AZ 628

Name: AZ 628
Brand: Selleck Chemicals
SKU: S2746
Rating: 5 (23 reviews)

For research use only. Not for use in humans.

Catalog No.S2746

23 publications

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.

Selleck's AZ 628 has been cited by 23 publications

Cancer Discov, 2013, 3(3):350-62

PubMed: 23288408 ( click the link to review the publication )

Mol Cell, 2019, 75(4):669-682

PubMed: 31302002 ( click the link to review the publication )

Sci Adv, 2019, 5(8):eaav8463

PubMed: 31453322 ( click the link to review the publication )

Dev Cell, 2019, 48(3):345-360

PubMed: 30595535 ( click the link to review the publication )

Dev Cell, 2019, 48(3):345-360

PubMed: 30595535 ( click the link to review the publication )

Pigment Cell Melanoma Res, 2019, 10.1111/pcmr.12824

PubMed: 31518489 ( click the link to review the publication )

J Cell Mol Med, 2019, 10.1111/jcmm.14514

PubMed: 31257716 ( click the link to review the publication )

Exp Gerontol, 2019, 126:110691

PubMed: 31421186 ( click the link to review the publication )

Chembiochem, 2019, 10.1002/cbic.201900266

PubMed: 31152574 ( click the link to review the publication )

Photodermatol Photoimmunol Photomed, 2019, 10.1111/phpp.12520

PubMed: 31618797 ( click the link to review the publication )

Stem Cell Reports, 2018, 11(2):380-394

PubMed: 29983389 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(10):2217-2225

PubMed: 30045926 ( click the link to review the publication )

BMC Cancer, 2018, 18(1):542

PubMed: 29739364 ( click the link to review the publication )

Chembiochem, 2018, 19(18):1988-1997

PubMed: 29992710 ( click the link to review the publication )

Oncotarget, 2018, 9(22):16110-16123

PubMed: 29662630 ( click the link to review the publication )

Am J Physiol Lung Cell Mol Physiol, 2016, 310(2-:L187-201

PubMed: 26589479 ( click the link to review the publication )

Oncotarget, 2016, 7(7):7960-9

PubMed: 26799289 ( click the link to review the publication )

Sci Signal, 2015, 8(373):ra38

PubMed: 25900832 ( click the link to review the publication )

J Med Chem, 2015,

PubMed: ( click the link to review the publication )

Stem Cells, 2015, 10.1002/stem.1990

PubMed: 25788415 ( click the link to review the publication )

Mol Cancer Ther, 2015, 14(12):2700-11

PubMed: 26351322 ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1278

PubMed: 24901049 ( click the link to review the publication )

Oncotarget, 2014, 5(21):10732-44

PubMed: 25313141 ( click the link to review the publication )

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	Incubation Time	Activity Description	PMID
ACN cell	MlXkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MmXTTY5pcWKrdHnvckBw\iCqdX3hckBCS05iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGwNUBvVQ>?	M{DHe3NCVkeHUh?=
SH-4 cell	NVzFcFNCT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NETacoNKdmirYnn0bY9vKG:oIHj1cYFvKFOKLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlAyKG6P	Mm\kV2FPT0WU
LB2518-MEL cell	NGjaVYJIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NYC4ZVNqUW6qaXLpeIlwdiCxZjDoeY1idiCOQkK1NVguVUWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;ND63OkBvVQ>?	Mo\FV2FPT0WU
A101D cell	NUSyPXJOT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NETMRndKdmirYnn0bY9vKG:oIHj1cYFvKEFzMEHEJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU45OiCwTR?=	NH2yN29USU6JRWK=
HT-144 cell	NV2xdnVYT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MoD6TY5pcWKrdHnvckBw\iCqdX3hckBJXC1zNESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22MlYyKG6P	M2XrcnNCVkeHUh?=
SIG-M5 cell	M2HDSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M3XS[2lvcGmkaYTpc44hd2ZiaIXtZY4hW0mJLV21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU41PSCwTR?=	M1PUV3NCVkeHUh?=
DU-4475 cell	NIT0PIxIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MVTJcohq[mm2aX;uJI9nKGi3bXHuJGRWNTR2N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE4zOyCwTR?=	M1zqWnNCVkeHUh?=
A375 cells	MVvGeY5kfGmxbjDhd5NigQ>?	M4fPcVc2KG2rboO=	M1TSPGlvcGmkaYTpc44hd2ZiQmLBSkBXPjByRTDteZRidnRvbXXkbYF1\WRiRWLLJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDBN\|c2KGOnbHzzJIFnfGW{IEe1JI1qdnNuIFnDOVA:OC5yMUWg{txO	Mnj3NlM{QTh2NUO=
OCI-AML2 cell	NXS4bndIT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		Mn[wTY5pcWKrdHnvckBw\iCqdX3hckBQS0lvQV3MNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODF5zszN	M4\ON3NCVkeHUh?=
COLO-829 cell	MmrQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NEX5[o1KdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tPFI6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjVwNkWgcm0>	NEH6SpFUSU6JRWK=
PSN1 cell	M2jaSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M{TjTGlvcGmkaYTpc44hd2ZiaIXtZY4hWFOQMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUK3MlM4KG6P	NWfOWZd7W0GQR1XS
UACC-257 cell	Mk\LS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M2nCRWlvcGmkaYTpc44hd2ZiaIXtZY4hXUGFQz2yOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPy52OTDuUS=>	MVjTRW5ITVJ?
RKO cell	NGXNSnhIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NEK0VXFKdmirYnn0bY9vKG:oIHj1cYFvKFKNTzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUO3MlY4KG6P	MW\TRW5ITVJ?
MMAC-SF cell	MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		Mn7rTY5pcWKrdHnvckBw\iCqdX3hckBOVUGFLWPGJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFAvODdibl2=	M{LSdHNCVkeHUh?=
Calu-6 cell	NVPFO4h5T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MnzJTY5pcWKrdHnvckBw\iCqdX3hckBE[Wy3LU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21NU41PyCwTR?=	NHHhNGpUSU6JRWK=
LS-513 cell	MnuyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M{fhb2lvcGmkaYTpc44hd2ZiaIXtZY4hVFNvNUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O\|QvOTVibl2=	NUnlTHBiW0GQR1XS
NOS-1 cell	NGPEcHRIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MVjJcohq[mm2aX;uJI9nKGi3bXHuJG5QWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;OUKuOlUhdk1?	M3vBWHNCVkeHUh?=
SW872 cell	NGX4co9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M3vpWGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d6N{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25Ok41QCCwTR?=	MlTxV2FPT0WU
KMOE-2 cell	MnjBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NGPkWWhKdmirYnn0bY9vKG:oIHj1cYFvKEuPT1WtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyPS56ODDuUS=>	Ml;lV2FPT0WU
MZ7-mel cell	MmTBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NW\0UnNbUW6qaXLpeIlwdiCxZjDoeY1idiCPWketcYVtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTF5LkK3JI5O	M2X0WnNCVkeHUh?=
CGTH-W-1 cell	NFHWWG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=		Mle1TY5pcWKrdHnvckBw\iCqdX3hckBET1SKLWetNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzOS5\|IH7N	Mk\MV2FPT0WU
CP66-MEL cell	NV7zcYRZT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		M1XlXGlvcGmkaYTpc44hd2ZiaIXtZY4hS1B4Nj3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOzFwN{[gcm0>	MmTSV2FPT0WU
K5 cell	Mo[5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M{XvV2lvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zM{SuNkBvVQ>?	MVXTRW5ITVJ?
HL-60 cell	MkDsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MljFTY5pcWKrdHnvckBw\iCqdX3hckBJVC14MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUG1OE41OSCwTR?=	MYrTRW5ITVJ?
ONS-76 cell	MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MlrXTY5pcWKrdHnvckBw\iCqdX3hckBQVlNvN{[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOlYvPjJibl2=	MYDTRW5ITVJ?
NB69 cell	MlXhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MmnNTY5pcWKrdHnvckBw\iCqdX3hckBPSjZ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MUmxMlMyKG6P	NWfWbVZKW0GQR1XS
LAMA-84 cell	M1vjfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NITXUlFKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yQTJwNEKgcm0>	NV3QcplHW0GQR1XS
EM-2 cell	MoPmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NFPacIdKdmirYnn0bY9vKG:oIHj1cYFvKEWPLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPVUvQTFibl2=	M1vZRXNCVkeHUh?=
IST-MEL1 cell	NWnhUVk5T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NIm3eVlKdmirYnn0bY9vKG:oIHj1cYFvKEmVVD3NSWwyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjB2LkGzJI5O	NFnHNpVUSU6JRWK=
HCC2998 cell	MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGhESzJ7OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIzOTh5IN88US=>	NGn4OYFUSU6JRWK=
GDM-1 cell	NW[5PJZ3T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NHnXdm9KdmirYnn0bY9vKG:oIHj1cYFvKEeGTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOjl2NzFOwG0>	Mmi1V2FPT0WU
MZ1-PC cell	NIPabIlIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M3HiWGlvcGmkaYTpc44hd2ZiaIXtZY4hVVpzLWDDJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zPzl7OTFOwG0>	MVPTRW5ITVJ?
BB49-HNC cell	NH;lfohIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGJDPDlvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4{PTF6IN88US=>	NV32cZdEW0GQR1XS
D-392MG cell	NGPUcYpIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M3ywdGlvcGmkaYTpc44hd2ZiaIXtZY4hTC1\|OULNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOzV4MEeg{txO	MofsV2FPT0WU
697 cell	NUS3U3FiT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MnnzTY5pcWKrdHnvckBw\iCqdX3hckA3QTdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1\|NkOuPFgh\|ryP	M4TzU3NCVkeHUh?=
ML-2 cell	M2Dobmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MWfJcohq[mm2aX;uJI9nKGi3bXHuJG1NNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1\|NkiuPFYhdk1?	Ml63V2FPT0WU
MEG-01 cell	MlfHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MYLJcohq[mm2aX;uJI9nKGi3bXHuJG1GTy1yMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuN\|c3KM7:TR?=	M1:4SnNCVkeHUh?=
SK-MEL-1 cell	NH7v[29Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NIe4eVVKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5\|OEO2NkDPxE1?	M2f3R3NCVkeHUh?=
KS-1 cell	NXHlO5p3T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NEnubldKdmirYnn0bY9vKG:oIHj1cYFvKEuVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM6OzN5IN88US=>	NVfUcGVzW0GQR1XS
NB14 cell	MorPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MYPJcohq[mm2aX;uJI9nKGi3bXHuJG5DOTRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS5N\|MyKM7:TR?=	Ml;lV2FPT0WU
NCI-H747 cell	MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		M{\0WmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3OFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjVyNkO3JO69VQ>?	MofIV2FPT0WU
K-562 cell	Ml[4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MYHJcohq[mm2aX;uJI9nKGi3bXHuJGsuPTZ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD62OlY6PSEQvF2=	MlPuV2FPT0WU
NCI-H1648 cell	MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		M3\POGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlQ5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54N{K2OkDPxE1?	MUnTRW5ITVJ?
LAN-6 cell	MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		M1L3VmlvcGmkaYTpc44hd2ZiaIXtZY4hVEGQLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlY5OjN4IN88US=>	MYfTRW5ITVJ?

... 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 Sci Signal 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 Sci Signal 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)

References

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 Download AZ 628 SDF

Molecular Weight	451.52
Formula	C₂₇H₂₅N₅O₂
CAS No.	878739-06-1
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	CN1C=NC2=C(C=C(NC3=CC(=CC=C3C)NC(=O)C4=CC(=CC=C4)C(C)(C)C#N)C=C2)C1=O

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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

If you have any other enquiries, please leave a message.

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

Selective Raf Inhibitors

SB590885 : B-Raf-selective, K_i=0.16 nM.
Selective Raf Inhibitors

ZM 336372 : C-Raf-selective, IC50=70 nM.
FDA-approved Raf Inhibitor

Sorafenib Tosylate : Approved by FDA for advanced renal cancer.
Newest Raf Inhibitor

TAK-632 ^New : Potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases.

Related Raf Products

LY3009120 ^New

LY03009120 is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. Phase 1.
Ravoxertinib (GDC-0994) ^New

GDC-0994 is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
Ulixertinib (BVD-523) ^New

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
Vemurafenib (PLX4032)

Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-Raf^V600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-Raf^V600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold.

Features:A novel and potent inhibitor of the B-RAF^V600E oncoprotein.
Dabrafenib (GSK2118436)

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.
Sorafenib

Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM in cell-free assays, respectively.
Sorafenib Tosylate

Sorafenib Tosylate is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM in cell-free assays, respectively.
PLX-4720

PLX4720 is a potent and selective inhibitor of B-Raf^V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.
TAK-632

TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf in cell-free assays, respectively, showing less or no inhibition against other tested kinases.
GDC-0879

GDC-0879 is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.

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