjubY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MmX4NlQ{OjV2NkG=
RT112 Mo[zR4VtdCCYaXHibYxqfHliQYPzZZk> MljVNU0yOCEQvF2= NGrMeHM4OiCq M1PYPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MX:yOFMzPTR4MR?=
T24 NWTGU4N{S2WubDDWbYFjcWyrdImgRZN{[Xl? MkLYNU0yOCEQvF2= NVzPTWJRPzJiaB?= NGXIfWRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MWOyOFMzPTR4MR?=
BFTC905 NYLzW3RnS2WubDDWbYFjcWyrdImgRZN{[Xl? NXLwcWRvOS1zMDFOwG0> MU[3NkBp M2rHXYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M37DeFI1OzJ3NE[x
TCC-SUP MmHNR4VtdCCYaXHibYxqfHliQYPzZZk> MWOxMVExKM7:TR?= MVu3NkBp MXHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NFOyblYzPDN{NUS2NS=>
RT4 MmXFR4VtdCCYaXHibYxqfHliQYPzZZk> NGDTcGMyNTFyIN88US=> M2TBVVczKGh? NYfTdFUxcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MkfINlQ{OjV2NkG=
HONE1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkCyNE4yNTFyIN88US=> M{jsTVQ5yqCq NFvtW3ZqdmS3Y3XzJGczN01iZHXsZZkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MkDpNlQzOzhyOUS=
HNE1 MoO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVSwMlEuOTBizszN M{P4W|Q5yqCq M1uzb4lv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NWfNdmVUOjR{M{iwPVQ>
CNE2  MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fSflAvOS1zMDFOwG0> NXXzSlNIPDkEoHi= Mn;hbY5lfWOnczDHNk9OKGSnbHH5JIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy NFTENIszPDJ|OEC5OC=>
C666-1 NYq5PYFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoX2NE4yNTFyIN88US=> NFe0fXo1QMLiaB?= M2naZ4lv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NVHSdodkOjR{M{iwPVQ>
HeLa NWPWUVBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzwT2l2OC5zLUGwJO69VQ>? NF;6dJQzPCCq NGTvV|dqdmS3Y3XzJGczN01iYYLy[ZN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MVmyOFI{QDB7NB?=
Hep3B M{Tte2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;1[lAvOS1zMDFOwG0> MYSyOEBp MXrpcoR2[2W|IFeyxsBienKnc4VCpC=> NWqyUlhXOjR{M{iwPVQ>
HepG2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWe0PEBp MoWxTWM2OD1{LkeyO{DDuSByLkSyPUDPxE1? NFmwcYYzOzV2NkW5NS=>
Hep3B MnzlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXi0PEBp M4nRfWlEPTB;ND6yNlMhyrFiMD64N|kh|ryP NEfwRWUzOzV2NkW5NS=>
PLC/PRF5 M2rJbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nHOlQ5KGh? NF\uZXRKSzVyPUG2MlEzOCEEsTC0MlAxOSEQvF2= M2jtd|I{PTR4NUmx
Huh7 M3zi[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU[0PEBp MkS3TWM2OD1zNT6wNFchyrFiNz6zN|Qh|ryP NYnpXlVSOjN3NE[1PVE>
HepG2 MmXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jGVlczKGh? NYO3UmdDUUN3ME2xMlIxOCEEsTCwMlIzPiEQvF2= NVXqd2tjOjN3NE[1PVE>
Hep3B NVnnSmx3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoK2O|IhcA>? MknvTWM2OD1yLki5NkDDuSByLkC0OEDPxE1? NWfHclZwOjN3NE[1PVE>
PLC/PRF5 MnLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;Lclh{PzJiaB?= NUDHWoNwUUN3ME2zMlEyOCEEsTCwMlM{PyEQvF2= NIfiXpIzOzV2NkW5NS=>
MFE280 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTKcnR[UUN3ME2wMlQzKMLzIECuNFYh|ryP MVGyN|Q1OzhyNR?=
