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

カスタマーフィードバック(7)

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 M1SwcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vS[mlEPTB;MD60OFkh|ryP M2jmTFI2OjB{MEez
SupB15-R MnqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTBwNUW4JO69VQ>? NYH3c2FjOjV{MEKwO|M>
BaF3-pSRα NWXSRW06T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfuTWM2OD1yLk[2PEDPxE1? M4nMOlI2OjB{MEez
BaF3-p210Bcr-Abl NV\aPW1LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\GN|BvUUN3ME2wMlY6OiEQvF2= Ml:2NlUzODJyN{O=
BaF3-p210Bcr-Abl-T315I Mm\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{npR2lEPTB;Mj62NlYh|ryP MX2yOVIxOjB5Mx?=
CCRF-CEM M2S0Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmeyTWM2OD1yLkO5PEDPxE1? M4nUSFI2OjB{MEey
CEM/C2 NXLHO2wyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXpc2pKSzVyPUGuNVI2KM7:TR?= MYOyOVIxOjB5Mh?=
Nalm-6 MmHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLsRmpKSzVyPUCuN|gzKM7:TR?= MnOxNlUzODJyN{K=
SEM-K2 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nKRWlEPTB;MD6wNlIh|ryP NYTqNmV4OjV{MEKwO|I>
HB-1119 M4rBZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfG[WpKSzVyPUCuNFI5KM7:TR?= Mmn0NlUzODJyN{K=
RS4:11 NIe1UGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYn1VIlOUUN3ME2yMlgyKM7:TR?= Ml3BNlUzODJyN{K=
Nalm-6 MVvBdI9xfG:|aYOgRZN{[Xl? NVPKZ5o2OiEQvF2= M33J[VI1NzR6IHi= MXfpcoR2[2W|IHHwc5B1d3OrczDy[ZN2dHSrbnegbY4h[WKxdYSgO|ImKG:oIHPlcIwh\GWjdHigZYZ1\XJiMkSgbEB1emWjdH3lcpQh[W6mIEixKUBi\nSncjC0PEBp NWHyW3JqOjV{MEKwO|I>
SEM-K2 NWixOnZJSXCxcITvd4l{KEG|c3H5 NUfxeJNVOC5zL{Gg{txO NGXQdlUzPCCq MV\pcoR2[2W|IHXhdox6KGGyb4D0c5NqeyCxZjDTSW0uUzJiY3XscJMh[XRiMD6xJO69VSCjZoTldkAzPCCq M4WxXlI2OjB{MEey
HCT-116 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLFTWM2OD1|LkC1NE42QCEQvF2= MoHpNlQ1QTV5NUC=
HT-29 NHy0cJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTVwMkGuPVMh|ryP MlvtNlQ1QTV5NUC=
SW-480 NWrSXVFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Ph[2lEPTB;ND6zN|AvPDdizszN NV;qfI1MOjR2OUW3OVA>
CaCO2 NVvTdpdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHziPJBKSzVyPUOuNlMxNjZ2IN88US=> NYjId5hWOjR2OUW3OVA>
LS174T M361N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTkXop7UUN3ME20MlM{OC52NzFOwG0> MXSyOFQ6PTd3MB?=
HEC-1A NWn0OmlbTnWwY4Tpc44hSXO|YYm= NGS3W3UxNjB3L{CuNU8xNjVizszN NFG0Wno4OiCq MlnqZ4F2e2W|IHGg[IVkemWjc3WgbY4hW1SDVEOsJGVTUyxiYX7kJGFMXCCyaH;zdIhwenmuYYTpc44> M{fQRlI1PDl3N{Ww
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MFE-296  MkXtSpVv[3Srb36gRZN{[Xl? NGWwUGkxNjB3L{CuNU8xNjVizszN NG[wRnU4OiCq M2LrNYNifXOnczDhJIRm[3KnYYPlJIlvKFOWQWSzMEBGWktuIHHu[EBCU1RicHjvd5Bpd3K7bHH0bY9v NYTsbnJFOjR2OUW3OVA>
UMC3 M{DRTmNmdGxiVnnhZoltcXS7IFHzd4F6 M1PUPFEuOTBizszN Mle4O|IhcA>? NWX6cW56cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M3u3VFI1OzJ3NE[x
5637 NETzcVdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1S2V|EuOTBizszN NUL2dJZIPzJiaB?= MmjGbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NWHDcIN1OjR|MkW0OlE>
HU456 MlTsR4VtdCCYaXHibYxqfHliQYPzZZk> M3j5bVEuOTBizszN MnLkO|IhcA>? Mn7LbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M1mzUVI1OzJ3NE[x
MGHU4 NY\DPZJNS2WubDDWbYFjcWyrdImgRZN{[Xl? M3\yVlEuOTBizszN NVvRfZZzPzJiaB?= NEDrd4VqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NXrq[VR7OjR|MkW0OlE>
HT1376 M3;LXWNmdGxiVnnhZoltcXS7IFHzd4F6 MnPWNU0yOCEQvF2= MoPLO|IhcA>? MXrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NIT4dWczPDN{NUS2NS=>
RT112 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWDGTXJtOS1zMDFOwG0> NVnsT2c3PzJiaB?= MWnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M4TCNFI1OzJ3NE[x
T24 MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYOxMVExKM7:TR?= NYTEcIR4PzJiaB?= NUD4VVN6cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MUWyOFMzPTR4MR?=
BFTC905 MmrZR4VtdCCYaXHibYxqfHliQYPzZZk> MnnBNU0yOCEQvF2= MnzCO|IhcA>? MVfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NXTqXlJUOjR|MkW0OlE>
TCC-SUP M3;4[WNmdGxiVnnhZoltcXS7IFHzd4F6 M{HKVFEuOTBizszN M{X0O|czKGh? Ml2zbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M1TNVlI1OzJ3NE[x
RT4 MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUjTVoJFOS1zMDFOwG0> MlO4O|IhcA>? NH;DXWNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NEmwbYIzPDN{NUS2NS=>
HONE1 MmP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX2wMlEuOTBizszN Mn7wOFjDqGh? M{DlfYlv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> M2P5WFI1OjN6MEm0
HNE1 MlHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkP6NE4yNTFyIN88US=> NWXyVG1xPDkEoHi= NX;XU|dPcW6mdXPld{BIOi:PIHTlcIF6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz Mk\pNlQzOzhyOUS=
CNE2  Mnf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jselAvOS1zMDFOwG0> MVi0POKhcA>? MYPpcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= MojPNlQzOzhyOUS=
C666-1 NYLnRWU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXofYplOC5zLUGwJO69VQ>? M1zDZ|Q5yqCq NYrRNpQzcW6mdXPld{BIOi:PIHTlcIF6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MmTLNlQzOzhyOUS=
HeLa NY\pR3AxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M32zd|AvOS1zMDFOwG0> NUK3cpZxOjRiaB?= NFPwelFqdmS3Y3XzJGczN01iYYLy[ZN1KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz M4\aW|I1OjN6MEm0
Hep3B MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTTNmcxNjFvMUCg{txO NX7zPXNuOjRiaB?= NEfGb3hqdmS3Y3XzJGczyqCjcoLld5TDqA>? MWSyOFI{QDB7NB?=
HepG2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILkNZo1QCCq NHHlZXFKSzVyPUKuO|I4KMLzIECuOFI6KM7:TR?= NX7uN|Q1OjN3NE[1PVE>
Hep3B NFHRN49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLEOFghcA>? NVHwe5M1UUN3ME20MlIzOyEEsTCwMlg{QSEQvF2= NIjFNGQzOzV2NkW5NS=>
PLC/PRF5 MnjUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvzd3A2PDhiaB?= MUDJR|UxRTF4LkGyNEDDuSB2LkCwNUDPxE1? Mli0NlM2PDZ3OUG=
Huh7 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4H0NFQ5KGh? NWW3cVBjUUN3ME2xOU4xODdiwsGgO{4{OzRizszN M4TSflI{PTR4NUmx
HepG2 M13nRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXpO|IhcA>? NV3SeYwyUUN3ME2xMlIxOCEEsTCwMlIzPiEQvF2= NF\RZ3QzOzV2NkW5NS=>
Hep3B M{S0c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[3NkBp M2ewZWlEPTB;MD64PVIhyrFiMD6wOFQh|ryP NXnueZNHOjN3NE[1PVE>
PLC/PRF5 M2jlWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHKO|IhcA>? NGj3NnBKSzVyPUOuNVExKMLzIECuN|M4KM7:TR?= NX;lTpExOjN3NE[1PVE>
Huh7 M3Xsfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3YSYVoPzJiaB?= NX\Zb49OUUN3ME2zMlk5OCEEsTCwMlgxOyEQvF2= M2\ObVI{PTR4NUmx
MFE280 NGfLO29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojmTWM2OD1yLkSyJOKyKDBwME[g{txO NUfhWlIzOjN2NEO4NFU>
AN3CA Mn;QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonDTWM2OD1yLkWwJOKyKDBwMUCg{txO MorUNlM1PDN6MEW=
HEC155 NHLBd|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTBwNk[gxtEhOC5yOTFOwG0> M323ZlI{PDR|OEC1
MFE296 M2jaPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTBwNk[gxtEhOC5zOTFOwG0> MXmyN|Q1OzhyNR?=
SPAC1S NVfDVGhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DKR2lEPTB;MD63O{DDuSByLkC4JO69VQ>? MXyyN|Q1OzhyNR?=
RL952 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFezOIlKSzVyPUCuPVMhyrFiMD6wNUDPxE1? NV3tU4EyOjN2NEO4NFU>
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SNGII NEfxfVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTFwMkSgxtEhOC5{ODFOwG0> MXGyN|Q1OzhyNR?=
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HEC1A MnflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFwM{SgxtEhOC5|MDFOwG0> M3T4[lI{PDR|OEC1
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USPC2 M3S5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LuOGlEPTB;MT62NkDDuSByLkCxJO69VQ>? MmnZNlM1PDN6MEW=
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MFE319 MlHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjBTWM2OD1zLki3JOKyKDBwNEWg{txO NVLzb4VFOjN2NEO4NFU>
EFE184 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3T6[2lEPTB;Mj6wOEDDuSByLkGzJO69VQ>? Mk\WNlM1PDN6MEW=
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HEC1B NYTEO|VnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HINWlEPTB;Mj61O{DDuSByLkKzJO69VQ>? MXiyN|Q1OzhyNR?=
USPC1 MlHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1r1Z2lEPTB;Mj62NEDDuSByLkGzJO69VQ>? MVmyN|Q1OzhyNR?=
SPAC1L NXH0e|JzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIn0dmlKSzVyPUOuNFYhyrFiMT6xOEDPxE1? M1vJ[FI{PDR|OEC1
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HMVEC M3jvTmNmdGxiVnnhZoltcXS7IFHzd4F6 MX6wMVI2KM7:TR?= M2\xZVczKGh? NGHoS|dFVVOR M3TlcYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz MUCyN|IzQDBzNx?=
MHCC-97H M{DV[GNmdGxiVnnhZoltcXS7IFHzd4F6 NEDvdFMxNTJ3IN88US=> NF7sPIs4OiCq M4XKfmROW09? NVPjSJZFcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MnXRNlMzOjhyMUe=
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Sk-Hep1 MVLBdI9xfG:|aYOgRZN{[Xl? MYiwMVEzNjVizszN MXKyOEBp NHrsPXdFVVORwrC= MWPz[Y5{cXSrenXzJGhESyClZXzsd{B1dyCWUlHJUE0h[W6mIITp[4F1fXq3bXHiMYlv\HWlZXSgZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MY[yNlI{ODR5OR?=
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PLC5 NYPKSpNISXCxcITvd4l{KEG|c3H5 MYiwMVEzNjVizszN NH:4SZUzPCCq MXLEUXNQyqB? Mojvd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NIXtUHUzOjJ|MES3PS=>
PLC5 MnLhR4VtdCCYaXHibYxqfHliQYPzZZk> M4LNcVAuOTVizszN MXm3NkBp MUny[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? NEPkeIkzOjF6MEOwPC=>
Hep3B NV\5e2FKS2WubDDWbYFjcWyrdImgRZN{[Xl? M{\UVlAuOTVizszN NIXLV3g4OiCq Mlu2doVlfWOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi M4\PO|IzOThyM{C4
Sk-Hep1 MWrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M1zkR|AuOTVizszN NXf1e3pnPzJiaB?= NF7oZW1z\WS3Y3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M{TWPFIzOThyM{C4
Huh-7 NWrUd2l5S2WubDDWbYFjcWyrdImgRZN{[Xl? NYroU4RFOC1zNTFOwG0> Mnm5O|IhcA>? M1TtNZJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MV6yNlE5ODNyOB?=
PLC5 NGD6c3lCeG:ydH;zbZMhSXO|YYm= M{LiTVAuOTVizszN M3rvN|I1KGh? MX7pcoNz\WG|ZYOgZZBweHSxdHnjJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZLDqA>? MonXNlIyQDB|MEi=
Hep3B MULBdI9xfG:|aYOgRZN{[Xl? MWCwMVE2KM7:TR?= Mm\YNlQhcA>? MnvlbY5kemWjc3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? MkewNlIyQDB|MEi=
Sk-Hep1 NFvFWIdCeG:ydH;zbZMhSXO|YYm= NGX2NnoxNTF3IN88US=> NUnnZnhPOjRiaB?= NVKySFVpcW6lcnXhd4V{KGGyb4D0c5Rq[yClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= MYCyNlE5ODNyOB?=
Huh-7 MmTXRZBweHSxc3nzJGF{e2G7 NE\sbowxNTF3IN88US=> NH36e|AzPCCq MnXJbY5kemWjc3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? MXWyNlE5ODNyOB?=
PLC5 M2TTdmZ2dmO2aX;uJGF{e2G7 MnvtNE0yOCEQvF2= NVi1O4NuOjRiaB?= NVX1Sogy[2G3c3XzJIRwe2VvZHXw[Y5l\W62IFTORUBnemGpbXXueIF1cW:w NHPTe|YzOjF6MEOwPC=>
Hep3B NYm1SopHTnWwY4Tpc44hSXO|YYm= Mn\ZNE0yOCEQvF2= MVKyOEBp MV7jZZV{\XNiZH;z[U1l\XCnbnTlcpQhTE6DIH\yZYdu\W62YYTpc44> M3LHbVIzOThyM{C4
Sk-Hep1 MnHySpVv[3Srb36gRZN{[Xl? NHz5RW8xNTFyIN88US=> M2nYWFI1KGh? NEPTeGpk[XW|ZYOg[I9{\S2mZYDlcoRmdnRiRF7BJIZz[WevZX70ZZRqd25? M3vJWlIzOThyM{C4
Huh-7 NULaS3U6TnWwY4Tpc44hSXO|YYm= M4LPZVAuOTBizszN NGDnfIczPCCq M3jGOYNifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? MVyyNlE5ODNyOB?=
SW780 M4njUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrufXA2KGR? NWjqXoJXUUN3ME21NEBvVQ>? NXzNb|c6OjFzMUm2OlE>
RT112 MoXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWK1JIQ> Mk\mTWM2OD1zNTDuUS=> NI\XPFUzOTFzOU[2NS=>
