Dovitinib (TKI-258, CHIR-258)

Dovitinib (TKI-258, CHIR-258)は非常に強い、新型の多い標的阻害剤、FLT3、c - kit、受容体、マウス/2/3、成長因子受容体と球コロニー刺激因子受容体ßに作用する時、IC50がそれぞれ 1 nM, 2 nM, 5 nM, 10 nM, 8 nM, 27 nM と 36 nMになる。

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Dovitinib (TKI-258, CHIR-258) 化学構造
分子量: 392.43

高品質保証

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Quality Control & MSDS

製品説明

  • Compare FLT3 Inhibitors
    FLT3製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Dovitinib (TKI-258, CHIR-258)は非常に強い、新型の多い標的阻害剤、FLT3、c - kit、受容体、マウス/2/3、成長因子受容体と球コロニー刺激因子受容体ßに作用する時、IC50がそれぞれ 1 nM, 2 nM, 5 nM, 10 nM, 8 nM, 27 nM と 36 nMになる。
ターゲット Flt3 c-Kit FGFR1/3 VEGFR1/2/3 PDGFRα/β
IC50 1 nM 2 nM 8 nM/9 nM 10 nM/13 nM/8 nM 210 nM/27 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
SupB15 NYjvOpZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvCTWM2OD1yLkS0PUDPxE1? NVnoNHY{OjV{MEKwO|M>
SupB15-R NHXkO5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXmzUXY4UUN3ME2wMlU2QCEQvF2= MlXaNlUzODJyN{O=
BaF3-pSRα Mk\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXztS4wzUUN3ME2wMlY3QCEQvF2= MkDCNlUzODJyN{O=
BaF3-p210Bcr-Abl NYDXNVRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEm0R29KSzVyPUCuOlkzKM7:TR?= MWiyOVIxOjB5Mx?=
BaF3-p210Bcr-Abl-T315I NUH0NXluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2mx[mlEPTB;Mj62NlYh|ryP M{TpOFI2OjB{MEez
CCRF-CEM NFXJ[XBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkT0TWM2OD1yLkO5PEDPxE1? NH3Sem0zPTJyMkC3Ni=>
CEM/C2 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnZTWM2OD1zLkGyOUDPxE1? MnLqNlUzODJyN{K=
Nalm-6 MmLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLQTWM2OD1yLkO4NkDPxE1? MUmyOVIxOjB5Mh?=
SEM-K2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwMEKyJO69VQ>? NELSU2czPTJyMkC3Ni=>
HB-1119 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInpTYJKSzVyPUCuNFI5KM7:TR?= MoXQNlUzODJyN{K=
RS4:11 MoLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTJwOEGg{txO M4DRWlI2OjB{MEey
Nalm-6 NVHab2NCSXCxcITvd4l{KEG|c3H5 MnLJNkDPxE1? MVSyOE81QCCq MYXpcoR2[2W|IHHwc5B1d3OrczDy[ZN2dHSrbnegbY4h[WKxdYSgO|ImKG:oIHPlcIwh\GWjdHigZYZ1\XJiMkSgbEB1emWjdH3lcpQh[W6mIEixKUBi\nSncjC0PEBp NI\ON4IzPTJyMkC3Ni=>
SEM-K2 M37DO2Fxd3C2b4Ppd{BCe3OjeR?= M1eye|AvOS9zIN88US=> M1XONVI1KGh? NF7FXnlqdmS3Y3XzJIViemy7IHHwc5B1d3OrczDv[kBUTU1vS{KgZ4VtdHNiYYSgNE4yKM7:TTDh[pRmeiB{NDDo NWDWZ2xpOjV{MEKwO|I>
HCT-116 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDJWVd1UUN3ME2zMlA2OC53ODFOwG0> M4XmRVI1PDl3N{Ww
HT-29 MkO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzyeJdKSzVyPUWuNlEvQTNizszN M4nBSVI1PDl3N{Ww
SW-480 NHfYU4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLJO4VZUUN3ME20MlM{OC52NzFOwG0> MnzMNlQ1QTV5NUC=
CaCO2 MlnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3y3SmlEPTB;Mz6yN|AvPjRizszN Mm\WNlQ1QTV5NUC=
LS174T NU\sZ2V4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37iRWlEPTB;ND6zN|AvPDdizszN NWSyT3VZOjR2OUW3OVA>
HEC-1A MUfGeY5kfGmxbjDBd5NigQ>? NFrQ[HcxNjB3L{CuNU8xNjVizszN M{nNUFczKGh? MY\jZZV{\XNiYTDk[YNz\WG|ZTDpckBUXEGWMzygSXJMNCCjbnSgRWtVKHCqb4PwbI9zgWyjdHnvci=> M4O5UVI1PDl3N{Ww
AN3CA NFXPPYRHfW6ldHnvckBCe3OjeR?= Mn3pNE4xPS9yLkGvNE42KM7:TR?= NI\uV2c4OiCq NXLYXI5s[2G3c3XzJIEh\GWlcnXhd4UhcW5iU2TBWFMtKEWUSzygZY5lKEGNVDDwbI9{eGixconsZZRqd25? M1rXUlI1PDl3N{Ww
MFE-296  NHLK[5pHfW6ldHnvckBCe3OjeR?= M3XoN|AvODVxMD6xM|AvPSEQvF2= MVG3NkBp NIfqUZNk[XW|ZYOgZUBl\WO{ZXHz[UBqdiCVVFHUN{whTVKNLDDhcoQhSUuWIIDoc5NxcG:{eXzheIlwdg>? MYKyOFQ6PTd3MB?=
UMC3 NEXabFVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXTkWIpNOS1zMDFOwG0> MlfaO|IhcA>? MnK0bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NYXKbXNsOjR|MkW0OlE>
5637 NYm1bZBuS2WubDDWbYFjcWyrdImgRZN{[Xl? NUPkdmtNOS1zMDFOwG0> NHrT[lg4OiCq NGO4OY9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? M2rFSlI1OzJ3NE[x
HU456 MmLaR4VtdCCYaXHibYxqfHliQYPzZZk> NXzSUZBWOS1zMDFOwG0> Mo\4O|IhcA>? NECzSIVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MViyOFMzPTR4MR?=
MGHU4 MnzIR4VtdCCYaXHibYxqfHliQYPzZZk> NVrXcIV{OS1zMDFOwG0> Ml\pO|IhcA>? NHexdFFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MnjsNlQ{OjV2NkG=
HT1376 MVrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MX2xMVExKM7:TR?= MVu3NkBp NVzEb|RZcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M3;hO|I1OzJ3NE[x
RT112 MlrGR4VtdCCYaXHibYxqfHliQYPzZZk> MXixMVExKM7:TR?= NX\EO41OPzJiaB?= MVLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NG\MeoozPDN{NUS2NS=>
T24 Ml3tR4VtdCCYaXHibYxqfHliQYPzZZk> MVOxMVExKM7:TR?= NHj6TW04OiCq Mn;ybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M13FXlI1OzJ3NE[x
BFTC905 NVmwRnpVS2WubDDWbYFjcWyrdImgRZN{[Xl? NWrMeo9MOS1zMDFOwG0> NYPmS4ZXPzJiaB?= NH\zSItqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MlfJNlQ{OjV2NkG=
TCC-SUP MWTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWT4fZRXOS1zMDFOwG0> MXG3NkBp M1[3OolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MX2yOFMzPTR4MR?=
RT4 MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWexMVExKM7:TR?= NX3TZ4N6PzJiaB?= NVi1PJVCcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M3LZblI1OzJ3NE[x
HONE1 MmHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLtNlgxNjFvMUCg{txO NUXXeoU1PDkEoHi= MlK0bY5lfWOnczDHNk9OKGSnbHH5JIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy M3z3U|I1OjN6MEm0
HNE1 M4rPPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWKwMlEuOTBizszN MlTwOFjDqGh? M4XJbIlv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> Mnu0NlQzOzhyOUS=
CNE2  NYHwbIZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHj1O5ExNjFvMUCg{txO NILUe2g1QMLiaB?= M{D5PIlv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> M2\wWVI1OjN6MEm0
C666-1 NELIXodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULvfot{OC5zLUGwJO69VQ>? M2rsUVQ5yqCq M4n4ZYlv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> MWqyOFI{QDB7NB?=
HeLa NHq4bGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXqwMlEuOTBizszN M{\ESFI1KGh? Mn6ybY5lfWOnczDHNk9OKGG{cnXzeEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NHHNdoQzPDJ|OEC5OC=>
Hep3B M4ntO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTLNE4yNTFyIN88US=> MVuyOEBp M120[Ilv\HWlZYOgS|LDqGG{cnXzeOKh NVPo[pB5OjR{M{iwPVQ>
HepG2 MlLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDqOFghcA>? MkPxTWM2OD1{LkeyO{DDuSByLkSyPUDPxE1? NFzHWlAzOzV2NkW5NS=>
Hep3B NHzWTGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUT5UoltPDhiaB?= NHq4dHRKSzVyPUSuNlI{KMLzIECuPFM6KM7:TR?= M3ziZlI{PTR4NUmx
PLC/PRF5 MlfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmL0OFghcA>? M3fXdmlEPTB;MU[uNVIxKMLzIESuNFAyKM7:TR?= NFzOW2wzOzV2NkW5NS=>
Huh7 NXuzSHhnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTYOFghcA>? M1ywUWlEPTB;MUWuNFA4KMLzIEeuN|M1KM7:TR?= M1K3XFI{PTR4NUmx
HepG2 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHi0XJc4OiCq MkfiTWM2OD1zLkKwNEDDuSByLkKyOkDPxE1? MmTuNlM2PDZ3OUG=
Hep3B NWLTcJJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;Qe|czKGh? M1XQbGlEPTB;MD64PVIhyrFiMD6wOFQh|ryP NY[xZ2xwOjN3NE[1PVE>
PLC/PRF5 MoLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;OO|IhcA>? NWq4TGNtUUN3ME2zMlEyOCEEsTCwMlM{PyEQvF2= M3vLSFI{PTR4NUmx
Huh7 NIiwT3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1S1bVczKGh? M2DkWGlEPTB;Mz65PFAhyrFiMD64NFMh|ryP NFiyToczOzV2NkW5NS=>
MFE280 NHzBVINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonsTWM2OD1yLkSyJOKyKDBwME[g{txO NX;zTJJKOjN2NEO4NFU>
AN3CA MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLJTWM2OD1yLkWwJOKyKDBwMUCg{txO M3[yblI{PDR|OEC1
HEC155 Mlu4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17odmlEPTB;MD62OkDDuSByLkC5JO69VQ>? MoX1NlM1PDN6MEW=
MFE296 NXHYXHBDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTPTo5KSzVyPUCuOlYhyrFiMD6xPUDPxE1? NWfYcmlROjN2NEO4NFU>
SPAC1S MlrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWL5dolWUUN3ME2wMlc4KMLzIECuNFgh|ryP NWnNUlhCOjN2NEO4NFU>
RL952 M{T6S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TWVmlEPTB;MD65N{DDuSByLkCxJO69VQ>? M2\aSVI{PDR|OEC1
EN1 NIjTfJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGGwVGhKSzVyPUGuNFIhyrFiMD6yOUDPxE1? MVuyN|Q1OzhyNR?=
SNGII MoDLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTFwMkSgxtEhOC5{ODFOwG0> MV[yN|Q1OzhyNR?=
ISHIKAWA MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTFwM{CgxtEhOC5zMTFOwG0> MXqyN|Q1OzhyNR?=
HEC1A NIjjVGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTFwM{SgxtEhOC5|MDFOwG0> NF;vb2EzOzR2M{iwOS=>
KLE MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTFwM{egxtEhOC5yMjFOwG0> MoHQNlM1PDN6MEW=
SNGM MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\yN2lEPTB;MT60NkDDuSByLkGzJO69VQ>? NXfCVoJ2OjN2NEO4NFU>
USPC2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjTPFViUUN3ME2xMlYzKMLzIECuNFEh|ryP NUjD[|B1OjN2NEO4NFU>
EN MmKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTFwNk[gxtEhOC5yMTFOwG0> NHG0Z4MzOzR2M{iwOS=>
MFE319 NXfoOIluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnlN3MxUUN3ME2xMlg4KMLzIECuOFUh|ryP NYO5bnQzOjN2NEO4NFU>
EFE184 NGTkWo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvITWM2OD1{LkC0JOKyKDBwMUOg{txO NHrid|EzOzR2M{iwOS=>
ECC1 M{DmTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXqwSJNUUUN3ME2yMlA4KMLzIECuNFEh|ryP MkSzNlM1PDN6MEW=
HEC1B MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHmd3JrUUN3ME2yMlU4KMLzIECuNlMh|ryP NE\ER4czOzR2M{iwOS=>
USPC1 MmLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rkc2lEPTB;Mj62NEDDuSByLkGzJO69VQ>? Mn72NlM1PDN6MEW=
SPAC1L NUjqZ5VFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTNwME[gxtEhOS5zNDFOwG0> NYnhXHljOjN2NEO4NFU>
HUVEC NXOxcnY2S2WubDDWbYFjcWyrdImgRZN{[Xl? MV[wMVI2KM7:TR?= NWLFd5NNPzJiaB?= M1HWTGROW09? NXu2XGx3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NVK5Z5lwOjN{MkiwNVc>
HMVEC Mn3RR4VtdCCYaXHibYxqfHliQYPzZZk> NEjpOHgxNTJ3IN88US=> Mo\lO|IhcA>? NFrWXFFFVVOR MmLBbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NUjqcolYOjN{MkiwNVc>
MHCC-97H MlSzR4VtdCCYaXHibYxqfHliQYPzZZk> M1\5d|AuOjVizszN MYK3NkBp MkP4SG1UVw>? M1HkWIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MlfTNlMzOjhyMUe=
SMMC7721 MkPiR4VtdCCYaXHibYxqfHliQYPzZZk> MUOwMVI2KM7:TR?= NIfpNHQ4OiCq NGnJV4ZFVVOR MUDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MlrNNlMzOjhyMUe=
Huh-7 MmrhRZBweHSxc3nzJGF{e2G7 MUCwMVEzNjVizszN NVXBZ3ZSOjRiaB?= MoCzSG1UV8Li Mnjmd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M3PsPVIzOjNyNEe5
Sk-Hep1 MorSRZBweHSxc3nzJGF{e2G7 NHnUfZYxNTF{LkWg{txO NGSwWowzPCCq M1PU[mROW00EoB?= NWr1S3hWe2Wwc3n0bZpmeyCKQ1OgZ4VtdHNidH:gWHJCUUxvIHHu[EB1cWejdIX6eY1i[i2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mkj6NlIzOzB2N{m=
Hep3B NXToTIQ1SXCxcITvd4l{KEG|c3H5 NVLCVJA2OC1zMj61JO69VQ>? MVOyOEBp M4rK[WROW00EoB?= M3fqd5NmdnOrdHn6[ZMhUEOFIHPlcIx{KHSxIGTSRWlNNSCjbnSgeIlo[XS3eoXtZYIucW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MnjsNlIzOzB2N{m=
PLC5 M1LI[mFxd3C2b4Ppd{BCe3OjeR?= NWHqVYNVOC1zMj61JO69VQ>? MUCyOEBp NWfzUlNxTE2VT9Mg M17wWpNmdnOrdHn6[ZMhUEOFIHPlcIx{KHSxIGTSRWlNNSCjbnSgeIlo[XS3eoXtZYIucW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1f5WFIzOjNyNEe5
PLC5 MnvyR4VtdCCYaXHibYxqfHliQYPzZZk> M2fiRVAuOTVizszN NVfTcXdxPzJiaB?= NYXLNndIemWmdXPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg MUSyNlE5ODNyOB?=
Hep3B MnTWR4VtdCCYaXHibYxqfHliQYPzZZk> MmjCNE0yPSEQvF2= M1vjeFczKGh? NWfORmZxemWmdXPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg NFXte5AzOjF6MEOwPC=>
Sk-Hep1 MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1\TbFAuOTVizszN NGSxUXY4OiCq NIDrc3dz\WS3Y3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= NXP4enFSOjJzOECzNFg>
Huh-7 M1vhOmNmdGxiVnnhZoltcXS7IFHzd4F6 MWSwMVE2KM7:TR?= NWm4Z4lNPzJiaB?= M{\wcJJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NIPVNIMzOjF6MEOwPC=>
PLC5 MlXLRZBweHSxc3nzJGF{e2G7 MWWwMVE2KM7:TR?= M1T6V|I1KGh? MmjtbY5kemWjc3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? Ml7wNlIyQDB|MEi=
Hep3B MoLMRZBweHSxc3nzJGF{e2G7 MorQNE0yPSEQvF2= M3;HXVI1KGh? M4S5UYlv[3KnYYPld{BieG:ydH;0bYMh[2WubDDk[YF1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi MnXONlIyQDB|MEi=
Sk-Hep1 NH3WXGlCeG:ydH;zbZMhSXO|YYm= M4H6dlAuOTVizszN MoewNlQhcA>? NXznem81cW6lcnXhd4V{KGGyb4D0c5Rq[yClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= NUjXcFI5OjJzOECzNFg>
Huh-7 Mo\oRZBweHSxc3nzJGF{e2G7 NYXpR21wOC1zNTFOwG0> M2OzSlI1KGh? NYG0fGFMcW6lcnXhd4V{KGGyb4D0c5Rq[yClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M{i2e|IzOThyM{C4
PLC5 MUTGeY5kfGmxbjDBd5NigQ>? NWCxfY9JOC1zMDFOwG0> NEezWIozPCCq MX7jZZV{\XNiZH;z[U1l\XCnbnTlcpQhTE6DIH\yZYdu\W62YYTpc44> NHzPdG0zOjF6MEOwPC=>
Hep3B M12zbmZ2dmO2aX;uJGF{e2G7 NXXXPFVsOC1zMDFOwG0> MX[yOEBp M1vm[4NifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? M3OxS|IzOThyM{C4
Sk-Hep1 NGDPS3RHfW6ldHnvckBCe3OjeR?= M4W1[lAuOTBizszN NYPJd3RIOjRiaB?= MXXjZZV{\XNiZH;z[U1l\XCnbnTlcpQhTE6DIH\yZYdu\W62YYTpc44> NFf3eJozOjF6MEOwPC=>
Huh-7 MVXGeY5kfGmxbjDBd5NigQ>? M4LvfFAuOTBizszN NHXOXY0zPCCq MlPpZ4F2e2W|IHTvd4Uu\GWyZX7k[Y51KESQQTDmdoFodWWwdHH0bY9v MonlNlIyQDB|MEi=
SW780 MkPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVW1JIQ> MV\JR|UxRTVyIH7N NFfQfmUzOTFzOU[2NS=>
RT112 NX3BdFVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\VelU2KGR? MoOwTWM2OD1zNTDuUS=> NIrTOHYzOTFzOU[2NS=>
RT4 NX23WWVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml2wOUBl MULJR|UxRTVibl2= MUKyNVEyQTZ4MR?=
JMSU1 Mn:5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTp[JNPPSCm M{m0ZmlEPTB;NUCgcm0> MWKyNVEyQTZ4MR?=
J82 NX;RR|UxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTkOUBl NFnSfZBKSzVyPUG0NFAhdk1? MWGyNVEyQTZ4MR?=
97-7 NWnFZnNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXy1JIQ> NWPzOoN4UUN3ME2xNFAxKG6P NGHDflkzOTFzOU[2NS=>
RT112 NH7WUVRHfW6ldHnvckBCe3OjeR?= M33HbFUxOCCwTR?= NFzRNIUzPCCq M3LzOIlv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= NGnNZWozOTFzOU[2NS=>
RT4 MVrGeY5kfGmxbjDBd5NigQ>? M2LOeFUxOCCwTR?= MXSyOEBp M3fOO4lv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= MnO1NlEyOTl4NkG=
MGH-U3 NHHiUnFHfW6ldHnvckBCe3OjeR?= MUC1NFAhdk1? NXvwUmdpOjRiaB?= MYHpcoNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gS|HDqGGlY3;tdIFvcWWmIHL5JIEh\GWlcnXhd4UhcW5iUzDhcoQhTzJxTTDwbIF{\XN? NVTMWFRoOjFzMUm2OlE>
SW780 NHPXU4hHfW6ldHnvckBCe3OjeR?= MkL5OVAxKG6P M3\SWlI1KGh? NEfzelVqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= M4iwOlIyOTF7Nk[x
97-7 M1njW2Z2dmO2aX;uJGF{e2G7 NWfVSnNkPTByIH7N NELoN3EzPCCq Moq5bY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| NVXXVpc6OjFzMUm2OlE>
 J807C NFnjZ3ZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{O1ZlAuPDByIH7N NGruS5M1QCCq M2j4RolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NFnkdpUyPTV7OEixOC=>
Y373C MkDqR4VtdCCYaXHibYxqfHliQYPzZZk> NV:2PXVROC12MECgcm0> M1zCT|Q5KGh? M2LEUIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NH7lNYIyPTV7OEixOC=>
K650E MmTUR4VtdCCYaXHibYxqfHliQYPzZZk> M3rwfVAuPDByIH7N MmPmOFghcA>? MnjHbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NGPtfpYyPTV7OEixOC=>
G384D Mn\TR4VtdCCYaXHibYxqfHliQYPzZZk> NV62dno3OC12MECgcm0> MnT0OFghcA>? NEXY[5lqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? Mlj6NVU2QTh6MUS=
F384L NGTQSGJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3vJ[|AuPDByIH7N MmfGOFghcA>? MVTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MoD6NVU2QTh6MUS=
KMS11 NFzaWnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjMepRNPzJiaB?= M2rX[WlEPTB;OUCgcm0> MYixOVU6QDhzNB?=
KMS18 MnHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnQWI84OiCq M4nyeGlEPTB;NUWwJI5O MYmxOVU6QDhzNB?=
OPM2 MoLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPZNlM4OiCq NGHCZ|VKSzVyPUmwJI5O MnL1NVU2QTh6MUS=
H929 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXmx[FNwPzJiaB?= NV7JcJhqUUN3ME6gNlUxOCCwTR?= NUn1fo9oOTV3OUi4NVQ>
8226 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYK3NkBp NHi5d|dKSzVyPjCyOVAxKG6P MnPSNVU2QTh6MUS=
U266 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjiNldDPzJiaB?= NF\4bllKSzVyPjCyOVAxKG6P MXKxOVU6QDhzNB?=

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 Dovitinib has entered in a phase II clinical trial for the treatment of adenoid cystic carcinoma.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.

細胞アッセイ: [1]

細胞株 B9 cells, MM cell lines
濃度 100 nM
反応時間 48-96 hours
実験の流れ 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.

動物実験: [1]

動物モデル 8-week-old female BNX mice bearing KMS11 cells
製剤 5 mM citrate buffer
投薬量 10, 30, or 60 mg/kg
投与方法 Gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Dovitinib (TKI-258, CHIR-258) SDF
分子量 392.43
化学式

C21H21FN6O

CAS No. 405169-16-6
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 30 mg/mL (76.44 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
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.
化学名 1-amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one

文献中の引用 (7)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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