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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Cited by 14 Publications

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 NUnjeJZIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mle1TY5pcWKrdHnvckBw\iCqdX3hckBCS05iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGwNUBvVQ>? M2DEfXNCVkeHUh?=
SH-4 cell NYTSc4VET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkLKTY5pcWKrdHnvckBw\iCqdX3hckBUUC12IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz6wNUBvVQ>? MUDTRW5ITVJ?
LB2518-MEL cell MkfzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGi5TGVKdmirYnn0bY9vKG:oIHj1cYFvKEyEMkWxPE1OTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Lke2JI5O Mn\EV2FPT0WU
A101D cell NX\kcmtlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmLWTY5pcWKrdHnvckBw\iCqdX3hckBCOTBzRDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFIhdk1? MkT6V2FPT0WU
HT-144 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEnyTpRKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUG0OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvPjFibl2= MYnTRW5ITVJ?
SIG-M5 cell NVPWRY5[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4PQWWlvcGmkaYTpc44hd2ZiaIXtZY4hW0mJLV21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU41PSCwTR?= Mn;IV2FPT0WU
DU-4475 cell M1j5cWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWrJcohq[mm2aX;uJI9nKGi3bXHuJGRWNTR2N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE4zOyCwTR?= NV:0NWpwW0GQR1XS
A375 cells NHvLTmFHfW6ldHnvckBie3OjeR?= MkKwO|UhdWmwcx?= MUPJcohq[mm2aX;uJI9nKEKUQV[gWlYxOEVibYX0ZY51NW2nZHnheIVlKEWUSzDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iQUO3OUBk\WyuczDh[pRmeiB5NTDtbY5{NCCLQ{WwQVAvODF3IN88US=> MY[yN|M6QDR3Mx?=
OCI-AML2 cell NVHISFNiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXTLWpRMUW6qaXLpeIlwdiCxZjDoeY1idiCRQ1mtRW1NOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMEG3{txO Mnv0V2FPT0WU
COLO-829 cell M1fTVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV[5cFNuUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVgzQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ3Lk[1JI5O MVfTRW5ITVJ?
PSN1 cell MmDOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYTJcohq[mm2aX;uJI9nKGi3bXHuJHBUVjFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Nz6zO{BvVQ>? MlnDV2FPT0WU
UACC-257 cell Mor6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYe5bWVuUW6qaXLpeIlwdiCxZjDoeY1idiCXQVPDMVI2PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ5LkS5JI5O M3LWPHNCVkeHUh?=
RKO cell M3e2O2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoHnTY5pcWKrdHnvckBw\iCqdX3hckBTU09iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Nz62O{BvVQ>? NYizOFJXW0GQR1XS
MMAC-SF cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{nvNWlvcGmkaYTpc44hd2ZiaIXtZY4hVU2DQz3TSkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQxNjB5IH7N MWrTRW5ITVJ?
Calu-6 cell NV3BPXd2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHqwVGJKdmirYnn0bY9vKG:oIHj1cYFvKEOjbIWtOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUyNjR5IH7N MkWxV2FPT0WU
LS-513 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1fKVGlvcGmkaYTpc44hd2ZiaIXtZY4hVFNvNUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|QvOTVibl2= MYXTRW5ITVJ?
NOS-1 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV3UcmxmUW6qaXLpeIlwdiCxZjDoeY1idiCQT2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkzNjZ3IH7N MWXTRW5ITVJ?
SW872 cell NUTqe3VkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWfJcohq[mm2aX;uJI9nKGi3bXHuJHNYQDd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OU[uOFghdk1? MkDIV2FPT0WU
KMOE-2 cell Mlr5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1XUXmlvcGmkaYTpc44hd2ZiaIXtZY4hU02RRT2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVE2Njh6IH7N M1rC[HNCVkeHUh?=
MZ7-mel cell NYT0VGk4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHjVN4lKdmirYnn0bY9vKG:oIHj1cYFvKE2cNz3t[Ywh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOTdwMkegcm0> MYrTRW5ITVJ?
CGTH-W-1 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2\DT2lvcGmkaYTpc44hd2ZiaIXtZY4hS0eWSD3XMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOjFwMzDuUS=> NH71e5JUSU6JRWK=
CP66-MEL cell NWDvXVVyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXPJcohq[mm2aX;uJI9nKGi3bXHuJGNRPjZvTVXMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMyNjd4IH7N M{CwWnNCVkeHUh?=
K5 cell Ml7xS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3KwSGlvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zM{SuNkBvVQ>? NUnDXXl6W0GQR1XS
HL-60 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGPNdHFKdmirYnn0bY9vKG:oIHj1cYFvKEiOLU[wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVU1NjRzIH7N Ml21V2FPT0WU
