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 MlmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPYeI5KSzVyPUCuOFQ6KM7:TR?= NHnhWpczPTJyMkC3Ny=>
SupB15-R M2roU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3Llb2lEPTB;MD61OVgh|ryP NIS4O5QzPTJyMkC3Ny=>
BaF3-pSRα MoC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fEVGlEPTB;MD62Olgh|ryP NEj0SoEzPTJyMkC3Ny=>
BaF3-p210Bcr-Abl NU\5boFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLMOFBKSzVyPUCuOlkzKM7:TR?= Ml7YNlUzODJyN{O=
BaF3-p210Bcr-Abl-T315I MnzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJwNkK2JO69VQ>? Mn:yNlUzODJyN{O=
CCRF-CEM NIrzO2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3ETWM2OD1yLkO5PEDPxE1? M{[5elI2OjB{MEey
CEM/C2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLSTWM2OD1zLkGyOUDPxE1? NUexbWpzOjV{MEKwO|I>
Nalm-6 NXTFdnpkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwM{iyJO69VQ>? NY\pRphKOjV{MEKwO|I>
SEM-K2 M3HJNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLTNVJKSzVyPUCuNFIzKM7:TR?= MmTRNlUzODJyN{K=
HB-1119 Mn2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nveWlEPTB;MD6wNlgh|ryP NVT1[Hk4OjV{MEKwO|I>
RS4:11 NFnNeVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrVXWRKSzVyPUKuPFEh|ryP M2HoN|I2OjB{MEey
Nalm-6 NUf0UllvSXCxcITvd4l{KEG|c3H5 M1HnfVIh|ryP MXeyOE81QCCq NV3PdJR4cW6mdXPld{BieG:ydH;zbZMhemW|dXz0bY5oKGmwIHHic5V1KDd{JTDv[kBk\WyuIHTlZZRpKGGodHXyJFI1KGhidILlZZRu\W62IHHu[EA5OSViYX\0[ZIhPDhiaB?= NXj4PZV5OjV{MEKwO|I>
SEM-K2 NWLLU4pzSXCxcITvd4l{KEG|c3H5 NGPjU44xNjFxMTFOwG0> NYDweFlYOjRiaB?= MUHpcoR2[2W|IHXhdox6KGGyb4D0c5NqeyCxZjDTSW0uUzJiY3XscJMh[XRiMD6xJO69VSCjZoTldkAzPCCq MYeyOVIxOjB5Mh?=
HCT-116 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV:1RWZJUUN3ME2zMlA2OC53ODFOwG0> NYnNd4U5OjR2OUW3OVA>
HT-29 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTVwMkGuPVMh|ryP MnnENlQ1QTV5NUC=
SW-480 MnnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTRwM{OwMlQ4KM7:TR?= M2\lflI1PDl3N{Ww
CaCO2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfyUYw6UUN3ME2zMlI{OC54NDFOwG0> M3jpfFI1PDl3N{Ww
LS174T MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzyfVhKSzVyPUSuN|MxNjR5IN88US=> NEnjS4wzPDR7NUe1NC=>
HEC-1A NXvlUYhrTnWwY4Tpc44hSXO|YYm= NVu3bFhvOC5yNT:wMlEwOC53IN88US=> NHXvfVY4OiCq M3TmWINifXOnczDhJIRm[3KnYYPlJIlvKFOWQWSzMEBGWktuIHHu[EBCU1RicHjvd5Bpd3K7bHH0bY9v NXjzenFVOjR2OUW3OVA>
AN3CA NIDWNFdHfW6ldHnvckBCe3OjeR?= M3rZVlAvODVxMD6xM|AvPSEQvF2= MmLuO|IhcA>? M{TtZoNifXOnczDhJIRm[3KnYYPlJIlvKFOWQWSzMEBGWktuIHHu[EBCU1RicHjvd5Bpd3K7bHH0bY9v NETJSZczPDR7NUe1NC=>
MFE-296  Mm\hSpVv[3Srb36gRZN{[Xl? NFHmPZAxNjB3L{CuNU8xNjVizszN M4HoU|czKGh? MoPxZ4F2e2W|IHGg[IVkemWjc3WgbY4hW1SDVEOsJGVTUyxiYX7kJGFMXCCyaH;zdIhwenmuYYTpc44> NYi0RVYyOjR2OUW3OVA>
UMC3 NYX1bVU2S2WubDDWbYFjcWyrdImgRZN{[Xl? NWXHRYJuOS1zMDFOwG0> M2PXe|czKGh? NYnne|NzcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MlHrNlQ{OjV2NkG=
5637 M3G0ZWNmdGxiVnnhZoltcXS7IFHzd4F6 NH:1WJkyNTFyIN88US=> M3rR[|czKGh? NWK0dpFGcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MXGyOFMzPTR4MR?=