HEC155 NFfjXWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2D4eWlEPTB;MD62OkDDuSByLkC5JO69VQ>? Mmi2NlM1PDN6MEW=
SPAC1S MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTBwN{egxtEhOC5yODFOwG0> MlKwNlM1PDN6MEW=
RL952 Mn\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULCeZBkUUN3ME2wMlk{KMLzIECuNFEh|ryP NXvjNYNrOjN2NEO4NFU>
EN1 MkC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XB[WlEPTB;MT6wNkDDuSByLkK1JO69VQ>? NV7Ne5pKOjN2NEO4NFU>
SNGII M1LIW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7tc4tTUUN3ME2xMlI1KMLzIECuNlgh|ryP MknQNlM1PDN6MEW=
HEC1A M3\E[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnmTYh4UUN3ME2xMlM1KMLzIECuN|Ah|ryP NXv1WVB{OjN2NEO4NFU>
KLE NX3LbZRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTFwM{egxtEhOC5yMjFOwG0> NUf3Sot7OjN2NEO4NFU>
USPC2 NEjy[G1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1[0[2lEPTB;MT62NkDDuSByLkCxJO69VQ>? NEXpelQzOzR2M{iwOS=>
EN MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[3fphGUUN3ME2xMlY3KMLzIECuNFEh|ryP NIPHO4UzOzR2M{iwOS=>
ECC1 MlfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrUZnlKSzVyPUKuNFchyrFiMD6wNUDPxE1? MkfENlM1PDN6MEW=
HEC1B NIG4S3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTJwNUegxtEhOC5{MzFOwG0> NFvEWIMzOzR2M{iwOS=>
USPC1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TSO2lEPTB;Mj62NEDDuSByLkGzJO69VQ>? MofrNlM1PDN6MEW=
SPAC1L NWfJT|J2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTNwME[gxtEhOS5zNDFOwG0> MUiyN|Q1OzhyNR?=
HUVEC NXfyUoxuS2WubDDWbYFjcWyrdImgRZN{[Xl? MWGwMVI2KM7:TR?= MkDQO|IhcA>? M12wcWROW09? NIPFc4VqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M17IN|I{OjJ6MEG3
HMVEC M17FW2NmdGxiVnnhZoltcXS7IFHzd4F6 NYHXc20zOC1{NTFOwG0> NYDV[2FNPzJiaB?= MluxSG1UVw>? MVPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NHrrVnMzOzJ{OECxOy=>
MHCC-97H M1;5V2NmdGxiVnnhZoltcXS7IFHzd4F6 NInnfYkxNTJ3IN88US=> NXmzcJZIPzJiaB?= MmjlSG1UVw>? NGjtdldqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NFqzVG0zOzJ{OECxOy=>
SMMC7721 MoK5R4VtdCCYaXHibYxqfHliQYPzZZk> NInjNpYxNTJ3IN88US=> M2myV|czKGh? NXjyTmdTTE2VTx?= NFTF[ppqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MkPINlMzOjhyMUe=
Huh-7 NV\kVotDSXCxcITvd4l{KEG|c3H5 NHjsSWYxNTF{LkWg{txO MmThNlQhcA>? MXTEUXNQyqB? M1HIPJNmdnOrdHn6[ZMhUEOFIHPlcIx{KHSxIGTSRWlNNSCjbnSgeIlo[XS3eoXtZYIucW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MmHrNlIzOzB2N{m=
Sk-Hep1 NFLmOZJCeG:ydH;zbZMhSXO|YYm= Mk\4NE0yOi53IN88US=> M4TSS|I1KGh? M4jYNGROW00EoB?= NGPZSJp{\W6|aYTpfoV{KEiFQzDj[YxteyC2bzDUVmFKVC1iYX7kJJRq\2G2dYr1cYFjNWmwZIXj[YQh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MnHsNlIzOzB2N{m=
Hep3B NUXyWmhoSXCxcITvd4l{KEG|c3H5 NIjEV|IxNTF{LkWg{txO MkH5NlQhcA>? NFvUbFFFVVORwrC= MlLwd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M2S2VVIzOjNyNEe5
PLC5 NX7idZppSXCxcITvd4l{KEG|c3H5 M3fndlAuOTJwNTFOwG0> NXv6WIc2OjRiaB?= NXrkV4ZQTE2VT9Mg Ml\ld4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Ml63NlIzOzB2N{m=
PLC5 MoPGR4VtdCCYaXHibYxqfHliQYPzZZk> MWKwMVE2KM7:TR?= NGjoS3A4OiCq MnHTdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi Mn\mNlIyQDB|MEi=
Hep3B MV3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn\TNE0yPSEQvF2= M3PZclczKGh? M2raUpJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MXiyNlE5ODNyOB?=
Sk-Hep1 MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3LNblAuOTVizszN NIPiUXM4OiCq M1O5bZJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NVLsXlF2OjJzOECzNFg>
Huh-7 NUP3RoViS2WubDDWbYFjcWyrdImgRZN{[Xl? M1PWWlAuOTVizszN NEPVOIE4OiCq M37LOJJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NFjm[I0zOjF6MEOwPC=>
PLC5 NHfleFdCeG:ydH;zbZMhSXO|YYm= MUKwMVE2KM7:TR?= NWnNcHdlOjRiaB?= NGj5VI5qdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NWPWelM6OjJzOECzNFg>
Hep3B NVPOZ254SXCxcITvd4l{KEG|c3H5 M3ezdFAuOTVizszN MWiyOEBp NF7MTZJqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NVrLe2tzOjJzOECzNFg>
Sk-Hep1 MmHwRZBweHSxc3nzJGF{e2G7 M4HPVVAuOTVizszN NEDDdpkzPCCq NFnKcoZqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= M4K2NVIzOThyM{C4
Huh-7 NGH6eYpCeG:ydH;zbZMhSXO|YYm= NYDLNYU3OC1zNTFOwG0> NXvPO4N[OjRiaB?= NVLJVGJZcW6lcnXhd4V{KGGyb4D0c5Rq[yClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= MoHvNlIyQDB|MEi=
PLC5 MYDGeY5kfGmxbjDBd5NigQ>? M3LGVlAuOTBizszN NHzZPVQzPCCq M3T5OINifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? NULBeHZLOjJzOECzNFg>
Hep3B MY\GeY5kfGmxbjDBd5NigQ>? MkP0NE0yOCEQvF2= MUiyOEBp M3ezV4NifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? MmjLNlIyQDB|MEi=
Sk-Hep1 NHzJbIhHfW6ldHnvckBCe3OjeR?= MnzYNE0yOCEQvF2= NWDHSYZROjRiaB?= NHfBN5Vk[XW|ZYOg[I9{\S2mZYDlcoRmdnRiRF7BJIZz[WevZX70ZZRqd25? MV2yNlE5ODNyOB?=
Huh-7 NVLUbYhQTnWwY4Tpc44hSXO|YYm= M{OzcVAuOTBizszN MWKyOEBp Mk\RZ4F2e2W|IHTvd4Uu\GWyZX7k[Y51KESQQTDmdoFodWWwdHH0bY9v MVyyNlE5ODNyOB?=
SW780 Ml\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHnblc2KGR? M3W2dGlEPTB;NUCgcm0> NF\5UVMzOTFzOU[2NS=>
RT112 NX\0VlhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFf2Tno2KGR? NFzzeWtKSzVyPUG1JI5O MlnRNlEyOTl4NkG=
RT4 Mkf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\6RVUh\A>? M3:3ZWlEPTB;NTDuUS=> MkfDNlEyOTl4NkG=
JMSU1 MnX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXe1JIQ> M4TmZmlEPTB;NUCgcm0> MkH1NlEyOTl4NkG=
97-7 NVP1UWxWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nMbVUh\A>? M1P6NmlEPTB;MUCwNEBvVQ>? Mlr0NlEyOTl4NkG=
RT112 NHLwTZBHfW6ldHnvckBCe3OjeR?= MUi1NFAhdk1? NH\XN5YzPCCq M3GwOIlv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= MWeyNVEyQTZ4MR?=
RT4 NXvDb5dpTnWwY4Tpc44hSXO|YYm= NIHuXZA2ODBibl2= NYjn[Gt5OjRiaB?= MmrHbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| M{e4VFIyOTF7Nk[x
MGH-U3 NHrNbnNHfW6ldHnvckBCe3OjeR?= M2HVVFUxOCCwTR?= MkLzNlQhcA>? M3:5dIlv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= MW[yNVEyQTZ4MR?=
SW780 MlL3SpVv[3Srb36gRZN{[Xl? NWrwTYRpPTByIH7N NWq4[ndVOjRiaB?= MX7pcoNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gS|HDqGGlY3;tdIFvcWWmIHL5JIEh\GWlcnXhd4UhcW5iUzDhcoQhTzJxTTDwbIF{\XN? MmK4NlEyOTl4NkG=
