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 NIfaVnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTncVM1UUN3ME2wMlQ1QSEQvF2= MUGyOVIxOjB5Mx?=
SupB15-R MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1[4OmlEPTB;MD61OVgh|ryP MljjNlUzODJyN{O=
BaF3-pSRα MnfnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTBwNk[4JO69VQ>? M{PQdVI2OjB{MEez
BaF3-p210Bcr-Abl MlHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\xZYpUUUN3ME2wMlY6OiEQvF2= MYSyOVIxOjB5Mx?=
BaF3-p210Bcr-Abl-T315I MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTJwNkK2JO69VQ>? M4\6SFI2OjB{MEez
CCRF-CEM NV3lZoRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfCd2FFUUN3ME2wMlM6QCEQvF2= NFvFSVYzPTJyMkC3Ni=>
CEM/C2 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2T0WmlEPTB;MT6xNlUh|ryP M3fBVFI2OjB{MEey
Nalm-6 MknOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XWNGlEPTB;MD6zPFIh|ryP M4PKfFI2OjB{MEey
SEM-K2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTPTWM2OD1yLkCyNkDPxE1? NGPnSWozPTJyMkC3Ni=>
HB-1119 NF7oW2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\xSYVKSzVyPUCuNFI5KM7:TR?= NUXPcGR1OjV{MEKwO|I>
RS4:11 NHLp[3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWToTFF7UUN3ME2yMlgyKM7:TR?= Mn\PNlUzODJyN{K=
Nalm-6 M37N[GFxd3C2b4Ppd{BCe3OjeR?= MnraNkDPxE1? MUmyOE81QCCq M1jUSIlv\HWlZYOgZZBweHSxc3nzJJJme3WudHnu[{BqdiCjYn;1eEA4OiVib3[gZ4VtdCCmZXH0bEBi\nSncjCyOEBpKHS{ZXH0cYVvfCCjbnSgPFEmKGGodHXyJFQ5KGh? MoHYNlUzODJyN{K=
SEM-K2 M12yT2Fxd3C2b4Ppd{BCe3OjeR?= M1fielAvOS9zIN88US=> NGDHT5czPCCq NX;EeYdlcW6mdXPld{Bm[XKueTDhdI9xfG:|aYOgc4YhW0WPLVuyJINmdGy|IHH0JFAvOSEQvF2gZYZ1\XJiMkSgbC=> MVKyOVIxOjB5Mh?=
HCT-116 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mki1TWM2OD1|LkC1NE42QCEQvF2= MX2yOFQ6PTd3MB?=
HT-29 NEPFcFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTVwMkGuPVMh|ryP NIXGRo8zPDR7NUe1NC=>
SW-480 NULhcm9ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjRV5ZKSzVyPUSuN|MxNjR5IN88US=> MnT2NlQ1QTV5NUC=
CaCO2 M1y2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXUTWM2OD1|LkKzNE43PCEQvF2= MV6yOFQ6PTd3MB?=
LS174T NGrjNXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLCRZN5UUN3ME20MlM{OC52NzFOwG0> NVvwN3BNOjR2OUW3OVA>
HEC-1A M{nYW2Z2dmO2aX;uJGF{e2G7 MYiwMlA2NzBwMT:wMlUh|ryP MY[3NkBp NUjWNWo2[2G3c3XzJIEh\GWlcnXhd4UhcW5iU2TBWFMtKEWUSzygZY5lKEGNVDDwbI9{eGixconsZZRqd25? M3foclI1PDl3N{Ww
AN3CA NVLWPFVJTnWwY4Tpc44hSXO|YYm= M4n2cVAvODVxMD6xM|AvPSEQvF2= MkfLO|IhcA>? MljsZ4F2e2W|IHGg[IVkemWjc3WgbY4hW1SDVEOsJGVTUyxiYX7kJGFMXCCyaH;zdIhwenmuYYTpc44> NYSzTWY3OjR2OUW3OVA>
MFE-296  M2Lz[mZ2dmO2aX;uJGF{e2G7 NELMOFIxNjB3L{CuNU8xNjVizszN NW\hdopkPzJiaB?= MofIZ4F2e2W|IHGg[IVkemWjc3WgbY4hW1SDVEOsJGVTUyxiYX7kJGFMXCCyaH;zdIhwenmuYYTpc44> MY[yOFQ6PTd3MB?=
UMC3 MWnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXjyeGdqOS1zMDFOwG0> M33Bb|czKGh? M3yzbYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M4n1XlI1OzJ3NE[x
5637 NYPkbJZ2S2WubDDWbYFjcWyrdImgRZN{[Xl? NYfQVXFTOS1zMDFOwG0> MVO3NkBp MV;pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MonGNlQ{OjV2NkG=