RT4 MorNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkH3OUBl NUXQNJdrUUN3ME21JI5O NH71VmczOTFzOU[2NS=>
JMSU1 M{\HOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1u0VFUh\A>? MXvJR|UxRTVyIH7N M3u3e|IyOTF7Nk[x
J82 NWrodoNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HifFUh\A>? NEHE[o9KSzVyPUG0NFAhdk1? NFfJd2EzOTFzOU[2NS=>
97-7 NVHoc4tHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDoUYpiPSCm MVHJR|UxRTFyMECgcm0> M2jaWVIyOTF7Nk[x
RT112 MXTGeY5kfGmxbjDBd5NigQ>? NXn2cJBTPTByIH7N NIHGXpEzPCCq NWDLZoZFcW6lcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKEdzwrDhZ4NwdXCjbnnl[EBjgSCjIHTlZ5Jm[XOnIHnuJHMh[W6mIFeyM20heGijc3Xz NVzXeIJiOjFzMUm2OlE>
RT4 MmXTSpVv[3Srb36gRZN{[Xl? MnzLOVAxKG6P MkjqNlQhcA>? M{i4Rolv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= NH3qNJEzOTFzOU[2NS=>
MGH-U3 NXXm[3N5TnWwY4Tpc44hSXO|YYm= NHPEU5A2ODBibl2= NFfnUnkzPCCq MlzkbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| MoDrNlEyOTl4NkG=
SW780 NU\3V|MxTnWwY4Tpc44hSXO|YYm= NYnJ[4lvPTByIH7N MXuyOEBp MlLMbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| NV3FcW83OjFzMUm2OlE>
97-7 NFvESWZHfW6ldHnvckBCe3OjeR?= NH7OPVQ2ODBibl2= NH;DXIgzPCCq M3f1V4lv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= MoTFNlEyOTl4NkG=
 J807C M2jkSWNmdGxiVnnhZoltcXS7IFHzd4F6 MXiwMVQxOCCwTR?= NH\6W|I1QCCq Mli3bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NWTlO4I6OTV3OUi4NVQ>
Y373C MlfkR4VtdCCYaXHibYxqfHliQYPzZZk> MkjBNE01ODBibl2= NU\NOG4xPDhiaB?= NUjZUJhMcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MoHQNVU2QTh6MUS=
K650E MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MofENE01ODBibl2= NHLhVFU1QCCq NXvrd|docW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NFrKXFkyPTV7OEixOC=>
G384D NVnvdY9[S2WubDDWbYFjcWyrdImgRZN{[Xl? Ml71NE01ODBibl2= NGXiUpU1QCCq MnrJbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NVLSV4I2OTV3OUi4NVQ>
F384L MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYewMVQxOCCwTR?= NYCxWppOPDhiaB?= NV;QNGxjcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NID5NIUyPTV7OEixOC=>
KMS11 NGXhVoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEm3eYE4OiCq M4TGZmlEPTB;OUCgcm0> M3q1T|E2PTl6OEG0
KMS18 NUn6UGVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzk[5E4OiCq Mnz2TWM2OD13NUCgcm0> Ml;iNVU2QTh6MUS=
OPM2 MoTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonwO|IhcA>? MWLJR|UxRTlyIH7N MoHWNVU2QTh6MUS=
H929 NWDNb5ZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3n3SVczKGh? MkfYTWM2OD5iMkWwNEBvVQ>? MlPGNVU2QTh6MUS=
8226 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjYeJpwPzJiaB?= MX\JR|UxRiB{NUCwJI5O NGHJNWcyPTV7OEixOC=>
U266 M4q5T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXe3NkBp NY\RTW1TUUN3ME6gNlUxOCCwTR?= NIrKU2IyPTV7OEixOC=>

... 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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