AZ 628

Catalog No.S2746

AZ 628 Chemical Structure

Molecular Weight(MW): 451.52

AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM in cell-free assays, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.

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In DMSO USD 270 In stock
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2 Customer Reviews

  • A375 cells were infected with the indicated shRNAs/ORFs. In parallel to the above, cells were also treated with 0.2 uM AZ628 for 16 h, cell lysates were analyzed by Western blotting for the indicated proteins.

    Cancer Discov 2013 3(3), 350-62. AZ 628 purchased from Selleck.

    Enzymatic activity of RIP3 from Abcam, the concentration-effect relationship of RIP3 inhibition by the tested protein kinase inhibitors and the mode of action of RIP3 inhibition by dabrafenib. The RIP3 inhibition rates of AZ628 at different concentrations were measured by the luminescent RIP3 assay. The data (mean ?SD from 3 independent experiments) were presented as the Lineweaver-Burk plots using Graphpad Prism 5.

    Cell Death Dis 2014 5, e1278. AZ 628 purchased from Selleck.

Purity & Quality Control

Choose Selective Raf Inhibitors

Biological Activity

Description AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM in cell-free assays, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.
Targets
C-Raf-1 [1]
(Cell-free assay)
B-Raf (V600E) [1]
(Cell-free assay)
B-Raf [1]
(Cell-free assay)
29 nM 34 nM 105 nM
In vitro