HU456 NI\DOWdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NE\WbIkyNTFyIN88US=> MlHRO|IhcA>? MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MYGyOFMzPTR4MR?=
MGHU4 M4rzbWNmdGxiVnnhZoltcXS7IFHzd4F6 NGTyNWQyNTFyIN88US=> NWDEOId6PzJiaB?= M4jzeIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MVSyOFMzPTR4MR?=
HT1376 NETYW2RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4TDSlEuOTBizszN NXTvTpJCPzJiaB?= MkLQbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M1X6cFI1OzJ3NE[x
RT112 MVHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHzaUXkyNTFyIN88US=> NXLLWW9jPzJiaB?= NFrVSolqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MUGyOFMzPTR4MR?=
T24 NIPkZo1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2HpRVEuOTBizszN M1jE[|czKGh? Mli4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> Ml\XNlQ{OjV2NkG=
BFTC905 MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkPWNU0yOCEQvF2= NW\s[5diPzJiaB?= NWPp[|FNcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MmPINlQ{OjV2NkG=
TCC-SUP M4Hi[GNmdGxiVnnhZoltcXS7IFHzd4F6 MXOxMVExKM7:TR?= M4PIfFczKGh? NWOwTW1zcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MlntNlQ{OjV2NkG=
RT4 MVnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXLzc2NEOS1zMDFOwG0> NGnGb|M4OiCq MV\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M{\uVlI1OzJ3NE[x
HONE1 NEDOeY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmC1NE4yNTFyIN88US=> NHLzTIo1QMLiaB?= NHno[lZqdmS3Y3XzJGczN01iZHXsZZkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MmTENlQzOzhyOUS=
HNE1 NWW0WXRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\QZlAvOS1zMDFOwG0> NInXUok1QMLiaB?= MlXKbY5lfWOnczDHNk9OKGSnbHH5JIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy NVPJeGlQOjR{M{iwPVQ>
CNE2  M4\sPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{CwcFAvOS1zMDFOwG0> MVS0POKhcA>? NYe2V3Z4cW6mdXPld{BIOi:PIHTlcIF6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz M{HlUVI1OjN6MEm0
C666-1 NGXJfI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHpNWIxNjFvMUCg{txO MlLGOFjDqGh? NVfFdpNrcW6mdXPld{BIOi:PIHTlcIF6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MXGyOFI{QDB7NB?=
HeLa MnHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MViwMlEuOTBizszN MUiyOEBp MYDpcoR2[2W|IFeyM20h[XK{ZYP0JIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy NYTMboxHOjR{M{iwPVQ>
Hep3B NGXuNY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\lZpFqOC5zLUGwJO69VQ>? NITwfZIzPCCq MVjpcoR2[2W|IFeyxsBienKnc4VCpC=> MmnuNlQzOzhyOUS=
HepG2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWW0PEBp MXjJR|UxRTJwN{K3JOKyKDBwNEK5JO69VQ>? NHjKSVAzOzV2NkW5NS=>
Hep3B M2Dqc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnH3OFghcA>? NHfUdFlKSzVyPUSuNlI{KMLzIECuPFM6KM7:TR?= MlOwNlM2PDZ3OUG=
PLC/PRF5 NVG1RmtbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUS0PEBp M1vIXWlEPTB;MU[uNVIxKMLzIESuNFAyKM7:TR?= MXmyN|U1PjV7MR?=
Huh7 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXqR2FGPDhiaB?= MXPJR|UxRTF3LkCwO{DDuSB5LkOzOEDPxE1? MlHoNlM2PDZ3OUG=
HepG2 NISyXGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\nO|IhcA>? NV64d|FIUUN3ME2xMlIxOCEEsTCwMlIzPiEQvF2= MlfINlM2PDZ3OUG=