HU456 NH\DRWhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NW\mT4FwOS1zMDFOwG0> MVK3NkBp MV7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NEewXpEzPDN{NUS2NS=>
MGHU4 NGfKRpRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUOxMVExKM7:TR?= NWjjT5VyPzJiaB?= MWHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M3nNVlI1OzJ3NE[x
HT1376 M2rNemNmdGxiVnnhZoltcXS7IFHzd4F6 MnvqNU0yOCEQvF2= Mn[wO|IhcA>? MoPYbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MVyyOFMzPTR4MR?=
RT112 NWjTO2NQS2WubDDWbYFjcWyrdImgRZN{[Xl? MXyxMVExKM7:TR?= M333PVczKGh? MlvXbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MViyOFMzPTR4MR?=
T24 NXrCWY1GS2WubDDWbYFjcWyrdImgRZN{[Xl? M3LOclEuOTBizszN M3rSXlczKGh? NEfIXIFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NXvoS4g2OjR|MkW0OlE>
BFTC905 MYHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnW1NU0yOCEQvF2= NFP4R|E4OiCq NWL1TGFUcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M3PLb|I1OzJ3NE[x
TCC-SUP M{DpS2NmdGxiVnnhZoltcXS7IFHzd4F6 M2rwNVEuOTBizszN NE\q[2I4OiCq MWjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> Mle1NlQ{OjV2NkG=
RT4 NUDQeGRVS2WubDDWbYFjcWyrdImgRZN{[Xl? NUfkS3FmOS1zMDFOwG0> NEfaZlQ4OiCq NGeyS4pqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? Mn34NlQ{OjV2NkG=
HONE1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTGNE4yNTFyIN88US=> MlTDOFjDqGh? M4jKbolv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> NF7vZVczPDJ|OEC5OC=>
HNE1 NWHPUGcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml71NE4yNTFyIN88US=> MV[0POKhcA>? MUfpcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= MYSyOFI{QDB7NB?=
CNE2  M2rnU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELSdo0xNjFvMUCg{txO MkXOOFjDqGh? Mne4bY5lfWOnczDHNk9OKGSnbHH5JIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy MV[yOFI{QDB7NB?=
C666-1 NVG4RW9WT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX6wMlEuOTBizszN M4LMS|Q5yqCq NIfvbZBqdmS3Y3XzJGczN01iZHXsZZkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZI> MnvYNlQzOzhyOUS=
HeLa NIXFeHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHHdG4xNjFvMUCg{txO MXKyOEBp MoDEbY5lfWOnczDHNk9OKGG{cnXzeEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> MlnWNlQzOzhyOUS=
Hep3B NXXxS4R3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnIRllvOC5zLUGwJO69VQ>? NFju[W4zPCCq M3r5TIlv\HWlZYOgS|LDqGG{cnXzeOKh NU\vSZdvOjR{M{iwPVQ>
HepG2 MoDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYD1[GpvPDhiaB?= MkHDTWM2OD1{LkeyO{DDuSByLkSyPUDPxE1? MYKyN|U1PjV7MR?=
Hep3B MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnkWmY6PDhiaB?= M33z[WlEPTB;ND6yNlMhyrFiMD64N|kh|ryP Ml64NlM2PDZ3OUG=
PLC/PRF5 NHLEUnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlz1OFghcA>? MoGwTWM2OD1zNj6xNlAhyrFiND6wNFEh|ryP M{Ds[lI{PTR4NUmx
Huh7 MmXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fKdFQ5KGh? MX7JR|UxRTF3LkCwO{DDuSB5LkOzOEDPxE1? MkHRNlM2PDZ3OUG=
HepG2 M3;LNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PaW|czKGh? NGjwUGFKSzVyPUGuNlAxKMLzIECuNlI3KM7:TR?= MnHrNlM2PDZ3OUG=
Hep3B NG\2Vm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3KzNVczKGh? M2ni[mlEPTB;MD64PVIhyrFiMD6wOFQh|ryP NVzNZYlpOjN3NE[1PVE>