AZ628 prevents activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ628 suppresses anchorage-dependent and -independent growth, gives rise to cell cycle arrest, and induces apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation. The profile of AZ628 cross-reactivity suggests that similar to sorafenib, AZ628 may be antiangiogenic based on prevention of VEGFR2. [1] AZ628-resistant clones are approximately 100-fold more resistant to AZ628 than the parental cell line, exhibiting IC50 of approximately 10 μM, compared with 0.1 μM for the parental cell line. Effective suppression of p-ERK1/2 levels is observed in the M14 parental cell line following treatment with increasing concentrations of AZ628. AZ628-resistant clones express elevated CRAF. Elevated CRAF expression is a potential mechanism of acquired resistance to continuous AZ628 exposure, resulting in sustained activation of ERK1/2. p-ERK1/2 activity is not significantly inhibited by exposure to AZ628 in one of these three AZ628-insensitive cell lines (Wm1552C). Unlike in the AZ628-resistant M14 cells in which AZ628 fails to suppress the activation of ERK, AZ628 treatment efficiently attenuates ERK activation in the NRAS mutant melanoma cells.[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ACN cell NV;Yfpp{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYDJcohq[mm2aX;uJI9nKGi3bXHuJGFEViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUCxJI5O NX;xVGdvW0GQR1XS
SH-4 cell MkfWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV3OeHRPUW6qaXLpeIlwdiCxZjDoeY1idiCVSD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{4xOSCwTR?= NUHp[pdtW0GQR1XS
LB2518-MEL cell MoXhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHjIeY9KdmirYnn0bY9vKG:oIHj1cYFvKEyEMkWxPE1OTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Lke2JI5O MXfTRW5ITVJ?
A101D cell M2TwUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2\SUWlvcGmkaYTpc44hd2ZiaIXtZY4hSTFyMVSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlgzKG6P MmryV2FPT0WU
HT-144 cell NVnpPXlKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2XySWlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUS0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok43OSCwTR?= NYfOTFN3W0GQR1XS
SIG-M5 cell MkPJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGrNVmtKdmirYnn0bY9vKG:oIHj1cYFvKFOLRz3NOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvPDVibl2= NXHjeFFxW0GQR1XS
DU-4475 cell NHr6eoFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF;ycIRKdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC5{MzDuUS=> NEjTenpUSU6JRWK=
A375 cells NYjrVXI3TnWwY4Tpc44h[XO|YYm= M171b|c2KG2rboO= NHnjXFBKdmirYnn0bY9vKG:oIFLSRWYhXjZyMFWgcZV1[W62LX3l[IlifGWmIFXST{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjC3OUBucW6|LDDJR|UxRTBwMEG1JO69VQ>? NVO1bFN7OjN|OUi0OVM>
OCI-AML2 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFnXVGhKdmirYnn0bY9vKG:oIHj1cYFvKE:FST3BUWwzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yMUhOwG0> M4nZXnNCVkeHUh?=
COLO-829 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2TJWmlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz24Nlkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPS54NTDuUS=> M1vtOnNCVkeHUh?=
PSN1 cell NVvGfllvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml\YTY5pcWKrdHnvckBw\iCqdX3hckBRW05zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkeuN|chdk1? Mnr1V2FPT0WU
UACC-257 cell M1XaWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmjYTY5pcWKrdHnvckBw\iCqdX3hckBWSUOFLUK1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4NjR7IH7N MWPTRW5ITVJ?
RKO cell NV:0cIpMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWSyZYNKUW6qaXLpeIlwdiCxZjDoeY1idiCUS1:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zO{43PyCwTR?= MmnKV2FPT0WU
MMAC-SF cell NF;NXYlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEe3fJZKdmirYnn0bY9vKG:oIHj1cYFvKE2PQVOtV2Yh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01OC5yNzDuUS=> NF;uXY1USU6JRWK=
Calu-6 cell NXfDU4c5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVrhcnh2UW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1MVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02OS52NzDuUS=> NH3DNGJUSU6JRWK=
LS-513 cell NX;0S21uT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3HtNmlvcGmkaYTpc44hd2ZiaIXtZY4hVFNvNUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|QvOTVibl2= MoeyV2FPT0WU
NOS-1 cell MknnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2PzNWlvcGmkaYTpc44hd2ZiaIXtZY4hVk:VLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25Nk43PSCwTR?= NV3OOmg1W0GQR1XS
SW872 cell M4q0OWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MY\Jcohq[mm2aX;uJI9nKGi3bXHuJHNYQDd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OU[uOFghdk1? MX\TRW5ITVJ?
KMOE-2 cell MkfIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkPVTY5pcWKrdHnvckBw\iCqdX3hckBMVU:HLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNVUvQDhibl2= NYL6fnlUW0GQR1XS
MZ7-mel cell M1nqZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXzJcohq[mm2aX;uJI9nKGi3bXHuJG1bPy2vZXygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNVcvOjdibl2= NFzXXYpUSU6JRWK=
CGTH-W-1 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXfsXotmUW6qaXLpeIlwdiCxZjDoeY1idiCFR2TIMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{MT6zJI5O MmOwV2FPT0WU
CP66-MEL cell NIn6XHpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGNRPjZvTVXMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMyNjd4IH7N MVnTRW5ITVJ?
K5 cell NFT3cJlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYDJcohq[mm2aX;uJI9nKGi3bXHuJGs2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTN2LkKgcm0> Mn;wV2FPT0WU
HL-60 cell M3\hVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFLXfYhKdmirYnn0bY9vKG:oIHj1cYFvKEiOLU[wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVU1NjRzIH7N NHXKZlJUSU6JRWK=
ONS-76 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NY\TZVlEUW6qaXLpeIlwdiCxZjDoeY1idiCRTmOtO|Yh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPjZwNkKgcm0> M{fVWnNCVkeHUh?=
NB69 cell MnfiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFPONnpKdmirYnn0bY9vKG:oIHj1cYFvKE6ENkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPVEvOzFibl2= NFHMU2NUSU6JRWK=
LAMA-84 cell NVG5T25RT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2O5W2lvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6Oi52MjDuUS=> NUfoR4VrW0GQR1XS
EM-2 cell  Mm\KS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mo\QTY5pcWKrdHnvckBw\iCqdX3hckBGVS1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUm1MlkyKG6P NH3LUFJUSU6JRWK=
IST-MEL1 cell NEOyR2lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M17oUmlvcGmkaYTpc44hd2ZiaIXtZY4hUVOWLV3FUFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zODRwMUOgcm0> M3m3OXNCVkeHUh?=
HCC2998 cell NISybJBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVPhSXF3UW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyPVk5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MkG4O{DPxE1? MoT3V2FPT0WU
GDM-1 cell MkXJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYnIWVF1UW6qaXLpeIlwdiCxZjDoeY1idiCJRF2tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjJ7NEeg{txO NHWwVGVUSU6JRWK=
MZ1-PC cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXXJcohq[mm2aX;uJI9nKGi3bXHuJG1bOS2SQzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlc6QTlizszN MkTOV2FPT0WU
BB49-HNC cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWfJcohq[mm2aX;uJI9nKGi3bXHuJGJDPDlvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PTF6IN88US=> NXzXXFczW0GQR1XS
D-392MG cell M4C0Omdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXfJcohq[mm2aX;uJI9nKGi3bXHuJGQuOzl{TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM2PjB5IN88US=> NFXtTFZUSU6JRWK=
697 cell MkjjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXnVV2RPUW6qaXLpeIlwdiCxZjDoeY1idiB4OUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOlMvQDhizszN NXLFcHp{W0GQR1XS
ML-2 cell NGrlNGNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXLjVHZwUW6qaXLpeIlwdiCxZjDoeY1idiCPTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|Y5Njh4IH7N NFn5OIlUSU6JRWK=
MEG-01 cell NHfkWIhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mm[2TY5pcWKrdHnvckBw\iCqdX3hckBOTUdvMEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM4PiEQvF2= M4X5TnNCVkeHUh?=
SK-MEL-1 cell NF;uPFZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkDGTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzh|NkKg{txO MlzaV2FPT0WU
KS-1 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV;BUVdWUW6qaXLpeIlwdiCxZjDoeY1idiCNUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{QTN|NzFOwG0> NFTOSINUSU6JRWK=
NB14 cell NIGwfFZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWixTWRwUW6qaXLpeIlwdiCxZjDoeY1idiCQQkG0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE41QTN|MTFOwG0> NF\3[ZdUSU6JRWK=
NCI-H747 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{S3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42ODZ|NzFOwG0> MojUV2FPT0WU
K-562 cell NH[5bJZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEDWPJlKdmirYnn0bY9vKG:oIHj1cYFvKEtvNU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43PjZ7NTFOwG0> NH3UWG5USU6JRWK=
NCI-H1648 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEfnTnBKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY1QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNkeyOlYh|ryP MXTTRW5ITVJ?
LAN-6 cell NHP1NYVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmXTTY5pcWKrdHnvckBw\iCqdX3hckBNSU5vNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlgzOzZizszN MkTtV2FPT0WU

... Click to View More Cell Line Experimental Data

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: M14 expressing the V600E BRAF mutation
  • Concentrations: 0.01-10 μM
  • Incubation Time: Overnight
  • Method: Approximately 0.5-2.5 × 105 M14 cells are seeded in 12 or 24 - well plates, respectively, in medium supplemented with 5% FBS. After overnight incubation, the cells are treated with various concentrations of AZ628. Fresh medium and drug is replaced every 2 days until the untreated control wells reached confluence. At this time-point, the media is removed and the cells are fixed in 4% formaldehyde in PBS for 20 minutes at room temperature. Cells are then washed twice with PBS and stained with a 1:5000 solution of the fluorescent nucleic acid stain Syto60. Quantitation of fluorescent signal intensity is carried out at 700 nm, using an Odyssey Infrared Imager. Each experiment is performed in quadruplicate and the results shown represent the average of the four values compared to untreated wells. Error bars represent standard deviation of the 4 values from the mean. High-throughput cell growth/viability assays are performed.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL (199.32 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% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
6mg/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 451.52
Formula

C27H25N5O2

CAS No. 878739-06-1
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID