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 NI\2WYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTBwNES5JO69VQ>? MXyyOVIxOjB5Mx?=
SupB15-R Moi0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PpXGlEPTB;MD61OVgh|ryP MljCNlUzODJyN{O=
BaF3-pSRα M1zF[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;kPGlEPTB;MD62Olgh|ryP MV[yOVIxOjB5Mx?=
BaF3-p210Bcr-Abl Mlq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7iXFFKSzVyPUCuOlkzKM7:TR?= NX;pTWtxOjV{MEKwO|M>
BaF3-p210Bcr-Abl-T315I MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nMWGlEPTB;Mj62NlYh|ryP NUXKNZRWOjV{MEKwO|M>
CCRF-CEM MnS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzjdnpMUUN3ME2wMlM6QCEQvF2= NH\WdW4zPTJyMkC3Ni=>
CEM/C2 NGTySlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnxXZFKSzVyPUGuNVI2KM7:TR?= Mnm4NlUzODJyN{K=
Nalm-6 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTBwM{iyJO69VQ>? NIC4bY0zPTJyMkC3Ni=>
SEM-K2 NGSyN4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnRT|JKSzVyPUCuNFIzKM7:TR?= M1rhO|I2OjB{MEey
HB-1119 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{G3[2lEPTB;MD6wNlgh|ryP NY\UTJdkOjV{MEKwO|I>
RS4:11 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTJwOEGg{txO NHT0eoozPTJyMkC3Ni=>
Nalm-6 Moq1RZBweHSxc3nzJGF{e2G7 M4L3NlIh|ryP NXm5WIdiOjRxNEigbC=> Mn:wbY5lfWOnczDhdI9xfG:|aYOgdoV{fWy2aX7nJIlvKGGkb4X0JFczLSCxZjDj[YxtKGSnYYToJIFnfGW{IEK0JIghfHKnYYTt[Y51KGGwZDC4NUUh[W[2ZYKgOFghcA>? NF7NeVIzPTJyMkC3Ni=>
SEM-K2 M1zhU2Fxd3C2b4Ppd{BCe3OjeR?= NHrQcZoxNjFxMTFOwG0> MWKyOEBp M1TkUYlv\HWlZYOg[YFzdHliYYDvdJRwe2m|IH;mJHNGVS2NMjDj[YxteyCjdDCwMlEh|ryPIHHmeIVzKDJ2IHi= MU[yOVIxOjB5Mh?=
HCT-116 NX;FcI1PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTNwMEWwMlU5KM7:TR?= NH;T[ZMzPDR7NUe1NC=>
HT-29 M1u0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTVwMkGuPVMh|ryP M1fWZ|I1PDl3N{Ww
SW-480 M{\xTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjoS3RKSzVyPUSuN|MxNjR5IN88US=> MlHjNlQ1QTV5NUC=
CaCO2 NV7wXGVNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHZcYJKSzVyPUOuNlMxNjZ2IN88US=> NGnGTmMzPDR7NUe1NC=>
LS174T MmS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTRwM{OwMlQ4KM7:TR?= NFK0NJYzPDR7NUe1NC=>
HEC-1A MW\GeY5kfGmxbjDBd5NigQ>? NGDyWm4xNjB3L{CuNU8xNjVizszN NXvJU3NuPzJiaB?= M37PdYNifXOnczDhJIRm[3KnYYPlJIlvKFOWQWSzMEBGWktuIHHu[EBCU1RicHjvd5Bpd3K7bHH0bY9v M2\zWVI1PDl3N{Ww
AN3CA MoOwSpVv[3Srb36gRZN{[Xl? MnLBNE4xPS9yLkGvNE42KM7:TR?= MXi3NkBp MVTjZZV{\XNiYTDk[YNz\WG|ZTDpckBUXEGWMzygSXJMNCCjbnSgRWtVKHCqb4PwbI9zgWyjdHnvci=> MWqyOFQ6PTd3MB?=
MFE-296  MkL5SpVv[3Srb36gRZN{[Xl? MUCwMlA2NzBwMT:wMlUh|ryP M2fRdFczKGh? NXe3bGw{[2G3c3XzJIEh\GWlcnXhd4UhcW5iU2TBWFMtKEWUSzygZY5lKEGNVDDwbI9{eGixconsZZRqd25? MYiyOFQ6PTd3MB?=
UMC3 NH7TdmFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYqxMVExKM7:TR?= NY\zWmtsPzJiaB?= MYPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M4HLUlI1OzJ3NE[x
5637 M1\hXWNmdGxiVnnhZoltcXS7IFHzd4F6 NYDJXIJ2OS1zMDFOwG0> Mn;5O|IhcA>? MXXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NGPKZlkzPDN{NUS2NS=>
HU456 MXLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYSxMVExKM7:TR?= MVe3NkBp MWrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NYHsVlk6OjR|MkW0OlE>
MGHU4 M2HGXmNmdGxiVnnhZoltcXS7IFHzd4F6 NUXvVow{OS1zMDFOwG0> M4Dib|czKGh? MVLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NGLHNpkzPDN{NUS2NS=>
HT1376 M{\W[WNmdGxiVnnhZoltcXS7IFHzd4F6 NYjZZWdrOS1zMDFOwG0> NYrQVXh4PzJiaB?= M1LwbYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NIHZZnczPDN{NUS2NS=>
RT112 MYfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYqxMVExKM7:TR?= MYK3NkBp Ml23bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M1fSRVI1OzJ3NE[x
T24 M2nhNWNmdGxiVnnhZoltcXS7IFHzd4F6 NVPGSIpVOS1zMDFOwG0> M3:3OFczKGh? NYixd|JMcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M2TiSFI1OzJ3NE[x
BFTC905 NXHqS2hFS2WubDDWbYFjcWyrdImgRZN{[Xl? NEnUfnUyNTFyIN88US=> M1fYSVczKGh? MVPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M4TxUVI1OzJ3NE[x
TCC-SUP NIDzc4ZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1qxfVEuOTBizszN NEXhcFI4OiCq MmX4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NYDRVI8yOjR|MkW0OlE>
RT4 MlPYR4VtdCCYaXHibYxqfHliQYPzZZk> NILX[mcyNTFyIN88US=> NUPUXI5WPzJiaB?= NYizbFJMcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NH7TNXUzPDN{NUS2NS=>
HONE1 MmfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\LNE4yNTFyIN88US=> NYrJbZhOPDkEoHi= NY\KR|RpcW6mdXPld{BIOi:PIHTlcIF6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz NWnoZZZROjR{M{iwPVQ>
HNE1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlH6NE4yNTFyIN88US=> NWnBZlI1PDkEoHi= M3TYcYlv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NE\0V|czPDJ|OEC5OC=>
CNE2  NHfSfmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrrb2kxNjFvMUCg{txO NWfaPXhEPDkEoHi= MXXpcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= MUeyOFI{QDB7NB?=
C666-1 M13GSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWCwMlEuOTBizszN MYm0POKhcA>? NV;o[oNicW6mdXPld{BIOi:PIHTlcIF6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz M33G[|I1OjN6MEm0
HeLa NID4TWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDPWFYxNjFvMUCg{txO M4X4e|I1KGh? M{OwO4lv\HWlZYOgS|IwVSCjcoLld5QhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MmewNlQzOzhyOUS=
Hep3B M1r6NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\xb5ZWOC5zLUGwJO69VQ>? NX7qcoNDOjRiaB?= NYDPfYpkcW6mdXPld{BIOsLiYYLy[ZN1yqB? NGT2XlMzPDJ|OEC5OC=>
HepG2 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWG0PEBp NIHJUlNKSzVyPUKuO|I4KMLzIECuOFI6KM7:TR?= NVLXcHIyOjN3NE[1PVE>
Hep3B M13FNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2ixV|Q5KGh? MYfJR|UxRTRwMkKzJOKyKDBwOEO5JO69VQ>? NIrRZnkzOzV2NkW5NS=>
PLC/PRF5 M4Lv[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{WydFQ5KGh? M4XQ[mlEPTB;MU[uNVIxKMLzIESuNFAyKM7:TR?= NXPpXGpJOjN3NE[1PVE>
Huh7 MmPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXmyfnREPDhiaB?= NE\KZWVKSzVyPUG1MlAxPyEEsTC3MlM{PCEQvF2= MnLKNlM2PDZ3OUG=
HepG2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLPc5c4OiCq MWTJR|UxRTFwMkCwJOKyKDBwMkK2JO69VQ>? NWTpO5U{OjN3NE[1PVE>
Hep3B MknSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3qWW04OiCq NGXTRYdKSzVyPUCuPFkzKMLzIECuNFQ1KM7:TR?= MVmyN|U1PjV7MR?=
PLC/PRF5 MmfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HxRlczKGh? Mn\yTWM2OD1|LkGxNEDDuSByLkOzO{DPxE1? M33oe|I{PTR4NUmx
Huh7 NXnsc3RrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYm5bW1EPzJiaB?= M4exSWlEPTB;Mz65PFAhyrFiMD64NFMh|ryP MVSyN|U1PjV7MR?=
MFE280 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwNEKgxtEhOC5yNjFOwG0> MkXZNlM1PDN6MEW=
AN3CA NGXTcolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\TcGlEPTB;MD61NEDDuSByLkGwJO69VQ>? M1;hS|I{PDR|OEC1
HEC155 NYHDVoFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVz0emUzUUN3ME2wMlY3KMLzIECuNFkh|ryP NF;DNlMzOzR2M{iwOS=>
MFE296 NHvrVoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUj0N5Q4UUN3ME2wMlY3KMLzIECuNVkh|ryP NIXO[GczOzR2M{iwOS=>
SPAC1S MlvhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PkVGlEPTB;MD63O{DDuSByLkC4JO69VQ>? MUWyN|Q1OzhyNR?=
RL952 NYfRVYY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTBwOUOgxtEhOC5yMTFOwG0> MUeyN|Q1OzhyNR?=
EN1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjMO4kxUUN3ME2xMlAzKMLzIECuNlUh|ryP NGS1[GMzOzR2M{iwOS=>
SNGII NXy4fI84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHDOGJKSzVyPUGuNlQhyrFiMD6yPEDPxE1? NHX1eZczOzR2M{iwOS=>
ISHIKAWA MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXza[WtiUUN3ME2xMlMxKMLzIECuNVEh|ryP M1;SfFI{PDR|OEC1
HEC1A MnLqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTGXFdtUUN3ME2xMlM1KMLzIECuN|Ah|ryP MmLUNlM1PDN6MEW=
KLE MoDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHYfXNKSzVyPUGuN|chyrFiMD6wNkDPxE1? NXLie|M4OjN2NEO4NFU>
SNGM MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTFwNEKgxtEhOC5zMzFOwG0> NELSUnczOzR2M{iwOS=>
USPC2 M3nHVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fVcmlEPTB;MT62NkDDuSByLkCxJO69VQ>? MV[yN|Q1OzhyNR?=
EN M2O2dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jlbGlEPTB;MT62OkDDuSByLkCxJO69VQ>? NHfPR3kzOzR2M{iwOS=>
MFE319 Mlf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnCTWM2OD1zLki3JOKyKDBwNEWg{txO NIHDZVIzOzR2M{iwOS=>
EFE184 M2jj[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTJwMESgxtEhOC5zMzFOwG0> M4XLelI{PDR|OEC1
ECC1 NWPqU4ZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDTTWM2OD1{LkC3JOKyKDBwMEGg{txO NH6wR|QzOzR2M{iwOS=>
HEC1B MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLRTWM2OD1{LkW3JOKyKDBwMkOg{txO M3vo[|I{PDR|OEC1
USPC1 NVL6eFMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3OXm5KSzVyPUKuOlAhyrFiMD6xN{DPxE1? MlHXNlM1PDN6MEW=
SPAC1L MmTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTNwME[gxtEhOS5zNDFOwG0> MYqyN|Q1OzhyNR?=
HUVEC NFn3eHVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1TI[VAuOjVizszN M3XIN|czKGh? M2XSPGROW09? M1r0SYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz Ml:4NlMzOjhyMUe=
HMVEC M{\0eWNmdGxiVnnhZoltcXS7IFHzd4F6 M3vabVAuOjVizszN MlfBO|IhcA>? M3;JdGROW09? NH\4NHdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MnLMNlMzOjhyMUe=
MHCC-97H MVzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXLLbmw{OC1{NTFOwG0> NX3PbnBNPzJiaB?= NYnMd|gxTE2VTx?= MmHJbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NYrhbYc{OjN{MkiwNVc>
SMMC7721 MWXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYDOO4xHOC1{NTFOwG0> MojkO|IhcA>? MnvGSG1UVw>? NUPLO2dXcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M1HPRlI{OjJ6MEG3
Huh-7 MnrTRZBweHSxc3nzJGF{e2G7 NXfmNHN2OC1zMj61JO69VQ>? MmnBNlQhcA>? NFruSYJFVVORwrC= M2P4XJNmdnOrdHn6[ZMhUEOFIHPlcIx{KHSxIGTSRWlNNSCjbnSgeIlo[XS3eoXtZYIucW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NYrBUXBKOjJ{M{C0O|k>
Sk-Hep1 M3:xVGFxd3C2b4Ppd{BCe3OjeR?= MYqwMVEzNjVizszN NF;4PXEzPCCq NIrvXGZFVVORwrC= MWfz[Y5{cXSrenXzJGhESyClZXzsd{B1dyCWUlHJUE0h[W6mIITp[4F1fXq3bXHiMYlv\HWlZXSgZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M1jY[lIzOjNyNEe5
Hep3B MXjBdI9xfG:|aYOgRZN{[Xl? NYHRWW1iOC1zMj61JO69VQ>? MorxNlQhcA>? M374W2ROW00EoB?= MkWwd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYqyNlI{ODR5OR?=
PLC5 M2rFb2Fxd3C2b4Ppd{BCe3OjeR?= NGTLSJkxNTF{LkWg{txO NUTibFViOjRiaB?= NIX1UZBFVVORwrC= NV7VS4s6e2Wwc3n0bZpmeyCKQ1OgZ4VtdHNidH:gWHJCUUxvIHHu[EB1cWejdIX6eY1i[i2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MonHNlIzOzB2N{m=
PLC5 MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2joNFAuOTVizszN M4qwNlczKGh? NWqxPYd2emWmdXPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg NU\scVkyOjJzOECzNFg>
Hep3B M3Pi[GNmdGxiVnnhZoltcXS7IFHzd4F6 NH;UcHYxNTF3IN88US=> MUi3NkBp M{TBS5Jm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= Mly0NlIyQDB|MEi=
Sk-Hep1 NYPv[FB[S2WubDDWbYFjcWyrdImgRZN{[Xl? MWSwMVE2KM7:TR?= M3ztWlczKGh? NVTSfVFFemWmdXPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nctMg NYLKTFdIOjJzOECzNFg>
Huh-7 MkfRR4VtdCCYaXHibYxqfHliQYPzZZk> MYWwMVE2KM7:TR?= NULCdYplPzJiaB?= MoXFdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi MlzUNlIyQDB|MEi=
PLC5 NYrPOYpRSXCxcITvd4l{KEG|c3H5 MkjoNE0yPSEQvF2= Ml:yNlQhcA>? NWjKOXFncW6lcnXhd4V{KGGyb4D0c5Rq[yClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M3z6O|IzOThyM{C4
Hep3B Ml\JRZBweHSxc3nzJGF{e2G7 M3nielAuOTVizszN NF7hUXUzPCCq M1fVSYlv[3KnYYPld{BieG:ydH;0bYMh[2WubDDk[YF1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi NXv5THJOOjJzOECzNFg>
Sk-Hep1 MkPnRZBweHSxc3nzJGF{e2G7 M2ryUlAuOTVizszN MmW2NlQhcA>? MoTzbY5kemWjc3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? MVuyNlE5ODNyOB?=
Huh-7 MUjBdI9xfG:|aYOgRZN{[Xl? NUnTVY96OC1zNTFOwG0> NGXrUpUzPCCq NI\qbXJqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= Ml;oNlIyQDB|MEi=
PLC5 NITtR2xHfW6ldHnvckBCe3OjeR?= MoDYNE0yOCEQvF2= M3;PdFI1KGh? Mmf6Z4F2e2W|IHTvd4Uu\GWyZX7k[Y51KESQQTDmdoFodWWwdHH0bY9v M{PH[|IzOThyM{C4
Hep3B Mn6zSpVv[3Srb36gRZN{[Xl? NIXOdGkxNTFyIN88US=> NU[zc5pROjRiaB?= NIfy[o5k[XW|ZYOg[I9{\S2mZYDlcoRmdnRiRF7BJIZz[WevZX70ZZRqd25? MXeyNlE5ODNyOB?=
Sk-Hep1 M4nuR2Z2dmO2aX;uJGF{e2G7 NFv2dWwxNTFyIN88US=> MlHlNlQhcA>? NFmxRZJk[XW|ZYOg[I9{\S2mZYDlcoRmdnRiRF7BJIZz[WevZX70ZZRqd25? NWC2TnJGOjJzOECzNFg>
Huh-7 NYXjfo5VTnWwY4Tpc44hSXO|YYm= MWewMVExKM7:TR?= NFTwc5gzPCCq Mle1Z4F2e2W|IHTvd4Uu\GWyZX7k[Y51KESQQTDmdoFodWWwdHH0bY9v MmTYNlIyQDB|MEi=
SW780 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPXOUBl NVzLR5RGUUN3ME21NEBvVQ>? MljHNlEyOTl4NkG=
RT112 NVLUPZlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTGc4tvPSCm NIXtW4dKSzVyPUG1JI5O M1zFO|IyOTF7Nk[x
RT4 NFq5bXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TnNlUh\A>? MYnJR|UxRTVibl2= MmnINlEyOTl4NkG=
JMSU1 NWL3WpF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWq1JIQ> NHvoc3dKSzVyPUWwJI5O Mn\YNlEyOTl4NkG=
J82 NHf5e5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1KzbVUh\A>? MUXJR|UxRTF2MECgcm0> NEnuUmMzOTFzOU[2NS=>
97-7 NEHsbXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmj6OUBl MX\JR|UxRTFyMECgcm0> NGq2OG8zOTFzOU[2NS=>
RT112 MkPsSpVv[3Srb36gRZN{[Xl? NGPlVVg2ODBibl2= NEjWUYIzPCCq MkS1bY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| MXyyNVEyQTZ4MR?=