PLC/PRF5 NFzlcY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fhZlczKGh? NH\OO5lKSzVyPUOuNVExKMLzIECuN|M4KM7:TR?= NHLL[ZgzOzV2NkW5NS=>
Huh7 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDNO|IhcA>? M1PrfWlEPTB;Mz65PFAhyrFiMD64NFMh|ryP M4nT[FI{PTR4NUmx
MFE280 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\QTWM2OD1yLkSyJOKyKDBwME[g{txO NX62R3pXOjN2NEO4NFU>
AN3CA MlK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\afWlEPTB;MD61NEDDuSByLkGwJO69VQ>? MmD6NlM1PDN6MEW=
HEC155 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7i[XNbUUN3ME2wMlY3KMLzIECuNFkh|ryP NX[5[oRoOjN2NEO4NFU>
MFE296 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLIZ3ZvUUN3ME2wMlY3KMLzIECuNVkh|ryP M4HPWlI{PDR|OEC1
SPAC1S NGnxXHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHk[IxKSzVyPUCuO|chyrFiMD6wPEDPxE1? NGTTZ24zOzR2M{iwOS=>
RL952 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnlV5FlUUN3ME2wMlk{KMLzIECuNFEh|ryP NFTLN3UzOzR2M{iwOS=>
EN1 NXTGemlKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTFwMEKgxtEhOC5{NTFOwG0> MV[yN|Q1OzhyNR?=
SNGII MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3POV2lEPTB;MT6yOEDDuSByLkK4JO69VQ>? NXS0WZZoOjN2NEO4NFU>
ISHIKAWA MojRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzETmZiUUN3ME2xMlMxKMLzIECuNVEh|ryP MWiyN|Q1OzhyNR?=
HEC1A NFX5SHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWWxT4dQUUN3ME2xMlM1KMLzIECuN|Ah|ryP M1voelI{PDR|OEC1
KLE MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTLTWM2OD1zLkO3JOKyKDBwMEKg{txO M1[wbFI{PDR|OEC1
SNGM NHn4SIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LHXGlEPTB;MT60NkDDuSByLkGzJO69VQ>? MUeyN|Q1OzhyNR?=
USPC2 MlPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vTeGlEPTB;MT62NkDDuSByLkCxJO69VQ>? MVSyN|Q1OzhyNR?=
EN M4fIcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnrOVRUUUN3ME2xMlY3KMLzIECuNFEh|ryP NGLPfFkzOzR2M{iwOS=>
MFE319 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTFwOEegxtEhOC52NTFOwG0> M3TsWlI{PDR|OEC1
EFE184 NVjlNHVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHjdXZ1UUN3ME2yMlA1KMLzIECuNVMh|ryP M17MNFI{PDR|OEC1
ECC1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPlXpVKSzVyPUKuNFchyrFiMD6wNUDPxE1? NYTId|dYOjN2NEO4NFU>
HEC1B MonTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPwTWM2OD1{LkW3JOKyKDBwMkOg{txO NH\EXGgzOzR2M{iwOS=>
USPC1 NVHHbY5ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTJwNkCgxtEhOC5zMzFOwG0> NFPnZ4kzOzR2M{iwOS=>
SPAC1L MnHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHlcGVUUUN3ME2zMlA3KMLzIEGuNVQh|ryP MX:yN|Q1OzhyNR?=
HUVEC M134eGNmdGxiVnnhZoltcXS7IFHzd4F6 MYSwMVI2KM7:TR?= NGPZcXA4OiCq NW\0[YdUTE2VTx?= NIi0eFlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MUKyN|IzQDBzNx?=
HMVEC MYjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHnaSo0xNTJ3IN88US=> NFTabpE4OiCq NEO3e5BFVVOR NV33XHZ7cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M{XOO|I{OjJ6MEG3
MHCC-97H MVjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGT2c5YxNTJ3IN88US=> NXHlUJJmPzJiaB?= NHzqe2JFVVOR MXXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MVmyN|IzQDBzNx?=