Hep3B NWnMWFhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknxO|IhcA>? M130NGlEPTB;MD64PVIhyrFiMD6wOFQh|ryP NH\ybYszOzV2NkW5NS=>
PLC/PRF5 NVW5fVl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEL0NnI4OiCq MkDlTWM2OD1|LkGxNEDDuSByLkOzO{DPxE1? MWSyN|U1PjV7MR?=
Huh7 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmD6O|IhcA>? Ml3ETWM2OD1|Lkm4NEDDuSByLkiwN{DPxE1? NFfSeWozOzV2NkW5NS=>
MFE280 NGjneIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rxc2lEPTB;MD60NkDDuSByLkC2JO69VQ>? NVPVbWFpOjN2NEO4NFU>
AN3CA M3nCTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHGzbXBKSzVyPUCuOVAhyrFiMD6xNEDPxE1? NY[1RlRIOjN2NEO4NFU>
HEC155 NXvNc4d7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTBwNk[gxtEhOC5yOTFOwG0> MljGNlM1PDN6MEW=
MFE296 NFnpSpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\a[WJtUUN3ME2wMlY3KMLzIECuNVkh|ryP M3vSZ|I{PDR|OEC1
SPAC1S MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvUTWM2OD1yLke3JOKyKDBwMEig{txO NGP4OGYzOzR2M{iwOS=>
RL952 M17wN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTBwOUOgxtEhOC5yMTFOwG0> Mm[3NlM1PDN6MEW=
EN1 M4npemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTFwMEKgxtEhOC5{NTFOwG0> NWT4V25zOjN2NEO4NFU>
SNGII NXiwOZRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHYR4tZUUN3ME2xMlI1KMLzIECuNlgh|ryP MUeyN|Q1OzhyNR?=
ISHIKAWA NUO3fWF4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTFwM{CgxtEhOC5zMTFOwG0> NFXsUFAzOzR2M{iwOS=>
HEC1A NV;3WHZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;sbpJKSzVyPUGuN|QhyrFiMD6zNEDPxE1? MXiyN|Q1OzhyNR?=
KLE MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLQTWM2OD1zLkO3JOKyKDBwMEKg{txO MWiyN|Q1OzhyNR?=
SNGM NIDjWFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;qXmlEPTB;MT60NkDDuSByLkGzJO69VQ>? MVWyN|Q1OzhyNR?=
USPC2 MmLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHsTWM2OD1zLk[yJOKyKDBwMEGg{txO MljMNlM1PDN6MEW=
EN MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWS0dIs2UUN3ME2xMlY3KMLzIECuNFEh|ryP NEP0cYQzOzR2M{iwOS=>
MFE319 M1LTOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\RTWM2OD1zLki3JOKyKDBwNEWg{txO NFvwd2YzOzR2M{iwOS=>
EFE184 NIPaT3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVf2ZZZbUUN3ME2yMlA1KMLzIECuNVMh|ryP MnX2NlM1PDN6MEW=
ECC1 NInpSWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHLTWM2OD1{LkC3JOKyKDBwMEGg{txO NGrzOpkzOzR2M{iwOS=>
HEC1B MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTJwNUegxtEhOC5{MzFOwG0> MlHRNlM1PDN6MEW=
USPC1 M2j1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PQcmlEPTB;Mj62NEDDuSByLkGzJO69VQ>? NVPOTIVlOjN2NEO4NFU>
SPAC1L MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF[zR3dKSzVyPUOuNFYhyrFiMT6xOEDPxE1? MWeyN|Q1OzhyNR?=
HUVEC M4DvXWNmdGxiVnnhZoltcXS7IFHzd4F6 M3eyNFAuOjVizszN MVu3NkBp NHzVb3JFVVOR NXPwXXZTcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NGi3NpgzOzJ{OECxOy=>
HMVEC NGnBbGRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mk\qNE0zPSEQvF2= M4\xZ|czKGh? NGLVOodFVVOR M3;zUolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NYPwTmtnOjN{MkiwNVc>
MHCC-97H MV3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWewMVI2KM7:TR?= M4DR[VczKGh? M2TLO2ROW09? Mn\hbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NHjYcpozOzJ{OECxOy=>
SMMC7721 MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXKwMVI2KM7:TR?= M3q5[VczKGh? NEn3[5VFVVOR M1LySIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MnWxNlMzOjhyMUe=
Huh-7 NYe2XJFWSXCxcITvd4l{KEG|c3H5 Mn;GNE0yOi53IN88US=> NXv2V45kOjRiaB?= NHX4[2dFVVORwrC= MmPZd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NFGydlMzOjJ|MES3PS=>
Sk-Hep1 M1fRUWFxd3C2b4Ppd{BCe3OjeR?= NGnkTHgxNTF{LkWg{txO MWeyOEBp NXvnfYM2TE2VT9Mg M3HxfpNmdnOrdHn6[ZMhUEOFIHPlcIx{KHSxIGTSRWlNNSCjbnSgeIlo[XS3eoXtZYIucW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MWqyNlI{ODR5OR?=
Hep3B M{nZcGFxd3C2b4Ppd{BCe3OjeR?= M1\QOlAuOTJwNTFOwG0> M2DXXFI1KGh? M2fEVmROW00EoB?= MlXSd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYKyNlI{ODR5OR?=
PLC5 Mn;aRZBweHSxc3nzJGF{e2G7 NWfVSJQyOC1zMj61JO69VQ>? M4DnU|I1KGh? M2DU[WROW00EoB?= NHqw[ZV{\W6|aYTpfoV{KEiFQzDj[YxteyC2bzDUVmFKVC1iYX7kJJRq\2G2dYr1cYFjNWmwZIXj[YQh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M13hXVIzOjNyNEe5
PLC5 NFvPb5JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYX6eZZZOC1zNTFOwG0> M2TWWVczKGh? MX\y[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? NY\3d4R4OjJzOECzNFg>
Hep3B M3TTc2NmdGxiVnnhZoltcXS7IFHzd4F6 MVGwMVE2KM7:TR?= NI[0ZYY4OiCq MWjy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? M4mxVVIzOThyM{C4
Sk-Hep1 NUX0e2RVS2WubDDWbYFjcWyrdImgRZN{[Xl? NHfR[VQxNTF3IN88US=> NVn2THFnPzJiaB?= NYTLVG1QemWmdXPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg MX:yNlE5ODNyOB?=
Huh-7 M{\EbWNmdGxiVnnhZoltcXS7IFHzd4F6 M2DyUlAuOTVizszN MV63NkBp MYXy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? NHPVcmIzOjF6MEOwPC=>
PLC5 M4rnRmFxd3C2b4Ppd{BCe3OjeR?= MkHRNE0yPSEQvF2= NVS0OYdDOjRiaB?= MUDpcoNz\WG|ZYOgZZBweHSxdHnjJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZLDqA>? NH3P[XozOjF6MEOwPC=>
Hep3B MlrlRZBweHSxc3nzJGF{e2G7 MYCwMVE2KM7:TR?= M1\XclI1KGh? Mk[wbY5kemWjc3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? MXOyNlE5ODNyOB?=
Sk-Hep1 MYTBdI9xfG:|aYOgRZN{[Xl? MoSxNE0yPSEQvF2= MnL0NlQhcA>? Ml\ubY5kemWjc3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? MX6yNlE5ODNyOB?=
Huh-7 Mlm4RZBweHSxc3nzJGF{e2G7 NXfu[oVuOC1zNTFOwG0> M3TMT|I1KGh? M1zUVIlv[3KnYYPld{BieG:ydH;0bYMh[2WubDDk[YF1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi M4K1RVIzOThyM{C4
PLC5 NFjhb3ZHfW6ldHnvckBCe3OjeR?= NV;Zc|luOC1zMDFOwG0> MnjzNlQhcA>? M2fUWoNifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? NHKwdJMzOjF6MEOwPC=>
Hep3B NF\hdoRHfW6ldHnvckBCe3OjeR?= MoTkNE0yOCEQvF2= M4jmcFI1KGh? NXPSdGpW[2G3c3XzJIRwe2VvZHXw[Y5l\W62IFTORUBnemGpbXXueIF1cW:w NIXXVmMzOjF6MEOwPC=>
Sk-Hep1 MVzGeY5kfGmxbjDBd5NigQ>? NY\FWI1YOC1zMDFOwG0> Moj5NlQhcA>? MknYZ4F2e2W|IHTvd4Uu\GWyZX7k[Y51KESQQTDmdoFodWWwdHH0bY9v MUCyNlE5ODNyOB?=
Huh-7 NI\sN5pHfW6ldHnvckBCe3OjeR?= M4jETVAuOTBizszN M1XleVI1KGh? Mnm3Z4F2e2W|IHTvd4Uu\GWyZX7k[Y51KESQQTDmdoFodWWwdHH0bY9v NFnydoEzOjF6MEOwPC=>
SW780 MkLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TFVVUh\A>? NU\kSIVFUUN3ME21NEBvVQ>? NFzjWVUzOTFzOU[2NS=>
RT112 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnn2OUBl MWLJR|UxRTF3IH7N M173TFIyOTF7Nk[x
RT4 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU[1JIQ> NYjNeVg1UUN3ME21JI5O M4jqUFIyOTF7Nk[x
JMSU1 NGLzV|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;UOUBl MofpTWM2OD13MDDuUS=> NHLpSVEzOTFzOU[2NS=>
J82 MmewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnn[lQ2KGR? M3;ZO2lEPTB;MUSwNEBvVQ>? NFzlW|czOTFzOU[2NS=>
97-7 Mn7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWq1JIQ> M1LacmlEPTB;MUCwNEBvVQ>? M1i5dVIyOTF7Nk[x
RT112 MV;GeY5kfGmxbjDBd5NigQ>? NGfvXXE2ODBibl2= NHLrXXEzPCCq MXPpcoNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gS|HDqGGlY3;tdIFvcWWmIHL5JIEh\GWlcnXhd4UhcW5iUzDhcoQhTzJxTTDwbIF{\XN? MUGyNVEyQTZ4MR?=
RT4 NVywXoRPTnWwY4Tpc44hSXO|YYm= M{TwdFUxOCCwTR?= M3jqbVI1KGh? NVTEXHJxcW6lcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKEdzwrDhZ4NwdXCjbnnl[EBjgSCjIHTlZ5Jm[XOnIHnuJHMh[W6mIFeyM20heGijc3Xz M{SzcVIyOTF7Nk[x
MGH-U3 M{fIdWZ2dmO2aX;uJGF{e2G7 NXH2PWREPTByIH7N NGTreHczPCCq NFHk[XhqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= MlXYNlEyOTl4NkG=
SW780 MofISpVv[3Srb36gRZN{[Xl? M4XvcFUxOCCwTR?= NYKwXYdtOjRiaB?= NH3YTYpqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= MWSyNVEyQTZ4MR?=
97-7 NICwdJdHfW6ldHnvckBCe3OjeR?= MXG1NFAhdk1? MYSyOEBp NWnxPFlVcW6lcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKEdzwrDhZ4NwdXCjbnnl[EBjgSCjIHTlZ5Jm[XOnIHnuJHMh[W6mIFeyM20heGijc3Xz NXjUXoJsOjFzMUm2OlE>
 J807C NVTQRYN1S2WubDDWbYFjcWyrdImgRZN{[Xl? MoHENE01ODBibl2= MXu0PEBp NETjXWhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? Mn65NVU2QTh6MUS=
Y373C NYfwUldlS2WubDDWbYFjcWyrdImgRZN{[Xl? MXqwMVQxOCCwTR?= MmPIOFghcA>? NV\VUHZIcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MUCxOVU6QDhzNB?=
K650E NInNWFlE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGrFOogxNTRyMDDuUS=> NGmzVlU1QCCq MmXWbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NEnYXnAyPTV7OEixOC=>
G384D NE\1c41E\WyuIG\pZYJqdGm2eTDBd5NigQ>? MoLuNE01ODBibl2= MojOOFghcA>? MXzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M3zkcVE2PTl6OEG0
F384L NVj5U3FqS2WubDDWbYFjcWyrdImgRZN{[Xl? NFr2VJIxNTRyMDDuUS=> MWC0PEBp NGG0NFdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NEftZYcyPTV7OEixOC=>
KMS11 NGP6fXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LtNlczKGh? MYjJR|UxRTlyIH7N MXuxOVU6QDhzNB?=
KMS18 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3YO|IhcA>? M3LNVmlEPTB;NUWwJI5O MV6xOVU6QDhzNB?=
OPM2 M1nxN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWq3NkBp M3v6fmlEPTB;OUCgcm0> NX[1flZoOTV3OUi4NVQ>
H929 NGHTU4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjNWmM4OiCq MkTxTWM2OD5iMkWwNEBvVQ>? MY[xOVU6QDhzNB?=
8226 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPHO|IhcA>? MWTJR|UxRiB{NUCwJI5O NH63dZcyPTV7OEixOC=>
U266 NVrCTnVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NISyO4g4OiCq M{fOcmlEPTB-IEK1NFAhdk1? NGT6WGQyPTV7OEixOC=>

... 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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