RT4 MVfGeY5kfGmxbjDBd5NigQ>? MX61NFAhdk1? NWLDdY5wOjRiaB?= M33hXolv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= NF\TZnUzOTFzOU[2NS=>
MGH-U3 NX20[G1HTnWwY4Tpc44hSXO|YYm= NIDVRok2ODBibl2= M1O5S|I1KGh? NGnqcZBqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= M12wUFIyOTF7Nk[x
SW780 NH3Ie3dHfW6ldHnvckBCe3OjeR?= NIDjPXY2ODBibl2= NETXbW8zPCCq MVnpcoNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gS|HDqGGlY3;tdIFvcWWmIHL5JIEh\GWlcnXhd4UhcW5iUzDhcoQhTzJxTTDwbIF{\XN? Mk\xNlEyOTl4NkG=
97-7 NHrRdndHfW6ldHnvckBCe3OjeR?= MX61NFAhdk1? M{nLNlI1KGh? MkH5bY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| NV3DVXlnOjFzMUm2OlE>
 J807C NGnwZ5JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXnMU2FTOC12MECgcm0> Mkm4OFghcA>? MnXwbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MV:xOVU6QDhzNB?=
Y373C NY\5NnVsS2WubDDWbYFjcWyrdImgRZN{[Xl? NWXDb21lOC12MECgcm0> M2rxNVQ5KGh? NI[4OY1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MnnhNVU2QTh6MUS=
K650E NGLrbnFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NWfZclRUOC12MECgcm0> NHiyXIo1QCCq M{TWXolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NFLBUZgyPTV7OEixOC=>
G384D MnfHR4VtdCCYaXHibYxqfHliQYPzZZk> MlLTNE01ODBibl2= MmrBOFghcA>? NH\rZmRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NFPSXFUyPTV7OEixOC=>
F384L NWmyc5dOS2WubDDWbYFjcWyrdImgRZN{[Xl? NV72fnB5OC12MECgcm0> MUG0PEBp MV\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MnzjNVU2QTh6MUS=
KMS11 M2\he2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXW3NkBp NXS2V|RtUUN3ME25NEBvVQ>? NXvFb4RCOTV3OUi4NVQ>
KMS18 NWOzeYpWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrufoZ[PzJiaB?= NEW5PWZKSzVyPUW1NEBvVQ>? NVfRVo5lOTV3OUi4NVQ>
OPM2 M{DFWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnT4O|IhcA>? MXnJR|UxRTlyIH7N M3PtPFE2PTl6OEG0
H929 MmnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPtZoE4OiCq MmHJTWM2OD5iMkWwNEBvVQ>? MnPUNVU2QTh6MUS=
8226 M{TuTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXu3NkBp MVXJR|UxRiB{NUCwJI5O NX\XO3NjOTV3OUi4NVQ>
U266 NVXw[241T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV63NkBp NYnXd|JnUUN3ME6gNlUxOCCwTR?= NFLvbXYyPTV7OEixOC=>

... 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

カスタマーフィードバック (7)


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Rating
Source haematologica, 2011, 96, 922-926. Dovitinib (TKI-258, CHIR-258) purchased from Selleck
Method Western blot, Apoptotic assay
Cell Lines Ba/F3 cells
Concentrations 0-10000 nM
Incubation Time 48 h
Results CUX1-FGFR1-expressing Ba/F3 cells displayed IL-3 independent proliferation (Figure A). Treatment of the CUX1-FGFR1-expressing Ba/F3 cells with the kinase inhibitor TKI258 significantly inhibited cell growth with an IC 50 of 489 nM (Figure B). Western blot analysis demonstrated a corresponding decrease in CUX1-FGFR1 phosphorylation with increasing doses of TKI258, while protein expression was unaffected (Figure C).Furthermore, using an Annexin-V/propidium iodide-based apoptosis assay, we could show that 48 h exposure to TKI258 induced apoptosis followed by cell death in CUX1-FGFR1-expressing Ba/F3 cells. Massive apoptosis/necrosis was recorded at 500 nM of TKI258 (Figure D).

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Rating
Source Brit J Cancer , 2010, 104, 75-82. Dovitinib (TKI-258, CHIR-258) purchased from Selleck
Method Western blotting, Immunoprecipitation
Cell Lines RT112 cells
Concentrations 500 nM
Incubation Time 1 h
Results RT112 cells show constitutive activation of FGFR3 and were used to assess the effects of PD173074, SU5402 and TKI-258 on FGFR3 phosphorylation and downstream signalling (Figure B and C). A time-course of treatment with PD173074 showed a rapid and sustained inactivation of FGFR3 (Figure B). After 2 h of treatment, TKI-258 and other inhibitors all showed profound inhibition of FGFR3 phosphorylation. Recently, we have shown that FGFR3 activates the MAPK pathway in normal urothelial cells.

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Rating
Source Brit J Cancer , 2010, 104, 75-82. Dovitinib (TKI-258, CHIR-258) purchased from Selleck
Method Cell cycle and apoptosis analysis
Cell Lines RT112/RT4/SW780/MGH-U3/97-7 cell lines
Concentrations 500 nM
Incubation Time 24 h
Results A significant increase in the proportion of cells in G1 accompanied by a decrease in S and G2 /M phases was observed in PD173074- and TKI-258-treated RT112, RT4, MGH-U3 and 97-7 cells after 24-h exposure.

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Source Oral Oncol, 2012, 48, 1242-9. Dovitinib (TKI-258, CHIR-258) purchased from Selleck
Method HNSCC xenografts
Cell Lines OSC-19 cells/SCC-1 cells/Athymic female nude mice
Concentrations 20mg/kg/day
Incubation Time 12-14 day
Results The antitumor efficacy of broad spectrum RTK inhibition was evaluated in HNSCC xenografts dosed with dovitinib (20 mg/kg/ day) orally for 12–14 days. Treatments were initiated when orthotopic tongue tumors average 10 mm2 (Fig. 2). Significant antitumor activity was seen in both OSC-19 and SCC-1 models. Growth stabilization was seen by day 2 in the SCC-1 xenografts (Fig. 2A) and by day 8 of treatment in the OSC-19 xenografts (Fig. 2B). In addition, growth reduction was seen in both SCC-1 (p < 0.0001; day 12) and OSC-19 (p < 0.0001; day 15) xenografts. During the final week of treatment, the tumors in the treatment cohort had areas of necrosis evident on gross examination which were not present in the tumors of untreated control mice.

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Rating
Source Oral Oncol, 2012, 48, 1242-9. Dovitinib (TKI-258, CHIR-258) purchased from Selleck
Method Immunohistochemical and immunofluorescence analysis
Cell Lines Athymic female nude mice
Concentrations 20 mg/kg/d
Incubation Time 12-14 d
Results 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).

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Rating
Source Oral Oncol, 2012, 48, 1242-9. Dovitinib (TKI-258, CHIR-258) purchased from Selleck
Method Cell proliferation assays
Cell Lines HNSCC /fibroblast cell lines
Concentrations 0–1000 nM
Incubation Time
Results Inhibition of RTKs by dovitinib reduced proliferation in all HNSCC and fibroblast cell lines in a dose-dependent fashion.

Click to enlarge
Rating
Source AACR, 2011, Dovitinib (TKI-258, CHIR-258) purchased from Selleck
Method Cell viability assay
Cell Lines Ba/F3 cells
Concentrations 0-1000 nM
Incubation Time
Results

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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