SMMC7721 NWS5dG9CS2WubDDWbYFjcWyrdImgRZN{[Xl? NHTlSY0xNTJ3IN88US=> NGrxUIY4OiCq NFL1OI9FVVOR MkfMbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> NYPJZVVGOjN{MkiwNVc>
Huh-7 NW\aZnI{SXCxcITvd4l{KEG|c3H5 M{HrTlAuOTJwNTFOwG0> NU\jS4VQOjRiaB?= NUTlV5NTTE2VT9Mg MnTSd4Vve2m2aYrld{BJS0NiY3XscJMhfG9iVGLBTWwuKGGwZDD0bYdifHW8dX3hZk1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MlvwNlIzOzB2N{m=
Sk-Hep1 M4HVemFxd3C2b4Ppd{BCe3OjeR?= NV3ySW1mOC1zMj61JO69VQ>? MmG2NlQhcA>? MnzCSG1UV8Li M3W2VJNmdnOrdHn6[ZMhUEOFIHPlcIx{KHSxIGTSRWlNNSCjbnSgeIlo[XS3eoXtZYIucW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVKyNlI{ODR5OR?=
Hep3B M{XhdWFxd3C2b4Ppd{BCe3OjeR?= MV6wMVEzNjVizszN NHS1TJkzPCCq NFnKZXJFVVORwrC= M3n6NpNmdnOrdHn6[ZMhUEOFIHPlcIx{KHSxIGTSRWlNNSCjbnSgeIlo[XS3eoXtZYIucW6mdXPl[EBieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NEPQb24zOjJ|MES3PS=>
PLC5 MWLBdI9xfG:|aYOgRZN{[Xl? M{m3PVAuOTJwNTFOwG0> MXKyOEBp NWnvRnk4TE2VT9Mg NUXoO|JDe2Wwc3n0bZpmeyCKQ1OgZ4VtdHNidH:gWHJCUUxvIHHu[EB1cWejdIX6eY1i[i2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NILtcnAzOjJ|MES3PS=>
PLC5 NV;TeHlGS2WubDDWbYFjcWyrdImgRZN{[Xl? MYCwMVE2KM7:TR?= NFzSbHc4OiCq MVTy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? MXiyNlE5ODNyOB?=
Hep3B M1m2emNmdGxiVnnhZoltcXS7IFHzd4F6 MWSwMVE2KM7:TR?= MljzO|IhcA>? M4\GWpJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= M1fJUFIzOThyM{C4
Sk-Hep1 M4WyeGNmdGxiVnnhZoltcXS7IFHzd4F6 MXqwMVE2KM7:TR?= NWHIenpIPzJiaB?= MknPdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi MVWyNlE5ODNyOB?=
Huh-7 NGX2N5hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MVuwMVE2KM7:TR?= M3T6flczKGh? MX;y[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? MYWyNlE5ODNyOB?=
PLC5 MYjBdI9xfG:|aYOgRZN{[Xl? NI[3RlIxNTF3IN88US=> MWWyOEBp M3qyeIlv[3KnYYPld{BieG:ydH;0bYMh[2WubDDk[YF1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi Mo\nNlIyQDB|MEi=
Hep3B MX;BdI9xfG:|aYOgRZN{[Xl? Mni0NE0yPSEQvF2= MXuyOEBp M1LQV4lv[3KnYYPld{BieG:ydH;0bYMh[2WubDDk[YF1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi NW\rO|hVOjJzOECzNFg>
Sk-Hep1 MVzBdI9xfG:|aYOgRZN{[Xl? NYPtOIdDOC1zNTFOwG0> NYX5S|ZQOjRiaB?= NIPjWpZqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MVKyNlE5ODNyOB?=
Huh-7 Ml3URZBweHSxc3nzJGF{e2G7 Mk\HNE0yPSEQvF2= NYHwWXk1OjRiaB?= NWP3cJV1cW6lcnXhd4V{KGGyb4D0c5Rq[yClZXzsJIRm[XSqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{wrC= M4K2OlIzOThyM{C4
PLC5 NHzVRlNHfW6ldHnvckBCe3OjeR?= M4Xx[VAuOTBizszN MX[yOEBp NX[3eGJz[2G3c3XzJIRwe2VvZHXw[Y5l\W62IFTORUBnemGpbXXueIF1cW:w NVrKb|VUOjJzOECzNFg>
Hep3B M1O2O2Z2dmO2aX;uJGF{e2G7 NGjOemwxNTFyIN88US=> NI\wVZgzPCCq M3r1c4NifXOnczDkc5NmNWSncHXu[IVvfCCGTlGg[pJi\22nboTheIlwdg>? NWXuNGhJOjJzOECzNFg>
Sk-Hep1 M3qyRWZ2dmO2aX;uJGF{e2G7 M3izbVAuOTBizszN NWPMXnRwOjRiaB?= NUSzc2NT[2G3c3XzJIRwe2VvZHXw[Y5l\W62IFTORUBnemGpbXXueIF1cW:w NFjTPFgzOjF6MEOwPC=>
Huh-7 M2XBN2Z2dmO2aX;uJGF{e2G7 MnXVNE0yOCEQvF2= MYeyOEBp NHjKdZRk[XW|ZYOg[I9{\S2mZYDlcoRmdnRiRF7BJIZz[WevZX70ZZRqd25? NYTxO2hHOjJzOECzNFg>
SW780 NYPjW2RXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHhd48yPSCm M3HGcmlEPTB;NUCgcm0> NX72eo05OjFzMUm2OlE>
