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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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 M{fIN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwNES5JO69VQ>? NXjwNI9JOjV{MEKwO|M>
SupB15-R MlL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv6TWM2OD1yLkW1PEDPxE1? MlnCNlUzODJyN{O=
BaF3-pSRα NVzmfJFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTBwNk[4JO69VQ>? MXuyOVIxOjB5Mx?=
BaF3-p210Bcr-Abl MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PrXmlEPTB;MD62PVIh|ryP NIPvNWYzPTJyMkC3Ny=>
BaF3-p210Bcr-Abl-T315I MnLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2mzNGlEPTB;Mj62NlYh|ryP NUHUR|B{OjV{MEKwO|M>
CCRF-CEM MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\VVXdbUUN3ME2wMlM6QCEQvF2= M3KwUFI2OjB{MEey
CEM/C2 NEjUUIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnqUWhYUUN3ME2xMlEzPSEQvF2= M17GflI2OjB{MEey
Nalm-6 M3rXVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTBwM{iyJO69VQ>? NX;hbYxLOjV{MEKwO|I>
SEM-K2 MnfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVL5V3QzUUN3ME2wMlAzOiEQvF2= MmjQNlUzODJyN{K=
HB-1119 NHXuWplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGP1TpdKSzVyPUCuNFI5KM7:TR?= NU\4ZYx[OjV{MEKwO|I>
RS4:11 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF2wd2hKSzVyPUKuPFEh|ryP MXuyOVIxOjB5Mh?=
Nalm-6 MWLBdI9xfG:|aYOgRZN{[Xl? M{LXNVIh|ryP MVSyOE81QCCq MmC2bY5lfWOnczDhdI9xfG:|aYOgdoV{fWy2aX7nJIlvKGGkb4X0JFczLSCxZjDj[YxtKGSnYYToJIFnfGW{IEK0JIghfHKnYYTt[Y51KGGwZDC4NUUh[W[2ZYKgOFghcA>? NELIbFIzPTJyMkC3Ni=>
SEM-K2 M4jpWGFxd3C2b4Ppd{BCe3OjeR?= MlXLNE4yNzFizszN M2n1c|I1KGh? NXrUOVFicW6mdXPld{Bm[XKueTDhdI9xfG:|aYOgc4YhW0WPLVuyJINmdGy|IHH0JFAvOSEQvF2gZYZ1\XJiMkSgbC=> MkLRNlUzODJyN{K=
HCT-116 NWriTpRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvDTWM2OD1|LkC1NE42QCEQvF2= NInkbHQzPDR7NUe1NC=>
HT-29 MlTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTVwMkGuPVMh|ryP M{fEd|I1PDl3N{Ww
SW-480 NXSye2M2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzM[lF6UUN3ME20MlM{OC52NzFOwG0> NVf0XGViOjR2OUW3OVA>
CaCO2 NETsUolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTNwMkOwMlY1KM7:TR?= NH71clEzPDR7NUe1NC=>
LS174T NVjs[VhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LrdmlEPTB;ND6zN|AvPDdizszN NH;sTpozPDR7NUe1NC=>
HEC-1A Mo\0SpVv[3Srb36gRZN{[Xl? MVKwMlA2NzBwMT:wMlUh|ryP NXXiZVZ2PzJiaB?= NVHVV2lZ[2G3c3XzJIEh\GWlcnXhd4UhcW5iU2TBWFMtKEWUSzygZY5lKEGNVDDwbI9{eGixconsZZRqd25? MmryNlQ1QTV5NUC=
AN3CA MWnGeY5kfGmxbjDBd5NigQ>? MlrLNE4xPS9yLkGvNE42KM7:TR?= MX23NkBp NVr4VWo5[2G3c3XzJIEh\GWlcnXhd4UhcW5iU2TBWFMtKEWUSzygZY5lKEGNVDDwbI9{eGixconsZZRqd25? NFm3VpIzPDR7NUe1NC=>
MFE-296  NXnMfFVGTnWwY4Tpc44hSXO|YYm= NF22SJUxNjB3L{CuNU8xNjVizszN M{TBcVczKGh? MnOyZ4F2e2W|IHGg[IVkemWjc3WgbY4hW1SDVEOsJGVTUyxiYX7kJGFMXCCyaH;zdIhwenmuYYTpc44> M1PQWVI1PDl3N{Ww
UMC3 MWrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3fqeVEuOTBizszN M1jh[FczKGh? NEXNWlNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NYfIc3FqOjR|MkW0OlE>
5637 NEG4fnZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGXwdlMyNTFyIN88US=> NF;DPWo4OiCq NYX0UHJycW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NGCySoIzPDN{NUS2NS=>
HU456 M13IPGNmdGxiVnnhZoltcXS7IFHzd4F6 MVKxMVExKM7:TR?= NYXtTWJXPzJiaB?= NGHVeGxqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NX\RdnU2OjR|MkW0OlE>
MGHU4 MUfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{\zfVEuOTBizszN MnjmO|IhcA>? NV\aXVVqcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MVGyOFMzPTR4MR?=
HT1376 NGD1R|dE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MV2xMVExKM7:TR?= NXW5eYVmPzJiaB?= M17ZZYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz NXfz[2piOjR|MkW0OlE>
RT112 MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUexMVExKM7:TR?= NGnqRZk4OiCq NHywOoVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MmTHNlQ{OjV2NkG=
T24 M4HJSmNmdGxiVnnhZoltcXS7IFHzd4F6 M1K4clEuOTBizszN MXG3NkBp NUD6SGNFcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NWL3VZN7OjR|MkW0OlE>
BFTC905 MVTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYLodnBQOS1zMDFOwG0> NILKdlc4OiCq M2ryfolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz M2LtUVI1OzJ3NE[x
TCC-SUP MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MW[xMVExKM7:TR?= MU[3NkBp MlHvbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MofDNlQ{OjV2NkG=
RT4 M1z4NmNmdGxiVnnhZoltcXS7IFHzd4F6 Mkm0NU0yOCEQvF2= NX7UW4dOPzJiaB?= NILPb5BqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NYT3clJXOjR|MkW0OlE>
HONE1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rPeFAvOS1zMDFOwG0> NVL0dXlYPDkEoHi= NYj2dWZmcW6mdXPld{BIOi:PIHTlcIF6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MVmyOFI{QDB7NB?=
HNE1 NWXCW3l2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MViwMlEuOTBizszN NUTJXnk4PDkEoHi= M2r2UIlv\HWlZYOgS|IwVSCmZXzhfUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> MWKyOFI{QDB7NB?=
CNE2  Ml;CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVmwdohzOC5zLUGwJO69VQ>? M{njXlQ5yqCq MYTpcoR2[2W|IFeyM20h\GWuYYmgbY4h[SClb37j[Y51emG2aX;uMYRmeGWwZHXueEBu[W6wZYK= M{HNWFI1OjN6MEm0
C666-1 NVHYbIN1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHz3S5kxNjFvMUCg{txO NVX0OlJlPDkEoHi= NYe1ToJ{cW6mdXPld{BIOi:PIHTlcIF6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVz MnXhNlQzOzhyOUS=
HeLa NEHpWJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnpU4gxNjFvMUCg{txO NFH6VWczPCCq NYrw[FVncW6mdXPld{BIOi:PIHHydoV{fCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NXTrbXg{OjR{M{iwPVQ>
Hep3B MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFG2UI0xNjFvMUCg{txO NWXYPHRFOjRiaB?= NUHmVGxEcW6mdXPld{BIOsLiYYLy[ZN1yqB? NX61Z3VvOjR{M{iwPVQ>
HepG2 NEHkZnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljMOFghcA>? NF62doxKSzVyPUKuO|I4KMLzIECuOFI6KM7:TR?= M{WxNVI{PTR4NUmx
Hep3B NFH5OnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;6flQ5KGh? NE[wZYVKSzVyPUSuNlI{KMLzIECuPFM6KM7:TR?= NXHpSpMxOjN3NE[1PVE>
PLC/PRF5 M1vzUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3OySFQ5KGh? Mk[1TWM2OD1zNj6xNlAhyrFiND6wNFEh|ryP Mn\jNlM2PDZ3OUG=
Huh7 M3\KUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXZcpU1QCCq M3PDdWlEPTB;MUWuNFA4KMLzIEeuN|M1KM7:TR?= MYeyN|U1PjV7MR?=
HepG2 M1\OfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUS3NkBp MoWyTWM2OD1zLkKwNEDDuSByLkKyOkDPxE1? NVj6WXk6OjN3NE[1PVE>
Hep3B M17nNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlviO|IhcA>? NGnBVm9KSzVyPUCuPFkzKMLzIECuNFQ1KM7:TR?= M4HHSVI{PTR4NUmx
PLC/PRF5 Mnq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3XO|IhcA>? NVn0e202UUN3ME2zMlEyOCEEsTCwMlM{PyEQvF2= MUeyN|U1PjV7MR?=
Huh7 Mn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:3NkBp NVXq[|JbUUN3ME2zMlk5OCEEsTCwMlgxOyEQvF2= M3qxTFI{PTR4NUmx
MFE280 NGXGfJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7l[5FKSzVyPUCuOFIhyrFiMD6wOkDPxE1? MUWyN|Q1OzhyNR?=
AN3CA Ml\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlKwTWM2OD1yLkWwJOKyKDBwMUCg{txO M{fMeFI{PDR|OEC1
HEC155 NXO5NlNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LNRmlEPTB;MD62OkDDuSByLkC5JO69VQ>? MV2yN|Q1OzhyNR?=
MFE296 MnH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1S0N2lEPTB;MD62OkDDuSByLkG5JO69VQ>? Mn7MNlM1PDN6MEW=
SPAC1S MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHSOYxFUUN3ME2wMlc4KMLzIECuNFgh|ryP NHPoV5ozOzR2M{iwOS=>
RL952 NUfGfWY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTBwOUOgxtEhOC5yMTFOwG0> NXzk[G9mOjN2NEO4NFU>
EN1 NXHvcpByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHi3[JhKSzVyPUGuNFIhyrFiMD6yOUDPxE1? MY[yN|Q1OzhyNR?=
SNGII M2\ucWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrUfodKSzVyPUGuNlQhyrFiMD6yPEDPxE1? NX\5fYM1OjN2NEO4NFU>
ISHIKAWA MnHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn1fppDUUN3ME2xMlMxKMLzIECuNVEh|ryP NIO4OZUzOzR2M{iwOS=>
HEC1A M{n0XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MluzTWM2OD1zLkO0JOKyKDBwM{Cg{txO NUTp[WNoOjN2NEO4NFU>
KLE MlnzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIn4WHhKSzVyPUGuN|chyrFiMD6wNkDPxE1? MnjmNlM1PDN6MEW=
SNGM MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7yTWM2OD1zLkSyJOKyKDBwMUOg{txO M4LiOFI{PDR|OEC1
USPC2 M3;nO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYK2V5BIUUN3ME2xMlYzKMLzIECuNFEh|ryP MWiyN|Q1OzhyNR?=
EN Mlm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTFwNk[gxtEhOC5yMTFOwG0> MkXJNlM1PDN6MEW=
MFE319 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjqTWM2OD1zLki3JOKyKDBwNEWg{txO MVyyN|Q1OzhyNR?=
EFE184 NIe0eHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF:w[JhKSzVyPUKuNFQhyrFiMD6xN{DPxE1? M{frUVI{PDR|OEC1
ECC1 Mn7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLSZnM2UUN3ME2yMlA4KMLzIECuNFEh|ryP NXHjW3ZvOjN2NEO4NFU>
HEC1B M1y4WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGSxXFlKSzVyPUKuOVchyrFiMD6yN{DPxE1? NF[zb5ozOzR2M{iwOS=>
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SPAC1L MlLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXK0dGdyUUN3ME2zMlA3KMLzIEGuNVQh|ryP MXSyN|Q1OzhyNR?=
HUVEC MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn[5NE0zPSEQvF2= MoCzO|IhcA>? MXHEUXNQ NIPtR5ZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NWrOO41HOjN{MkiwNVc>
HMVEC M3TYdmNmdGxiVnnhZoltcXS7IFHzd4F6 NUnYTYF7OC1{NTFOwG0> NVfw[olpPzJiaB?= NIK5NZdFVVOR NFvC[oZqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MoXLNlMzOjhyMUe=
MHCC-97H MVfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYjxeW13OC1{NTFOwG0> NHSwUVQ4OiCq NHPJbmFFVVOR NULLZok2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NEDLOVIzOzJ{OECxOy=>
SMMC7721 MVLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MofMNE0zPSEQvF2= M{LBeVczKGh? NW\WR4E1TE2VTx?= MWLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NEfpfGEzOzJ{OECxOy=>
Huh-7 NULaW41WSXCxcITvd4l{KEG|c3H5 MmXwNE0yOi53IN88US=> MUOyOEBp NUDPUXg5TE2VT9Mg MUHz[Y5{cXSrenXzJGhESyClZXzsd{B1dyCWUlHJUE0h[W6mIITp[4F1fXq3bXHiMYlv\HWlZXSgZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NWXqfm1GOjJ{M{C0O|k>
Sk-Hep1 MVzBdI9xfG:|aYOgRZN{[Xl? NV7MbYVDOC1zMj61JO69VQ>? M1mzNFI1KGh? M{mxPWROW00EoB?= NXvS[JFZe2Wwc3n0bZpmeyCKQ1OgZ4VtdHNidH:gWHJCUUxvIHHu[EB1cWejdIX6eY1i[i2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MnzINlIzOzB2N{m=
Hep3B NWXSUFJYSXCxcITvd4l{KEG|c3H5 NInReFYxNTF{LkWg{txO MnTWNlQhcA>? MoC4SG1UV8Li NE\qTIZ{\W6|aYTpfoV{KEiFQzDj[YxteyC2bzDUVmFKVC1iYX7kJJRq\2G2dYr1cYFjNWmwZIXj[YQh[XCxcITvd4l{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NESxS2ozOjJ|MES3PS=>
PLC5 NFK3UWZCeG:ydH;zbZMhSXO|YYm= MXSwMVEzNjVizszN NVXh[FZCOjRiaB?= MojsSG1UV8Li NXK0VFlqe2Wwc3n0bZpmeyCKQ1OgZ4VtdHNidH:gWHJCUUxvIHHu[EB1cWejdIX6eY1i[i2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4LiXlIzOjNyNEe5
PLC5 MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUSwMVE2KM7:TR?= NYrPelhWPzJiaB?= M1;xc5Jm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= Mk\kNlIyQDB|MEi=
Hep3B MUfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MniyNE0yPSEQvF2= M4rOdlczKGh? MnHjdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5mesLi NID4eGozOjF6MEOwPC=>
Sk-Hep1 NUf0fZdSS2WubDDWbYFjcWyrdImgRZN{[Xl? NWGwcWt2OC1zNTFOwG0> MnzkO|IhcA>? MXfy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? NXfvTI8yOjJzOECzNFg>
Huh-7 NYG2T4tPS2WubDDWbYFjcWyrdImgRZN{[Xl? M1W2clAuOTVizszN NHP5b2k4OiCq M3y3[JJm\HWlZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= MkSxNlIyQDB|MEi=
PLC5 MYjBdI9xfG:|aYOgRZN{[Xl? MlvENE0yPSEQvF2= MVuyOEBp MX7pcoNz\WG|ZYOgZZBweHSxdHnjJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZLDqA>? M3LC[|IzOThyM{C4
Hep3B Ml36RZBweHSxc3nzJGF{e2G7 NYjZXGUzOC1zNTFOwG0> NIDJNmkzPCCq NG\CcGhqdmO{ZXHz[ZMh[XCxcITveIlkKGOnbHyg[IVifGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XMEoB?= NIHPfpMzOjF6MEOwPC=>
Sk-Hep1 NVqwXYUxSXCxcITvd4l{KEG|c3H5 M{nMSlAuOTVizszN NVXS[WttOjRiaB?= MnjIbY5kemWjc3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzyqB? NEP4R|AzOjF6MEOwPC=>
Huh-7 NUfLTnZ6SXCxcITvd4l{KEG|c3H5 Mlm0NE0yPSEQvF2= NGLPb3ozPCCq MWPpcoNz\WG|ZYOgZZBweHSxdHnjJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZLDqA>? NGDRN2gzOjF6MEOwPC=>
PLC5 NEDIXphHfW6ldHnvckBCe3OjeR?= NGXLS4UxNTFyIN88US=> NFq3b4MzPCCq MUjjZZV{\XNiZH;z[U1l\XCnbnTlcpQhTE6DIH\yZYdu\W62YYTpc44> NGP3T|EzOjF6MEOwPC=>
Hep3B NGDtbW9HfW6ldHnvckBCe3OjeR?= MnLKNE0yOCEQvF2= NUXYOWFbOjRiaB?= NIf2c4Jk[XW|ZYOg[I9{\S2mZYDlcoRmdnRiRF7BJIZz[WevZX70ZZRqd25? MXyyNlE5ODNyOB?=
Sk-Hep1 NXr3bmlUTnWwY4Tpc44hSXO|YYm= MWSwMVExKM7:TR?= MkLuNlQhcA>? MWfjZZV{\XNiZH;z[U1l\XCnbnTlcpQhTE6DIH\yZYdu\W62YYTpc44> NUS5RVZNOjJzOECzNFg>
Huh-7 MkDNSpVv[3Srb36gRZN{[Xl? M4XD[VAuOTBizszN MVGyOEBp MYXjZZV{\XNiZH;z[U1l\XCnbnTlcpQhTE6DIH\yZYdu\W62YYTpc44> NFPGUIczOjF6MEOwPC=>
SW780 M37INmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DEU|Uh\A>? NFjPSWtKSzVyPUWwJI5O MkLSNlEyOTl4NkG=
RT112 M3PJS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NISxNFU2KGR? M1\KWmlEPTB;MUWgcm0> NVq2UIRNOjFzMUm2OlE>
RT4 Mnu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHxfJc2KGR? M4\UfGlEPTB;NTDuUS=> MW[yNVEyQTZ4MR?=
JMSU1 NHrEUpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HablUh\A>? MmrzTWM2OD13MDDuUS=> MVqyNVEyQTZ4MR?=
J82 M32xW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjFOUBl MUHJR|UxRTF2MECgcm0> M1fLUFIyOTF7Nk[x
97-7 MmjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moj1OUBl MUfJR|UxRTFyMECgcm0> NWPGPYxWOjFzMUm2OlE>
RT112 NEPBbFJHfW6ldHnvckBCe3OjeR?= NXXOeFFOPTByIH7N NH7nZ3MzPCCq Mnv6bY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| MUOyNVEyQTZ4MR?=
RT4 NF\ibWpHfW6ldHnvckBCe3OjeR?= NXTsSVhYPTByIH7N MUSyOEBp MlntbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| M2LRVFIyOTF7Nk[x
MGH-U3 M{O4VWZ2dmO2aX;uJGF{e2G7 MVG1NFAhdk1? Mom2NlQhcA>? MkHSbY5kemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJGcyyqCjY3PvcZBidmmnZDDifUBiKGSnY4LlZZNmKGmwIGOgZY5lKEd{L12gdIhie2W| MoezNlEyOTl4NkG=
SW780 MXfGeY5kfGmxbjDBd5NigQ>? NV7z[XFSPTByIH7N MmDKNlQhcA>? MV\pcoNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gS|HDqGGlY3;tdIFvcWWmIHL5JIEh\GWlcnXhd4UhcW5iUzDhcoQhTzJxTTDwbIF{\XN? M3PWS|IyOTF7Nk[x
97-7 MYTGeY5kfGmxbjDBd5NigQ>? NVmyemwzPTByIH7N NFi2T40zPCCq NEPUb3hqdmO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzIEoHHjZ49ueGGwaXXkJIJ6KGFiZHXjdoVie2ViaX6gV{BidmRiR{KvUUBxcGG|ZYO= NXHPPWlCOjFzMUm2OlE>
 J807C M{PyRmNmdGxiVnnhZoltcXS7IFHzd4F6 M{DwU|AuPDByIH7N M4r0VFQ5KGh? M3\hR4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\SCmZYDlcoRmdnRibXHucoVz Ml\1NVU2QTh6MUS=
Y373C MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NELoOIwxNTRyMDDuUS=> NGPjVXE1QCCq Mo[ybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> MnToNVU2QTh6MUS=
K650E MnXlR4VtdCCYaXHibYxqfHliQYPzZZk> M3vodFAuPDByIH7N MkjPOFghcA>? NFfJdIhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHLkWZIyPTV7OEixOC=>
G384D NVfURodiS2WubDDWbYFjcWyrdImgRZN{[Xl? M2H3NFAuPDByIH7N NGWzZpc1QCCq NEThNIhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NHfnU4EyPTV7OEixOC=>
F384L NFnPN|hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXKwMVQxOCCwTR?= Mmj4OFghcA>? NV7LbnRmcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MnvFNVU2QTh6MUS=
KMS11 M3T6[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7FO|IhcA>? Mn3aTWM2OD17MDDuUS=> NHzx[48yPTV7OEixOC=>
KMS18 M3HzT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3ztUlczKGh? M1f3SWlEPTB;NUWwJI5O NH:yZ|gyPTV7OEixOC=>
OPM2 M{X6S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrwfo1kPzJiaB?= NHi3N4lKSzVyPUmwJI5O NU\OeW9HOTV3OUi4NVQ>
H929 NV\4[5dtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LlTFczKGh? MkjlTWM2OD5iMkWwNEBvVQ>? NGDhbHgyPTV7OEixOC=>
8226 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjvUXQ4OiCq M1zwdGlEPTB-IEK1NFAhdk1? NWLtcYozOTV3OUi4NVQ>
U266 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\IO|IhcA>? M17oS2lEPTB-IEK1NFAhdk1? MYmxOVU6QDhzNB?=

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 30 mg/mL (76.44 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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)

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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