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 27 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 NXLnZoZQTnWwY4Tpc44h[XO|YYm= MVrCbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIF6tTIl{Pi22YXfn[YQhSi2UYX[g[ZhxemW|c3XkJIlvKFOoOTDj[YxteyxiS3S9NE4xODBzNt88US=> NX\k[3ZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwNlQxOzBpPkKyNFI1ODNyPD;hQi=>
white blood cells M4TzfWFvfGmoaXLyc5Rq[yCjc4PhfS=> MnK1NlUhfG9iMUWwJI1oN2up MVixN{Bl[Xm| M3;TPWFvfGmoaXLyc5Rq[yCjY4Tpeol1gSCrbjDicIVwdXmlaX6tbY5lfWOnZDDDOVdDOS94IH3veZNmKG2xZHXsJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[ge4hqfGViYnzvc4Qh[2WubIOgbY4h[nKxbnPoc4FtfmWxbHHyJIxifmGpZTDheEAzPSC2bzCxOVAhdWdxa3esJJBwKGKrZDDh[I1qdmm|dHXy[YQhOiCqcoOgdJJqd3JiYnzlc416[2mwIHnu[JVkfGmxbjDmc5IhOTNiZHH5dy=> M1jjVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkKyNFM3Lz5{MkKyNlA{PjxxYU6=
insect cells NF\CSnBHfW6ldHnvckBie3OjeR?= M2jGTlMxKG2rboO= NGTvbJVKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJIh2dWGwIE\IbZMufGGpZ3XkJGJTSUZiVk[wNGUhdXW2YX70JIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDpcpNm[3RiY3XscJMh[29vZYjwdoV{e2mwZzDoeY1idiCFRFOzO{ApOSC2bzCzO|ghemW|aXT1[ZMqKHW|aX7nJG1GUzFiYYOgd5Vje3S{YYTlJIFnfGW{IEOwJI1qdnNuIFnDOVA:OC5yMECxOu69VQ>? M1:3ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NE[xPFI4Lz5{OUS2NVgzPzxxYU6=
A549 M1TIW2Z2dmO2aX;uJIF{e2G7 M1u3[FYxKG2rboO= NX;2c2FIUW6qaXLpeIlwdiCxZjDCMXJi\iCYNkCwSUBufXSjboStcYVlcWG2ZXSgSZJsKHCqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFYxKG2rboOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|LDDFR|UxRTBwMEK4{txO NGLHV5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKyNlA{Pid-MkKyNlIxOzZ:L3G+
Colo205 MXnGeY5kfGmxbjDhd5NigQ>? NHvYWFU3OCCvaX7z Mn3xTY5pcWKrdHnvckBw\iCELWLh[kBXPjByRTDteZRidnRvbXXkbYF1\WRiRYLrJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDDc4xwOjB3IHPlcIx{KGGodHXyJFYxKG2rboOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|LDDFR|UxRTBwMEK4{txO MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ{MkCzOkc,OjJ{MkKwN|Y9N2F-
HT-29 M1fveGZ2dmO2aX;uJIF{e2G7 M1XIUlYxKG2rboO= MlfSTY5pcWKrdHnvckBw\iCELWLh[kBXPjByRTDteZRidnRvbXXkbYF1\WRiRYLrJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC2NEBucW6|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqeyxiRVO1NF0xNjB{ON88US=> M4\6WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkKyNFM3Lz5{MkKyNlA{PjxxYU6=
MALME3M NUjYeHoyTnWwY4Tpc44h[XO|YYm= MoHpOlAhdWmwcx?= M4SzZ2lvcGmkaYTpc44hd2ZiQj3SZYYhXjZyMFWgcZV1[W62LX3l[IlifGWmIFXyb{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWFNVUV|TTDj[YxteyCjZoTldkA3OCCvaX7zJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygSWM2OD1yLkCyPO69VQ>? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ{MkCzOkc,OjJ{MkKwN|Y9N2F-
SKMEL28 NU\qUlRvTnWwY4Tpc44h[XO|YYm= MnK5OlAhdWmwcx?= NFzXbVJKdmirYnn0bY9vKG:oIFKtVoFnKFZ4MEDFJI12fGGwdD3t[YRq[XSnZDDFdosheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJHNMVUWOMkigZ4VtdHNiYX\0[ZIhPjBibXnud{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYOsJGVEPTB;MD6wNljPxE1? NX3iNWdNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNlIxOzZpPkKyNlIzODN4PD;hQi=>
A375 M2\oZWZ2dmO2aX;uJIF{e2G7 MVvJcohq[mm2aX;uJI9nKGJvUnHmJIlvKGi3bXHuJGE{PzViY3XscJMh[XO|ZYPz[YQheGixc4Doc5J6dGG2aX;uJI9nKEWUSzygTWM2OD1yLkK5{txO MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyOEmxNUc,OjJ6MEi5NVE9N2F-
A375 NGjW[oZHfW6ldHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKEKUQV[gWlYxOEVibYX0ZY51KGmwIHj1cYFvKEF|N{WgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEWUSzDwbI9{eGixconsZZRqd25iYomgbY1ufW6xYnzveEBidmGueYPpd{whUUN3ME2wMlI6|ryP NYradJFbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OlE5OjdpPkK5OFYyQDJ5PD;hQi=>
A375 M2TEcWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF|N{WgZ4VtdHNiZYjwdoV{e2mwZzDCMXJi\iCYNkCwSUBufXSjboSgZY5lKHerbHSgeJlx\SCUYYOsJGlEPTB;MD6zO:69VQ>? NFL5PFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiwPFkyOSd-MkK4NFg6OTF:L3G+
A375 NF7rRZFEgXSxdH;4bYNqfHliYYPzZZk> MXG0PEBpenN? Mnf1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVM4PSClZXzsd{Bp[XKkb4LpcochSlKDRjDWOlAxTSCvdYThcpQh[W[2ZYKgOFghcHK|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEmFNUC9NE4{P87:TR?= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR4MUiyO{c,Ojl2NkG4Nlc9N2F-
HFF M3yy[GZ2dmO2aX;uJIF{e2G7 MorZOlAhdWmwcx?= NGji[3dKdmirYnn0bY9vKG:oIFKtVoFnNW2nZHnheIVlKEW{azDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iSF\GJINmdGy|IHHmeIVzKDZyIH3pcpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nzMEBGSzVyPUGuNe69VQ>? M3HOclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkKyNFM3Lz5{MkKyNlA{PjxxYU6=
HMEC MoLuSpVv[3Srb36gZZN{[Xl? NX;wZWNzPjBibXnudy=> NVLO[Hl6UW6qaXLpeIlwdiCxZjDCMXJi\i2vZXTpZZRm\CCHcnugdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFjNSWMh[2WubIOgZYZ1\XJiNkCgcYlveyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZMtKEWFNUC9NU4y|ryP NY[0TJFwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNlIxOzZpPkKyNlIzODN4PD;hQi=>
PREC NV3mUJc6TnWwY4Tpc44h[XO|YYm= M4TrTFYxKG2rboO= NXS0OnVDUW6qaXLpeIlwdiCxZjDCMXJi\i2vZXTpZZRm\CCHcnugdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGDSSWMh[2WubIOgZYZ1\XJiNkCgcYlveyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZMtKEWFNUC9NU4y|ryP NXGzb|N7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNlIxOzZpPkKyNlIzODN4PD;hQi=>
HCT116 Mk\LS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEX6ZoE4OiCqcoO= MYnHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMh\XiycnXzd4lv\yC5aXzkMZR6eGViQj3SZYYh[W6mIFutVoF{OiCJMUPEJI12fGGwdDDh[pRmeiB5MjDodpMh[nliV2PUMVEh[XO|YYmsJGVEPTB;MT6x{txO M4DsUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkKyNFM3Lz5{MkKyNlA{PjxxYU6=
SK-MEL-2 M33McWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYHINXpDPzJiaILz MX7Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDTT{1OTUxvMjDj[YxteyCneIDy[ZN{cW6pIIfpcIQufHmyZTDCMXJi\iCjbnSgUk1T[XN{IGG2NXIhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDXV3QuOSCjc4PhfUwhTUN3ME2xMlHPxE1? NWTaOWhGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNlIxOzZpPkKyNlIzODN4PD;hQi=>
HCT116 M3rNdmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MlS4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOg[ZhxemW|c3nu[{B4cWymIIT5dIUh[i2UYX[gZY5lKEuUQWOgcZV1[W62LDDJR|UxRTRwNt88US=> MkTqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEi5NVEoRjJ{OEC4PVEyRC:jPh?=
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.
  • (Only for Reference)
Animal Research:[1]
  • Animal Models: Female nude mice injected s.c. with of A375P cells
  • Dosages: 50 mg/kg/day
  • Administration: Injection i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 5 mg/mL
(11.02 mM)
Water Insoluble
Ethanol Insoluble

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

* 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.

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)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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

Mass Concentration Volume Molecular Weight

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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