RT112 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHmyZZY2KGR? NX\K[mdPUUN3ME2xOUBvVQ>? NGDLWZczOTFzOU[2NS=>
RT4 M4PicWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYC1JIQ> MULJR|UxRTVibl2= NUPW[4RXOjFzMUm2OlE>
JMSU1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PJcVUh\A>? MoLzTWM2OD13MDDuUS=> MWCyNVEyQTZ4MR?=
J82 M{\Vcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjxOUBl MXnJR|UxRTF2MECgcm0> MVqyNVEyQTZ4MR?=
97-7 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfVWHJXPSCm MlWwTWM2OD1zMECwJI5O Mn:yNlEyOTl4NkG=
RT112 MoXSSpVv[3Srb36gRZN{[Xl? MUO1NFAhdk1? MYOyOEBp MoHXbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| NF63ToczOTFzOU[2NS=>
RT4 M3LhVGZ2dmO2aX;uJGF{e2G7 MnnmOVAxKG6P NXntV29oOjRiaB?= MWHpcoNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gS|HDqGGlY3;tdIFvcWWmIHL5JIEh\GWlcnXhd4UhcW5iUzDhcoQhTzJxTTDwbIF{\XN? NX\6bHprOjFzMUm2OlE>
MGH-U3 MX\GeY5kfGmxbjDBd5NigQ>? NVThdWNSPTByIH7N MnfBNlQhcA>? Mn75bY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| M4i4VFIyOTF7Nk[x
SW780 MlT1SpVv[3Srb36gRZN{[Xl? M4jTSVUxOCCwTR?= M1\MXlI1KGh? MlnabY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| MmL6NlEyOTl4NkG=
97-7 M2OzXWZ2dmO2aX;uJGF{e2G7 NX7kSWl4PTByIH7N NYXHPWNMOjRiaB?= M2fCN4lv[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOcLiYXPjc41x[W6rZXSgZpkh[SCmZXPy[YF{\SCrbjDTJIFv\CCJMj;NJJBp[XOncx?= M37F[VIyOTF7Nk[x
 J807C MkC5R4VtdCCYaXHibYxqfHliQYPzZZk> NXvlSGlJOC12MECgcm0> M{W2VVQ5KGh? NGe4NplqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MVmxOVU6QDhzNB?=
Y373C MWLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{OwcVAuPDByIH7N MV:0PEBp NFf3TZRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NFvje3kyPTV7OEixOC=>
K650E M1rMc2NmdGxiVnnhZoltcXS7IFHzd4F6 NFfucnoxNTRyMDDuUS=> NYfFXIVUPDhiaB?= MUjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MorGNVU2QTh6MUS=
G384D M4r6cmNmdGxiVnnhZoltcXS7IFHzd4F6 M1\XTlAuPDByIH7N NI\pPZI1QCCq MYnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MojTNVU2QTh6MUS=
F384L NFjPUmZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUG3cYpMOC12MECgcm0> M{jsTVQ5KGh? MXrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> M{SzUVE2PTl6OEG0
KMS11 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vySFczKGh? MnTqTWM2OD17MDDuUS=> MofINVU2QTh6MUS=
KMS18 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYO3NkBp M4fGbGlEPTB;NUWwJI5O MYmxOVU6QDhzNB?=
OPM2 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3lVVJxPzJiaB?= NH;ye|BKSzVyPUmwJI5O NHvPO5UyPTV7OEixOC=>
H929 M13uVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPDO|IhcA>? NVnwT|lyUUN3ME6gNlUxOCCwTR?= MVuxOVU6QDhzNB?=
8226 NFLhSVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13uW|czKGh? MXXJR|UxRiB{NUCwJI5O MY[xOVU6QDhzNB?=
U266 NG\6Ro5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWCyR5VnPzJiaB?= M3XqRWlEPTB-IEK1NFAhdk1? NYjMTZUyOTV3OUi4NVQ>

... 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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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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