ONS-76 cell NF\0c3dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{nMWmlvcGmkaYTpc44hd2ZiaIXtZY4hV06VLUe2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVY3NjZ{IH7N M4XYcnNCVkeHUh?=
NB69 cell NHL6dVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3XabWlvcGmkaYTpc44hd2ZiaIXtZY4hVkJ4OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5NU4{OSCwTR?= MWrTRW5ITVJ?
LAMA-84 cell NX\H[JJtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1XpTGlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6Oi52MjDuUS=> MYLTRW5ITVJ?
EM-2 cell  MlnlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEjHZpJKdmirYnn0bY9vKG:oIHj1cYFvKEWPLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPVUvQTFibl2= M2C2e3NCVkeHUh?=
IST-MEL1 cell NV;iN2luT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYD3fJhEUW6qaXLpeIlwdiCxZjDoeY1idiCLU2StUWVNOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJyND6xN{BvVQ>? M3Tve3NCVkeHUh?=
HCC2998 cell MnTuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFeyPWhKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{K5PVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ{MUi3JO69VQ>? NWH4bJlxW0GQR1XS
GDM-1 cell NHiwWHdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4m0UGlvcGmkaYTpc44hd2ZiaIXtZY4hT0SPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIzQTR5IN88US=> NEfOXpRUSU6JRWK=
MZ1-PC cell M4[5fWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVfw[nlvUW6qaXLpeIlwdiCxZjDoeY1idiCPWkGtVGMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ5OUm5JO69VQ>? MWHTRW5ITVJ?
BB49-HNC cell NX;ySWViT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIfPTJVKdmirYnn0bY9vKG:oIHj1cYFvKEKENEmtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5|NUG4JO69VQ>? NVe2bnFzW0GQR1XS
D-392MG cell NFPzO4xIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGQuOzl{TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM2PjB5IN88US=> NXr1RnU{W0GQR1XS
697 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M37ReWlvcGmkaYTpc44hd2ZiaIXtZY4hPjl5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{[zMlg5KM7:TR?= MnLwV2FPT0WU
ML-2 cell NWWxZ2gzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFjVc4hKdmirYnn0bY9vKG:oIHj1cYFvKE2OLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOlgvQDZibl2= NFfpV4tUSU6JRWK=
MEG-01 cell M4PjeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3LPT2lvcGmkaYTpc44hd2ZiaIXtZY4hVUWJLUCxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PzZizszN NY\Vb3gxW0GQR1XS
SK-MEL-1 cell NVHoUWp7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mm\5TY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzh|NkKg{txO NYLme2lzW0GQR1XS
KS-1 cell NYjr[nZsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnG5TY5pcWKrdHnvckBw\iCqdX3hckBMWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6zPVM{PyEQvF2= NIfSUFVUSU6JRWK=
NB14 cell NFrGe2pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWTJcohq[mm2aX;uJI9nKGi3bXHuJG5DOTRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5N|MyKM7:TR?= NULldpZuW0GQR1XS
NCI-H747 cell NWe5V5hJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M37wV2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3OFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjVyNkO3JO69VQ>? Ml3UV2FPT0WU
K-562 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVzXS2ZrUW6qaXLpeIlwdiCxZjDoeY1idiCNLUW2NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjZ4OUWg{txO M4iyWHNCVkeHUh?=
NCI-H1648 cell M2CwV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVLDNJdJUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[3NlY3KM7:TR?= M3P5[XNCVkeHUh?=
LAN-6 cell NHzle4dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVezcZNCUW6qaXLpeIlwdiCxZjDoeY1idiCOQV6tOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjh{M{[g{txO MorCV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ERK / ERK / p-MEK / MEK / BIM / BRAF / CRAF ; 

PubMed: 21098728     


Western blots of RAF-MEK pathway components and effectors in parental and AR cells treated with the indicated concentrations of AZ628 for 24 hours.

21098728
Growth inhibition assay
Cell viability ; 

PubMed: 21098728     


Parental (solid lines) COLO201 and COLO206F cells and AR (dashed lines) COLO201-AR and COLO206F-AR cells were treated in triplicate with the indicated concentrations of drug for 72 hours. Viable cell titer was determined, and the average values are shown relative to untreated controls for each cell line. Error bars represent the SD for each measurement. For each cell line, the IC50s for each inhibitor are shown in tabular form along with the increase in IC50 in AR cells relative to parental cells.

21098728

Protocol

Cell Research:[1]
- Collapse
  • 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID