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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USD 470 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 Mm\wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYXrXIpwUW6qaXLpeIlwdiCxZjDoeY1idiCDQ16gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlExOSCwTR?= NHfWNnhUSU6JRWK=
SH-4 cell NWPud|RiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHnnR3JKdmirYnn0bY9vKG:oIHj1cYFvKFOKLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlAyKG6P NV\tOG5lW0GQR1XS
LB2518-MEL cell Mmf2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmXHTY5pcWKrdHnvckBw\iCqdX3hckBNSjJ3MUitUWVNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC55NjDuUS=> M3rN[3NCVkeHUh?=
A101D cell NECxS2hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGfFNlZKdmirYnn0bY9vKG:oIHj1cYFvKEFzMEHEJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU45OiCwTR?= NYfhV3ZoW0GQR1XS
HT-144 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlHKTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zNESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlYyKG6P M4\Qd3NCVkeHUh?=
SIG-M5 cell M{PvT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{DWOGlvcGmkaYTpc44hd2ZiaIXtZY4hW0mJLV21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU41PSCwTR?= M1G0SHNCVkeHUh?=
DU-4475 cell NYPabmhDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGnPWWZKdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC5{MzDuUS=> M4PaWHNCVkeHUh?=
A375 cells NXTkUWQ6TnWwY4Tpc44h[XO|YYm= MYq3OUBucW6| MXrJcohq[mm2aX;uJI9nKEKUQV[gWlYxOEVibYX0ZY51NW2nZHnheIVlKEWUSzDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iQUO3OUBk\WyuczDh[pRmeiB5NTDtbY5{NCCLQ{WwQVAvODF3IN88US=> MmHJNlM{QTh2NUO=
OCI-AML2 cell NHjiNlFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXvJcohq[mm2aX;uJI9nKGi3bXHuJG9EUS2DTVyyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xOTgQvF2= NXGzSYRYW0GQR1XS
COLO-829 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1rv[mlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz24Nlkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPS54NTDuUS=> NIDt[WFUSU6JRWK=
PSN1 cell NG\HV2NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWnnbJlzUW6qaXLpeIlwdiCxZjDoeY1idiCSU16xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlcvOzdibl2= NYDaV4RpW0GQR1XS
UACC-257 cell NVjwSHR1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MofOTY5pcWKrdHnvckBw\iCqdX3hckBWSUOFLUK1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4NjR7IH7N MXjTRW5ITVJ?
RKO cell NFvlXXJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlK1TY5pcWKrdHnvckBw\iCqdX3hckBTU09iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Nz62O{BvVQ>? MVjTRW5ITVJ?
MMAC-SF cell NEf3RmhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn3XTY5pcWKrdHnvckBw\iCqdX3hckBOVUGFLWPGJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFAvODdibl2= NGnBfldUSU6JRWK=
Calu-6 cell NGWyNldIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NILudGxKdmirYnn0bY9vKG:oIHj1cYFvKEOjbIWtOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUyNjR5IH7N NVr0WIdoW0GQR1XS
LS-513 cell NEnVfXhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4T1N2lvcGmkaYTpc44hd2ZiaIXtZY4hVFNvNUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|QvOTVibl2= MXPTRW5ITVJ?
NOS-1 cell MmHpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYPJcohq[mm2aX;uJI9nKGi3bXHuJG5QWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUKuOlUhdk1? M1zNW3NCVkeHUh?=
SW872 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3rKSWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d6N{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25Ok41QCCwTR?= MXnTRW5ITVJ?
KMOE-2 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3Pt[mlvcGmkaYTpc44hd2ZiaIXtZY4hU02RRT2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVE2Njh6IH7N NESzW3hUSU6JRWK=
MZ7-mel cell M4TTSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVPxNlN2UW6qaXLpeIlwdiCxZjDoeY1idiCPWketcYVtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTF5LkK3JI5O NGnVRnVUSU6JRWK=
CGTH-W-1 cell Mon5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml\OTY5pcWKrdHnvckBw\iCqdX3hckBET1SKLWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzOS5|IH7N NULqXpNMW0GQR1XS
CP66-MEL cell NIrWfYdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWTJcohq[mm2aX;uJI9nKGi3bXHuJGNRPjZvTVXMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMyNjd4IH7N NX3wfXN5W0GQR1XS
K5 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVfJcohq[mm2aX;uJI9nKGi3bXHuJGs2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTN2LkKgcm0> NV21SGJ4W0GQR1XS
HL-60 cell NXjOOHVtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXXJVYRkUW6qaXLpeIlwdiCxZjDoeY1idiCKTD22NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2PC52MTDuUS=> M3L1b3NCVkeHUh?=
ONS-76 cell NYH0NG1JT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHfNPVFKdmirYnn0bY9vKG:oIHj1cYFvKE:QUz23OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE3Pi54MjDuUS=> NGjWOZNUSU6JRWK=
NB69 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFXE[oxKdmirYnn0bY9vKG:oIHj1cYFvKE6ENkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPVEvOzFibl2= M4jqO3NCVkeHUh?=
LAMA-84 cell Ml;vS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEPaSINKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yQTJwNEKgcm0> M1zJZ3NCVkeHUh?=
EM-2 cell  NIjFTmdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX;EdFNIUW6qaXLpeIlwdiCxZjDoeY1idiCHTT2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVk2NjlzIH7N MWnTRW5ITVJ?
IST-MEL1 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M37UVWlvcGmkaYTpc44hd2ZiaIXtZY4hUVOWLV3FUFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zODRwMUOgcm0> NIDPfJpUSU6JRWK=
HCC2998 cell NIXFXYpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlnJTY5pcWKrdHnvckBw\iCqdX3hckBJS0N{OUm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOjF6NzFOwG0> MV\TRW5ITVJ?
GDM-1 cell NGnJcHBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MULJcohq[mm2aX;uJI9nKGi3bXHuJGdFVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yNlk1PyEQvF2= NGnLb5RUSU6JRWK=
MZ1-PC cell NEDrXYtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUG5elJlUW6qaXLpeIlwdiCxZjDoeY1idiCPWkGtVGMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ5OUm5JO69VQ>? NXrhNGdEW0GQR1XS
BB49-HNC cell M3\RUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXTESIx4UW6qaXLpeIlwdiCxZjDoeY1idiCEQkS5MWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{WxPEDPxE1? MlPPV2FPT0WU
D-392MG cell NIjHZ25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1vIUWlvcGmkaYTpc44hd2ZiaIXtZY4hTC1|OULNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzV4MEeg{txO MU\TRW5ITVJ?
697 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4GwR2lvcGmkaYTpc44hd2ZiaIXtZY4hPjl5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{[zMlg5KM7:TR?= NFfaWZJUSU6JRWK=
ML-2 cell NWXVNodXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYfMcYJ2UW6qaXLpeIlwdiCxZjDoeY1idiCPTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|Y5Njh4IH7N M3LORXNCVkeHUh?=
MEG-01 cell MlXMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHXROohKdmirYnn0bY9vKG:oIHj1cYFvKE2HRz2wNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzd4IN88US=> MYDTRW5ITVJ?
SK-MEL-1 cell NYrrV2JUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH;ydVBKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|OEO2NkDPxE1? MVPTRW5ITVJ?
KS-1 cell MoLWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NI\XU|hKdmirYnn0bY9vKG:oIHj1cYFvKEuVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM6OzN5IN88US=> Mon2V2FPT0WU
NB14 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmK3TY5pcWKrdHnvckBw\iCqdX3hckBPSjF2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60PVM{OSEQvF2= NX3jWFUyW0GQR1XS
NCI-H747 cell NHPae4NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX\Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{S3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42ODZ|NzFOwG0> MlXTV2FPT0WU
K-562 cell MmP5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWnu[2xRUW6qaXLpeIlwdiCxZjDoeY1idiCNLUW2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjZ4OUWg{txO NXrJTFVbW0GQR1XS
NCI-H1648 cell NWO1VpB4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{f1S2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlQ5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54N{K2OkDPxE1? NE\zTWVUSU6JRWK=
LAN-6 cell M13ufWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1\lcGlvcGmkaYTpc44hd2ZiaIXtZY4hVEGQLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlY5OjN4IN88US=> MV3TRW5ITVJ?

... 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:
30% PEG400+0.5% Tween80+5% propylene glycol
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 451.52
Formula

C27H25N5O2

CAS No. 878739-06-1
Storage powder
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