97-7 NHv6V3RHfW6ldHnvckBCe3OjeR?= MU[1NFAhdk1? Ml;xNlQhcA>? NEO1V4RqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= NVixVVdPOjFzMUm2OlE>
 J807C M{nFZmNmdGxiVnnhZoltcXS7IFHzd4F6 NFOybY8xNTRyMDDuUS=> MlzWOFghcA>? M4TLWIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MWCxOVU6QDhzNB?=
Y373C NGnCSZZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXnafXN[OC12MECgcm0> NHPW[W41QCCq M3TjVYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M3K1VVE2PTl6OEG0
K650E NF73PJNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYDjbpJVOC12MECgcm0> MkDmOFghcA>? MYfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NUDj[HF[OTV3OUi4NVQ>
G384D Mne2R4VtdCCYaXHibYxqfHliQYPzZZk> MnLwNE01ODBibl2= MV60PEBp MonkbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MUCxOVU6QDhzNB?=
F384L M3yxbGNmdGxiVnnhZoltcXS7IFHzd4F6 NFXjZZIxNTRyMDDuUS=> MmrROFghcA>? Mom0bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MUmxOVU6QDhzNB?=
KMS11 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL5O|IhcA>? MV\JR|UxRTlyIH7N NUOzSXM{OTV3OUi4NVQ>
KMS18 M2GyWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnIV206PzJiaB?= NU\4eoNSUUN3ME21OVAhdk1? M1q4SVE2PTl6OEG0
OPM2 NGDvUohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUK3NkBp NIjnOIhKSzVyPUmwJI5O NEDQNHcyPTV7OEixOC=>
H929 M{L2d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PDV|czKGh? MVvJR|UxRiB{NUCwJI5O NFyzZ5gyPTV7OEixOC=>
8226 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2T2blczKGh? M33m[2lEPTB-IEK1NFAhdk1? MXOxOVU6QDhzNB?=
U266 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jIUFczKGh? M4XBS2lEPTB-IEK1NFAhdk1? MX2xOVU6QDhzNB?=

... Click to View More Cell Line Experimental Data

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]


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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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


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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01497392 Completed Adenocarcinoma of the Pancreas|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer|Unspecified Adult Solid Tumor, Protocol Specific Roswell Park Cancer Institute|National Cancer Institute (NCI)|Novartis March 29, 2012 Phase 1
NCT02048943 Withdrawn Duct Cell Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer|Unspecified Adult Solid Tumor, Protocol Specific Roswell Park Cancer Institute|National Cancer Institute (NCI)|Novartis March 2015 Phase 1
NCT02268435 Withdrawn Gastrointestinal Stromal Tumors Asan Medical Center March 2015 Phase 1
NCT02108782 Withdrawn Gastrinoma|Glucagonoma|Insulinoma|Pancreatic Polypeptide Tumor|Recurrent Islet Cell Carcinoma|Somatostatinoma Academic and Community Cancer Research United|National Cancer Institute (NCI) October 2014 Phase 2
NCT02116803 Completed Solid Tumors Novartis Pharmaceuticals|Novartis May 2014 Phase 2|Phase 3
NCT01994590 Active, not recruiting Prostate Cancer M.D. Anderson Cancer Center|Novartis May 2014 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID