SB590885

Catalog No.S2220

For research use only.

SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM in a cell-free assay, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.

SB590885 Chemical Structure

CAS No. 405554-55-4

Selleck's SB590885 has been cited by 29 publications

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Biological Activity

Description SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM in a cell-free assay, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.
Features Displays significant selectivity for B-Raf over c-Raf.
Targets
B-Raf [1]
(Cell-free assay)
0.16 nM(Ki)
In vitro

SB590885 displays significant selectivity for B-Raf over c-Raf with Ki of 0.16 nM over 1.72 nM. SB-590885 is a more potent inhibitor than the previously described Raf/VEGFR kinase inhibitor BAY 439006 (Ki = 38 nM for mutant B-Raf, 6 nM for c-Raf). SB590885 displays potent selectivity over 46 other kinases. Unlike the multi-kinase inhibitor BAY43-9006, SB590885 stabilizes the oncogenic B-Raf kinase domain in an active configuration. In Colo205, HT29, A375P, SKMEL28, and MALME-3M cells expressing oncogenic B-RafV600E, SB590885 treatment potently inhibits ERK phosphorylation with EC50 of 28 nM, 58 nM, 290 nM, 58 nM, and 190 nM, respectively, and consistently, inhibits the proliferation with EC50 of 0.1 μM, 0.87 μM, 0.37 μM, 0.12 μM, and 0.15 μM, respectively. SB590885 decreases anchorage-independent growth of melanoma cell lines in a BRAF mutant-selective manner. [1] SB590885 displays high affinity for B-Raf with Kd of 0.3 nM. [2] Most of the melanoma cell lines that harbor the BRAF V600E mutation and lack CDK4 mutations (451Lu, WM35, and WM983) are highly sensitive to SB590885 with IC50 of <1 μM. Increased levels of cyclin D1 resulting from genomic amplification mediate SB590885 resistance in B-Raf V600E-mutated melanomas. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 NVfOW|d6TnWwY4Tpc44h[XO|YYm= M2j0bWJqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gUk1JcXN4LYTh[4dm\CCELWLh[kBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|LDDL[F0xNjByMEG2{txO NViwc41XRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwNlQxOzBpPkKyNFI1ODNyPD;hQi=>
white blood cells NWfidIRySW62aX\pZpJwfGmlIHHzd4F6 NVrmcGx3OjVidH:gNVUxKG2pL3vn MniyNVMh\GG7cx?= MV;BcpRq\mmkcn;0bYMh[WO2aY\peJkhcW5iYnzlc416[2mwLXnu[JVk\WRiQ{W3RlEwPiCvb4Xz[UBud2SnbDDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIIfobZRmKGKub3;kJINmdGy|IHnuJIJzd26laH;hcJZmd2yjcjDsZZZi\2ViYYSgNlUhfG9iMUWwJI1oN2upLDDwc{BjcWRiYXTtbY5qe3SncnXkJFIhcHK|IIDybY9zKGKuZX;tfYNqdiCrbnT1Z5Rqd25iZn;yJFE{KGSjeYO= M3LCV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkKyNFM3Lz5{MkKyNlA{PjxxYU6=
insect cells Mn34SpVv[3Srb36gZZN{[Xl? NFPMTmY{OCCvaX7z MWHJcohq[mm2aX;uJI9nKG[3bHygcIVv\3SqIHj1cYFvKD[KaYOteIFo\2WmIFLSRWYhXjZyMFWgcZV1[W62IHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCrboPlZ5Qh[2WubIOgZ48u\XiycnXzd4lv\yCqdX3hckBETEN|NzCoNUB1dyB|N{igdoV{cWS3ZYOpJJV{cW6pIF3FT|Eh[XNic4Xid5Rz[XSnIHHmeIVzKDNyIH3pcpMtKEmFNUC9NE4xODBzNt88US=> Mo\pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NkG4NlcoRjJ7NE[xPFI4RC:jPh?=
A549 MWjGeY5kfGmxbjDhd5NigQ>? NYC3fWpRPjBibXnudy=> MlLhTY5pcWKrdHnvckBw\iCELWLh[kBXPjByRTDteZRidnRvbXXkbYF1\WRiRYLrJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IE[wJI1qdnNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCHQ{WwQVAvODJ6zszN M1jlUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkKyNFM3Lz5{MkKyNlA{PjxxYU6=
Colo205 NH:5NWRHfW6ldHnvckBie3OjeR?= M13yZlYxKG2rboO= MmPjTY5pcWKrdHnvckBw\iCELWLh[kBXPjByRTDteZRidnRvbXXkbYF1\WRiRYLrJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDDc4xwOjB3IHPlcIx{KGGodHXyJFYxKG2rboOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|LDDFR|UxRTBwMEK4{txO MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ{MkCzOkc,OjJ{MkKwN|Y9N2F-
HT-29 M336ZWZ2dmO2aX;uJIF{e2G7 NHfWdHk3OCCvaX7z NYPoRWlvUW6qaXLpeIlwdiCxZjDCMXJi\iCYNkCwSUBufXSjboStcYVlcWG2ZXSgSZJsKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA3OCCvaX7zJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygSWM2OD1yLkCyPO69VQ>? M2TCUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkKyNFM3Lz5{MkKyNlA{PjxxYU6=
MALME3M MnXkSpVv[3Srb36gZZN{[Xl? NYTiemF3PjBibXnudy=> M3\GXmlvcGmkaYTpc44hd2ZiQj3SZYYhXjZyMFWgcZV1[W62LX3l[IlifGWmIFXyb{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWFNVUV|TTDj[YxteyCjZoTldkA3OCCvaX7zJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygSWM2OD1yLkCyPO69VQ>? NHW5SJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKyNlA{Pid-MkKyNlIxOzZ:L3G+
SKMEL28 MoP1SpVv[3Srb36gZZN{[Xl? NWS5PVdHPjBibXnudy=> M37PcmlvcGmkaYTpc44hd2ZiQj3SZYYhXjZyMFWgcZV1[W62LX3l[IlifGWmIFXyb{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gV2tOTUx{ODDj[YxteyCjZoTldkA3OCCvaX7zJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygSWM2OD1yLkCyPO69VQ>? MnLrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MkKwN|YoRjJ{MkKyNFM3RC:jPh?=
A375 MV3GeY5kfGmxbjDhd5NigQ>? NGrVS4JKdmirYnn0bY9vKG:oIHKtVoFnKGmwIHj1cYFvKEF|N{WgZ4VtdHNiYYPz[ZN{\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXST{whUUN3ME2wMlI6|ryP MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyOEmxNUc,OjJ6MEi5NVE9N2F-
A375 MY\GeY5kfGmxbjDhd5NigQ>? MY\Jcohq[mm2aX;uJI9nKEKUQV[gWlYxOEVibYX0ZY51KGmwIHj1cYFvKEF|N{WgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEWUSzDwbI9{eGixconsZZRqd25iYomgbY1ufW6xYnzveEBidmGueYPpd{whUUN3ME2wMlI6|ryP M4TpZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NE[xPFI4Lz5{OUS2NVgzPzxxYU6=
A375 NVzzXmhISW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF|N{WgZ4VtdHNiZYjwdoV{e2mwZzDCMXJi\iCYNkCwSUBufXSjboSgZY5lKHerbHSgeJlx\SCUYYOsJGlEPTB;MD6zO:69VQ>? NH;MSZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiwPFkyOSd-MkK4NFg6OTF:L3G+
A375 MkTzR5l1d3SxeHnjbZR6KGG|c3H5 MXq0PEBpenN? MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIhiemKxcnnu[{BDWkGIIG[2NFBGKG23dHHueEBi\nSncjC0PEBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3ME2wMlM4|ryP NVLKVYx1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OlE5OjdpPkK5OFYyQDJ5PD;hQi=>
HFF NVnxbllETnWwY4Tpc44h[XO|YYm= NV;WcmZPPjBibXnudy=> MUXJcohq[mm2aX;uJI9nKEJvUnHmMY1m\GmjdHXkJGVzcyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hUE[IIHPlcIx{KGGodHXyJFYxKG2rboOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|LDDFR|UxRTFwMd88US=> MkjaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MkKwN|YoRjJ{MkKyNFM3RC:jPh?=
HMEC MUjGeY5kfGmxbjDhd5NigQ>? M3fHc|YxKG2rboO= MUDJcohq[mm2aX;uJI9nKEJvUnHmMY1m\GmjdHXkJGVzcyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hUE2HQzDj[YxteyCjZoTldkA3OCCvaX7zJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygSWM2OD1zLkJOwG0> MkjTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MkKwN|YoRjJ{MkKyNFM3RC:jPh?=
PREC NFPhN3BHfW6ldHnvckBie3OjeR?= MlT2OlAhdWmwcx?= MVPJcohq[mm2aX;uJI9nKEJvUnHmMY1m\GmjdHXkJGVzcyCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hWFKHQzDj[YxteyCjZoTldkA3OCCvaX7zJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygSWM2OD1zLkJOwG0> M2DvZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkKyNFM3Lz5{MkKyNlA{PjxxYU6=
HCT116 MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1PmZ|czKGi{cx?= MXXHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMh\XiycnXzd4lv\yC5aXzkMZR6eGViQj3SZYYh[W6mIFutVoF{OiCJMUPEJI12fGGwdDDh[pRmeiB5MjDodpMh[nliV2PUMVEh[XO|YYmsJGVEPTB;MT6x{txO MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ{MkCzOkc,OjJ{MkKwN|Y9N2F-
SK-MEL-2 MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVnE[G96PzJiaILz MXXHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDTT{1OTUxvMjDj[YxteyCneIDy[ZN{cW6pIIfpcIQufHmyZTDCMXJi\iCjbnSgUk1T[XN{IGG2NXIhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDXV3QuOSCjc4PhfUwhTUN3ME2xMlHPxE1? M37JcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkKyNFM3Lz5{MkKyNlA{PjxxYU6=
HCT116 MnGwRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M3nKcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKGJvUnHmJIFv\CCNUlHTJI12fGGwdDygTWM2OD12LkdOwG0> NVnBeI1iRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFg6OTFpPkKyPFA5QTFzPD;hQi=>
Assay
Methods Test Index PMID
Western blot p-MEK / MEK / p-ERK / ERK 25879420
In vivo Administration of SB590885 potently decreases tumorigenesis in murine xenografts established from mutant B-Raf-expressing A375P melanoma cells, and modestly inhibits tumor growth. [1]

Protocol (from reference)

Cell Research:[1]
  • Cell lines: Colo205, HT29, A375P, SKMEL28, and MALME-3M
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 72 hours
  • Method: Cells are treated with increasing concentrations of SB590885 and incubated for 72 hours. Viable cells are quantified using CellTiter-Glo reagent and luminescence detection on a Victor 2V plate reader. Cells are prepared for cell cycle analysis on a Becton Dickinson FACScan. Data is acquired and analyzed using CellQuest v3.3 software.
Animal Research:[1]
  • Animal Models: Female nude mice injected s.c. with of A375P cells
  • Dosages: 50 mg/kg/day
  • Administration: Injection i.p.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% Cremophor EL, 2% N,N-dimethylacetamide, pH 5.0
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 453.54
Formula

C27H27N5O2

CAS No. 405554-55-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CCOC1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC5=C(C=C4)C(=NO)CC5

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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