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 NG\ISXlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEW2empKdmirYnn0bY9vKG:oIHj1cYFvKEGFTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVAyKG6P M{\WPHNCVkeHUh?=
SH-4 cell MmTLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{nJOmlvcGmkaYTpc44hd2ZiaIXtZY4hW0hvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuNFEhdk1? NXfteItvW0GQR1XS
LB2518-MEL cell NInOXlhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHu1OldKdmirYnn0bY9vKG:oIHj1cYFvKEyEMkWxPE1OTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Lke2JI5O NY\ne2JjW0GQR1XS
A101D cell M4GyU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnHzTY5pcWKrdHnvckBw\iCqdX3hckBCOTBzRDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFIhdk1? NHyzSW1USU6JRWK=
HT-144 cell NVfRdJE1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUjJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTF2NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uOlEhdk1? NFPVN4xUSU6JRWK=
SIG-M5 cell NUjkNW9VT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4e2NWlvcGmkaYTpc44hd2ZiaIXtZY4hW0mJLV21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU41PSCwTR?= NWjUZ2l3W0GQR1XS
DU-4475 cell NILINFhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1\3SWlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjJ|IH7N NUnN[|RvW0GQR1XS
A375 cells Mlm3SpVv[3Srb36gZZN{[Xl? MorqO|UhdWmwcx?= NH;S[IVKdmirYnn0bY9vKG:oIFLSRWYhXjZyMFWgcZV1[W62LX3l[IlifGWmIFXST{BxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjC3OUBucW6|LDDJR|UxRTBwMEG1JO69VQ>? M{jY[lI{Ozl6NEWz
OCI-AML2 cell M{DMZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFPTbYpKdmirYnn0bY9vKG:oIHj1cYFvKE:FST3BUWwzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yMUhOwG0> NUC1UJlJW0GQR1XS
COLO-829 cell M{e4bWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXPJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vOEK5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlUvPjVibl2= M1TBdHNCVkeHUh?=
PSN1 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV3qUo1HUW6qaXLpeIlwdiCxZjDoeY1idiCSU16xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlcvOzdibl2= NFj6U4lUSU6JRWK=
UACC-257 cell NXrWSW9jT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmHHTY5pcWKrdHnvckBw\iCqdX3hckBWSUOFLUK1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4NjR7IH7N M17KdHNCVkeHUh?=
RKO cell NFnncmtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF\RVW1KdmirYnn0bY9vKG:oIHj1cYFvKFKNTzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO3MlY4KG6P M{LMOnNCVkeHUh?=
MMAC-SF cell NVfy[mN5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX3Jcohq[mm2aX;uJI9nKGi3bXHuJG1OSUNvU1[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20NE4xPyCwTR?= M4CwTnNCVkeHUh?=
Calu-6 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoC3TY5pcWKrdHnvckBw\iCqdX3hckBE[Wy3LU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21NU41PyCwTR?= M2LMfnNCVkeHUh?=
LS-513 cell NYHL[ldxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml:2TY5pcWKrdHnvckBw\iCqdX3hckBNWy13MUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23OE4yPSCwTR?= MVrTRW5ITVJ?
NOS-1 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1LXdWlvcGmkaYTpc44hd2ZiaIXtZY4hVk:VLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25Nk43PSCwTR?= NXjrZlROW0GQR1XS
SW872 cell NUTJOmxmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIj3U|JKdmirYnn0bY9vKG:oIHj1cYFvKFOZOEeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVYvPDhibl2= MVTTRW5ITVJ?
KMOE-2 cell M4HDemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYnJcohq[mm2aX;uJI9nKGi3bXHuJGtOV0VvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxOU45QCCwTR?= NEPIcZZUSU6JRWK=
MZ7-mel cell M1myNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NI\wU4tKdmirYnn0bY9vKG:oIHj1cYFvKE2cNz3t[Ywh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOTdwMkegcm0> NHu4W5ZUSU6JRWK=
CGTH-W-1 cell NF7Q[YhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVTJcohq[mm2aX;uJI9nKGi3bXHuJGNIXEhvVz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIyNjNibl2= MUPTRW5ITVJ?
CP66-MEL cell MmLOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXjxSY5rUW6qaXLpeIlwdiCxZjDoeY1idiCFUE[2MW1GVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|MT63OkBvVQ>? Mn\VV2FPT0WU
K5 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2DiZ2lvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zM{SuNkBvVQ>? M2\aUnNCVkeHUh?=
HL-60 cell M1j2S2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm\RTY5pcWKrdHnvckBw\iCqdX3hckBJVC14MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1OE41OSCwTR?= NUDUS2ZQW0GQR1XS
ONS-76 cell NGW2V3pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlfYTY5pcWKrdHnvckBw\iCqdX3hckBQVlNvN{[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOlYvPjJibl2= Ml3PV2FPT0WU
NB69 cell NW\6e20yT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUTVWnhIUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkyNjNzIH7N NXnpb3R[W0GQR1XS
LAMA-84 cell MnLVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHXqR|FKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yQTJwNEKgcm0> NYTHcmc3W0GQR1XS
EM-2 cell  NY\sU|V2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYPJcohq[mm2aX;uJI9nKGi3bXHuJGVONTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zOUWuPVEhdk1? MYXTRW5ITVJ?
IST-MEL1 cell M3XkTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1PXUWlvcGmkaYTpc44hd2ZiaIXtZY4hUVOWLV3FUFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zODRwMUOgcm0> Mo\EV2FPT0WU
HCC2998 cell MkewS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH3aU3BKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{K5PVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ{MUi3JO69VQ>? NWTjfGZPW0GQR1XS
GDM-1 cell M17TdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXvtRXJkUW6qaXLpeIlwdiCxZjDoeY1idiCJRF2tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjJ7NEeg{txO Mn64V2FPT0WU
MZ1-PC cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEXucppKdmirYnn0bY9vKG:oIHj1cYFvKE2cMT3QR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjd7OUmg{txO MlK5V2FPT0WU
BB49-HNC cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Moj2TY5pcWKrdHnvckBw\iCqdX3hckBDSjR7LVjOR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzVzODFOwG0> NX7wflVMW0GQR1XS
D-392MG cell M2fu[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1;nOmlvcGmkaYTpc44hd2ZiaIXtZY4hTC1|OULNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzV4MEeg{txO MoX1V2FPT0WU
697 cell MkP1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJFY6PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN4Mz64PEDPxE1? M{fSOnNCVkeHUh?=
ML-2 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlyzTY5pcWKrdHnvckBw\iCqdX3hckBOVC1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{[4Mlg3KG6P NFu1eZBUSU6JRWK=
MEG-01 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH\FN49KdmirYnn0bY9vKG:oIHj1cYFvKE2HRz2wNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzd4IN88US=> M4Pn[HNCVkeHUh?=
SK-MEL-1 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHfxb4pKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|OEO2NkDPxE1? MXPTRW5ITVJ?
KS-1 cell M3\sT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWHJcohq[mm2aX;uJI9nKGi3bXHuJGtUNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO5N|M4KM7:TR?= NY\DZpJoW0GQR1XS
NB14 cell NWK4XVA4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHrNS4lKdmirYnn0bY9vKG:oIHj1cYFvKE6EMUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ6OzNzIN88US=> NXHqdYlYW0GQR1XS
NCI-H747 cell MnyyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NILtdlNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IO|Q4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC53ME[zO{DPxE1? MXfTRW5ITVJ?
K-562 cell MoHYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3TUPWlvcGmkaYTpc44hd2ZiaIXtZY4hUy13NkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlY3Pjl3IN88US=> MWjTRW5ITVJ?
NCI-H1648 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmH0TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ5Mk[2JO69VQ>? M4DZRXNCVkeHUh?=
LAN-6 cell NEPEcXpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkC2TY5pcWKrdHnvckBw\iCqdX3hckBNSU5vNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlgzOzZizszN M4ny[3NCVkeHUh?=

... 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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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