Dovitinib (TKI-258)

For research use only.

Catalog No.S1018 Synonyms: CHIR-258

34 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 34 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 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWX6[GVCUUN3ME2wMlQ1QSEQvF2= NYrlVpJCOjV{MEKwO|M>
SupB15-R NELzfXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPyOpd3UUN3ME2wMlU2QCEQvF2= MlPUNlUzODJyN{O=
BaF3-pSRα NY\SfWRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPiSlVrUUN3ME2wMlY3QCEQvF2= M2HlU|I2OjB{MEez
BaF3-p210Bcr-Abl M3XiWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIX0[plKSzVyPUCuOlkzKM7:TR?= MkfjNlUzODJyN{O=
BaF3-p210Bcr-Abl-T315I Mn;WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37XVWlEPTB;Mj62NlYh|ryP NG\BfYQzPTJyMkC3Ny=>
CCRF-CEM NXTCNJNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Kxb2lEPTB;MD6zPVgh|ryP NGK5SHAzPTJyMkC3Ni=>
CEM/C2 M{i1ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTFwMUK1JO69VQ>? NGL6PYszPTJyMkC3Ni=>
Nalm-6 NYXEOG5HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7wTWM2OD1yLkO4NkDPxE1? MlrDNlUzODJyN{K=
SEM-K2 MoqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnO0TWM2OD1yLkCyNkDPxE1? NHXQemIzPTJyMkC3Ni=>
HB-1119 NWDkXZlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLKTWM2OD1yLkCyPEDPxE1? NGjCVY8zPTJyMkC3Ni=>
RS4:11 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTrdpB1UUN3ME2yMlgyKM7:TR?= NFm2WVQzPTJyMkC3Ni=>
Nalm-6 M1fVemFxd3C2b4Ppd{BCe3OjeR?= M13K[FIh|ryP NVGxXYdDOjRxNEigbC=> M3jo[Ilv\HWlZYOgZZBweHSxc3nzJJJme3WudHnu[{BqdiCjYn;1eEA4OiVib3[gZ4VtdCCmZXH0bEBi\nSncjCyOEBpKHS{ZXH0cYVvfCCjbnSgPFEmKGGodHXyJFQ5KGh? NEPKU4YzPTJyMkC3Ni=>
SEM-K2 MnzPRZBweHSxc3nzJGF{e2G7 MYGwMlEwOSEQvF2= MoHENlQhcA>? M2\VRolv\HWlZYOg[YFzdHliYYDvdJRwe2m|IH;mJHNGVS2NMjDj[YxteyCjdDCwMlEh|ryPIHHmeIVzKDJ2IHi= NX:we|R{OjV{MEKwO|I>
HCT-116 MmjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTkV3RIUUN3ME2zMlA2OC53ODFOwG0> MVOyOFQ6PTd3MB?=
HT-29 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDTd3pbUUN3ME21MlIyNjl|IN88US=> MlTONlQ1QTV5NUC=
SW-480 NHjXfIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPIco1[UUN3ME20MlM{OC52NzFOwG0> MlvSNlQ1QTV5NUC=
CaCO2 NIPaU5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvqdIxYUUN3ME2zMlI{OC54NDFOwG0> NWnnS3Y3OjR2OUW3OVA>
LS174T NXPuXJg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVqyeVlEUUN3ME20MlM{OC52NzFOwG0> NXf1VndxOjR2OUW3OVA>
HEC-1A MVvGeY5kfGmxbjDBd5NigQ>? NXzBeGYzOC5yNT:wMlEwOC53IN88US=> Mnf4O|IhcA>? NF\wd3Bk[XW|ZYOgZUBl\WO{ZXHz[UBqdiCVVFHUN{whTVKNLDDhcoQhSUuWIIDoc5NxcG:{eXzheIlwdg>? NUnrW5d2OjR2OUW3OVA>
AN3CA NXPVWoxuTnWwY4Tpc44hSXO|YYm= NHTmOXQxNjB3L{CuNU8xNjVizszN MlPOO|IhcA>? NFLmToZk[XW|ZYOgZUBl\WO{ZXHz[UBqdiCVVFHUN{whTVKNLDDhcoQhSUuWIIDoc5NxcG:{eXzheIlwdg>? MmPZNlQ1QTV5NUC=
MFE-296  Mkj2SpVv[3Srb36gRZN{[Xl? M3e5V|AvODVxMD6xM|AvPSEQvF2= M1zKR|czKGh? NWXqVWly[2G3c3XzJIEh\GWlcnXhd4UhcW5iU2TBWFMtKEWUSzygZY5lKEGNVDDwbI9{eGixconsZZRqd25? Mk\wNlQ1QTV5NUC=
UMC3 M4D3cmNmdGxiVnnhZoltcXS7IFHzd4F6 MkX1NU0yOCEQvF2= NFT4cnM4OiCq MY\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MmDiNlQ{OjV2NkG=
5637 MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYDRUmp2OS1zMDFOwG0> NFzyfHg4OiCq MlLtbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MnHGNlQ{OjV2NkG=
HU456 MUDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWWxMVExKM7:TR?= M4HzfFczKGh? MWDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NVP3TI9sOjR|MkW0OlE>
MGHU4 NV7iZZg2S2WubDDWbYFjcWyrdImgRZN{[Xl? MlfBNU0yOCEQvF2= M3XtdFczKGh? NXPqblVWcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MkjrNlQ{OjV2NkG=
HT1376 MYrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYHsdGdiOS1zMDFOwG0> MW[3NkBp NFvzNI9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MlizNlQ{OjV2NkG=
RT112 MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmTyNU0yOCEQvF2= MWK3NkBp MlTxbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NXjIcos6OjR|MkW0OlE>
T24 M2Ln[GNmdGxiVnnhZoltcXS7IFHzd4F6 M4DiXFEuOTBizszN MXy3NkBp MXTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M1nQPFI1OzJ3NE[x
BFTC905 NXjx[lZlS2WubDDWbYFjcWyrdImgRZN{[Xl? MnO1NU0yOCEQvF2= MWi3NkBp M2jxdYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M3L3OVI1OzJ3NE[x
TCC-SUP NGD0SY9E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWSxMVExKM7:TR?= MlHvO|IhcA>? NE\jSohqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M3mwPFI1OzJ3NE[x
RT4 Mn;vR4VtdCCYaXHibYxqfHliQYPzZZk> NHn1bWwyNTFyIN88US=> MWq3NkBp MljQbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NF[5d2UzPDN{NUS2NS=>
HONE1 Mor5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2P3OVAvOS1zMDFOwG0> NHn0XGk1QMLiaB?= MluzbY5lfWOnczDHNk9OKGSnbHH5JIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy MlTUNlQzOzhyOUS=
HNE1 M4qyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY[wMlEuOTBizszN MXS0POKhcA>? M4TUeYlv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> M3v3RVI1OjN6MEm0
CNE2  M3jVR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjnT|gxOC5zLUGwJO69VQ>? NYXtR|h5PDkEoHi= MX;pcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= MkXsNlQzOzhyOUS=
C666-1 NX;WSGt3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXmSXQ{OC5zLUGwJO69VQ>? MYe0POKhcA>? MU\pcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= NYXiNm95OjR{M{iwPVQ>
HeLa NHLmNIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknHNE4yNTFyIN88US=> MoDrNlQhcA>? NFXo[ZVqdmS3Y3XzJGczN01iYYLy[ZN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NIDhdIMzPDJ|OEC5OC=>
Hep3B MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPhPXM5OC5zLUGwJO69VQ>? M{XVVFI1KGh? NFywOVJqdmS3Y3XzJGczyqCjcoLld5TDqA>? NFe4ZWIzPDJ|OEC5OC=>
HepG2 NVnFdotET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{m0UFQ5KGh? MUjJR|UxRTJwN{K3JOKyKDBwNEK5JO69VQ>? MlP0NlM2PDZ3OUG=
Hep3B NFHZTYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXqyVJZQPDhiaB?= NXS5dGhKUUN3ME20MlIzOyEEsTCwMlg{QSEQvF2= NVG5VYg6OjN3NE[1PVE>
PLC/PRF5 NGjkcnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDWN2R{PDhiaB?= M2XLV2lEPTB;MU[uNVIxKMLzIESuNFAyKM7:TR?= MWCyN|U1PjV7MR?=
Huh7 MkLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3qOFghcA>? MYHJR|UxRTF3LkCwO{DDuSB5LkOzOEDPxE1? MkD3NlM2PDZ3OUG=
HepG2 NYDSbGY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETBbIQ4OiCq NVPpO25sUUN3ME2xMlIxOCEEsTCwMlIzPiEQvF2= NIjYPI0zOzV2NkW5NS=>
Hep3B M3i1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULaUJh[PzJiaB?= MkPJTWM2OD1yLki5NkDDuSByLkC0OEDPxE1? NGX2NGgzOzV2NkW5NS=>
PLC/PRF5 NFvEfW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoO3O|IhcA>? MVPJR|UxRTNwMUGwJOKyKDBwM{O3JO69VQ>? M4fNVlI{PTR4NUmx
Huh7 M4\2RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfmO|IhcA>? MYjJR|UxRTNwOUiwJOKyKDBwOECzJO69VQ>? M4\LeFI{PTR4NUmx
MFE280 NXXqfnVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX75UZltUUN3ME2wMlQzKMLzIECuNFYh|ryP MV:yN|Q1OzhyNR?=
AN3CA M2\1cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDqVmo5UUN3ME2wMlUxKMLzIECuNVAh|ryP NFrlfIgzOzR2M{iwOS=>
HEC155 MofCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDBSXRKSzVyPUCuOlYhyrFiMD6wPUDPxE1? MmLMNlM1PDN6MEW=
MFE296 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPTZ3F4UUN3ME2wMlY3KMLzIECuNVkh|ryP NUCz[HRFOjN2NEO4NFU>
SPAC1S MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTBwN{egxtEhOC5yODFOwG0> MV:yN|Q1OzhyNR?=
RL952 M3uxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTBwOUOgxtEhOC5yMTFOwG0> MWOyN|Q1OzhyNR?=
EN1 NYjMfnRuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PCeWlEPTB;MT6wNkDDuSByLkK1JO69VQ>? NYXCXYV5OjN2NEO4NFU>
SNGII NVfmcXkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTZUHIyUUN3ME2xMlI1KMLzIECuNlgh|ryP NFnMVoczOzR2M{iwOS=>
ISHIKAWA NF7lTY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzqe|dNUUN3ME2xMlMxKMLzIECuNVEh|ryP NVPFOIhqOjN2NEO4NFU>
HEC1A MlfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4GzOmlEPTB;MT6zOEDDuSByLkOwJO69VQ>? MoTCNlM1PDN6MEW=
KLE MmLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPOXHZKSzVyPUGuN|chyrFiMD6wNkDPxE1? MYiyN|Q1OzhyNR?=
SNGM NGTM[GxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFwNEKgxtEhOC5zMzFOwG0> M1zBZlI{PDR|OEC1
USPC2 M3fLTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofxTWM2OD1zLk[yJOKyKDBwMEGg{txO NI\RT5IzOzR2M{iwOS=>
EN NXrQVo41T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfTN4JKSzVyPUGuOlYhyrFiMD6wNUDPxE1? MXyyN|Q1OzhyNR?=
MFE319 NYPFbXNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nmXWlEPTB;MT64O{DDuSByLkS1JO69VQ>? NGPTdm0zOzR2M{iwOS=>
EFE184 NV7SfG0yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrxVIpKSzVyPUKuNFQhyrFiMD6xN{DPxE1? NGrBS3gzOzR2M{iwOS=>
ECC1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\IOGttUUN3ME2yMlA4KMLzIECuNFEh|ryP NFLEWmQzOzR2M{iwOS=>
HEC1B NHzxZW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXK4U|BCUUN3ME2yMlU4KMLzIECuNlMh|ryP M1rXcVI{PDR|OEC1
USPC1 NICzbINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjXRW1uUUN3ME2yMlYxKMLzIECuNVMh|ryP MlPNNlM1PDN6MEW=
SPAC1L NVLOfXlPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLSfIdKSzVyPUOuNFYhyrFiMT6xOEDPxE1? NX7ibopzOjN2NEO4NFU>
HUVEC M4DuZWNmdGxiVnnhZoltcXS7IFHzd4F6 NVjWPVl4OC1{NTFOwG0> NF7UeWw4OiCq NEPObW9FVVOR MVLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MnrwNlMzOjhyMUe=
HMVEC Mn3DR4VtdCCYaXHibYxqfHliQYPzZZk> NHrmV5ExNTJ3IN88US=> MkjDO|IhcA>? MkjtSG1UVw>? MUfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NV6ydJJ2OjN{MkiwNVc>
MHCC-97H MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1rKNlAuOjVizszN NXT5bIJWPzJiaB?= NETLZ29FVVOR NEDNRmtqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M2G2clI{OjJ6MEG3
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Huh-7 NVz2fZBzSXCxcITvd4l{KEG|c3H5 NXvjRm9POC1zMj61JO69VQ>? NH\mRnAzPCCq MU\EUXNQyqB? NGLBV5d{\W6|aYTpfoV{KEiFQzDj[YxteyC2bzDUVmFKVC1iYX7kJJRq\2G2dYr1cYFjNWmwZIXj[YQh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYWyNlI{ODR5OR?=
Sk-Hep1 MXfBdI9xfG:|aYOgRZN{[Xl? NFGxNpIxNTF{LkWg{txO NFPRfG4zPCCq NYXYenhsTE2VT9Mg NInMPGd{\W6|aYTpfoV{KEiFQzDj[YxteyC2bzDUVmFKVC1iYX7kJJRq\2G2dYr1cYFjNWmwZIXj[YQh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MnLPNlIzOzB2N{m=
Hep3B M{L4dmFxd3C2b4Ppd{BCe3OjeR?= Ml33NE0yOi53IN88US=> NGD0WY8zPCCq NW\5OXFyTE2VT9Mg MVvz[Y5{cXSrenXzJGhESyClZXzsd{B1dyCWUlHJUE0h[W6mIITp[4F1fXq3bXHiMYlv\HWlZXSgZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MmXqNlIzOzB2N{m=
PLC5 M{Gy[WFxd3C2b4Ppd{BCe3OjeR?= MWWwMVEzNjVizszN MoLMNlQhcA>? M{DaXWROW00EoB?= NVHNc3gye2Wwc3n0bZpmeyCKQ1OgZ4VtdHNidH:gWHJCUUxvIHHu[EB1cWejdIX6eY1i[i2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mo[xNlIzOzB2N{m=
PLC5 MkLaR4VtdCCYaXHibYxqfHliQYPzZZk> NFy4NWYxNTF3IN88US=> NIK2SFk4OiCq MXny[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? NVLqUWNIOjJzOECzNFg>
Hep3B MWfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHTQNG8xNTF3IN88US=> Ml:3O|IhcA>? M4PPc5Jm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NVHRcIFIOjJzOECzNFg>
Sk-Hep1 NVHKVVJjS2WubDDWbYFjcWyrdImgRZN{[Xl? M{XLN|AuOTVizszN Mlq1O|IhcA>? M1zXUpJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NX7tVpE4OjJzOECzNFg>
Huh-7 M{PPRmNmdGxiVnnhZoltcXS7IFHzd4F6 M3LjblAuOTVizszN MXS3NkBp M4rMfZJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MkfnNlIyQDB|MEi=
PLC5 M1X2cWFxd3C2b4Ppd{BCe3OjeR?= NXLyTpZkOC1zNTFOwG0> MV:yOEBp NHjHWoJqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MV:yNlE5ODNyOB?=
Hep3B NFzLNVBCeG:ydH;zbZMhSXO|YYm= MWiwMVE2KM7:TR?= MknXNlQhcA>? NX63VpZ4cW6lcnXhd4V{KGGyb4D0c5Rq[yClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= MUGyNlE5ODNyOB?=
Sk-Hep1 MWDBdI9xfG:|aYOgRZN{[Xl? MUGwMVE2KM7:TR?= NUL3TmlwOjRiaB?= MYDpcoNz\WG|ZYOgZZBweHSxdHnjJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZLDqA>? M4HDRVIzOThyM{C4
Huh-7 NXjBdVJkSXCxcITvd4l{KEG|c3H5 NXL0VmZCOC1zNTFOwG0> MYCyOEBp MU\pcoNz\WG|ZYOgZZBweHSxdHnjJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZLDqA>? M2i2TVIzOThyM{C4
PLC5 NHHUOJVHfW6ldHnvckBCe3OjeR?= M4ToWlAuOTBizszN MlnSNlQhcA>? NYjV[3Z7[2G3c3XzJIRwe2VvZHXw[Y5l\W62IFTORUBnemGpbXXueIF1cW:w MWOyNlE5ODNyOB?=
Hep3B NIHncohHfW6ldHnvckBCe3OjeR?= NInYc4gxNTFyIN88US=> M2nGVFI1KGh? NVT5blVP[2G3c3XzJIRwe2VvZHXw[Y5l\W62IFTORUBnemGpbXXueIF1cW:w MkjnNlIyQDB|MEi=
Sk-Hep1 MoO2SpVv[3Srb36gRZN{[Xl? M4\lfVAuOTBizszN M2\ycFI1KGh? MYHjZZV{\XNiZH;z[U1l\XCnbnTlcpQhTE6DIH\yZYdu\W62YYTpc44> MX:yNlE5ODNyOB?=
Huh-7 MnHJSpVv[3Srb36gRZN{[Xl? M4HrTFAuOTBizszN M1TLc|I1KGh? M1PJZ4NifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? MoPaNlIyQDB|MEi=
SW780 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLxOUBl MWfJR|UxRTVyIH7N Ml74NlEyOTl4NkG=
RT112 NHG3cmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2C0RVUh\A>? MXzJR|UxRTF3IH7N MUSyNVEyQTZ4MR?=
RT4 MnHtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoC5OUBl MmjCTWM2OD13IH7N NFH5NnMzOTFzOU[2NS=>
JMSU1 NIfrcVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmroOUBl NI\ZTpFKSzVyPUWwJI5O M4fOb|IyOTF7Nk[x
J82 M{TkNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\RW|Uh\A>? MYDJR|UxRTF2MECgcm0> MVGyNVEyQTZ4MR?=
97-7 NVTzU3RFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXTbGg2KGR? M37z[WlEPTB;MUCwNEBvVQ>? NU\VU|ZrOjFzMUm2OlE>
RT112 NUm3RoNRTnWwY4Tpc44hSXO|YYm= M2Xz[lUxOCCwTR?= M{Hld|I1KGh? Ml3EbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| MnX6NlEyOTl4NkG=
RT4 M{jRc2Z2dmO2aX;uJGF{e2G7 NFXN[JU2ODBibl2= MlnYNlQhcA>? NGHVOIhqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= MUWyNVEyQTZ4MR?=
MGH-U3 NYfodG9ETnWwY4Tpc44hSXO|YYm= MUm1NFAhdk1? MlPPNlQhcA>? NGPnT3FqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= MV[yNVEyQTZ4MR?=
SW780 NF3jW5ZHfW6ldHnvckBCe3OjeR?= MU[1NFAhdk1? MUeyOEBp MUXpcoNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gS|HDqGGlY3;tdIFvcWWmIHL5JIEh\GWlcnXhd4UhcW5iUzDhcoQhTzJxTTDwbIF{\XN? M4LiR|IyOTF7Nk[x
97-7 M2fRfGZ2dmO2aX;uJGF{e2G7 MWO1NFAhdk1? MmnGNlQhcA>? NVjydGRNcW6lcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKEdzwrDhZ4NwdXCjbnnl[EBjgSCjIHTlZ5Jm[XOnIHnuJHMh[W6mIFeyM20heGijc3Xz M3fBRVIyOTF7Nk[x
 J807C M3r0WmNmdGxiVnnhZoltcXS7IFHzd4F6 MojhNE01ODBibl2= NHzpZWQ1QCCq NIi3O3JqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MXmxOVU6QDhzNB?=
Y373C M4HafmNmdGxiVnnhZoltcXS7IFHzd4F6 Mn;yNE01ODBibl2= NWX4PVR5PDhiaB?= M3i1U4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MVqxOVU6QDhzNB?=
K650E MWnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYLKdYdTOC12MECgcm0> MWq0PEBp NGKzSVNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MkSzNVU2QTh6MUS=
G384D MUXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWmwMVQxOCCwTR?= NF72RmM1QCCq NGTNdGhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHLod4UyPTV7OEixOC=>
F384L MXPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFvURo0xNTRyMDDuUS=> M1nqPFQ5KGh? M1nTe4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NXvue281OTV3OUi4NVQ>
KMS11 MoDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DNRlczKGh? NH7HW3pKSzVyPUmwJI5O MVSxOVU6QDhzNB?=
KMS18 NGrYSYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33YflczKGh? NUn0UoxTUUN3ME21OVAhdk1? NFrVfZYyPTV7OEixOC=>
OPM2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzFO|IhcA>? NED5[YhKSzVyPUmwJI5O MXqxOVU6QDhzNB?=
H929 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUW3NkBp NE\SSJhKSzVyPjCyOVAxKG6P NGrXOIoyPTV7OEixOC=>
8226 M3rxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTzWVRWPzJiaB?= M1fWbGlEPTB-IEK1NFAhdk1? M3X1dlE2PTl6OEG0
U266 M{H5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXNVFZKPzJiaB?= M3L2[mlEPTB-IEK1NFAhdk1? MnjUNVU2QTh6MUS=

... 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)
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Step 2: Enter the in vivo formulation ()
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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):
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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