Regorafenib (BAY 73-4506)

Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively.

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Regorafenib (BAY 73-4506) Chemical Structure

Regorafenib (BAY 73-4506) Chemical Structure
Molecular Weight: 482.82

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Product Description

Biological Activity

Description Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively.
Targets RET [1]
(Cell-free assay)
Raf-1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
Kit [1]
(Cell-free assay)

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IC50 1.5 nM 2.5 nM 4.2 nM 7 nM
In vitro Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppress PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptors KITK642E and RETC634W, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively. [1] Regorafenib targets both tumor cell proliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) and serine/threonine kinases (Raf and p38MAPK). [2] Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner. [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Hep3BNV62WWxtSXCxcITvd4l{KEG|c3H5MkPYNgKBmzYEoN88US=>M1jLcFQ5KGh?MVTpcohq[mm2czDj[YxtKGe{b4f0bC=>NIjydJkzPjN{OU[wPC=>
PLC/PRF/5 NUnrUWdjSXCxcITvd4l{KEG|c3H5MYSx5qCUPcLizszNM3P3XlQ5KGh?NGG2RZlqdmirYnn0d{Bk\WyuIHfyc5d1cA>?M1nWTlI3OzJ7NkC4
HepG2 NImyWGVCeG:ydH;zbZMhSXO|YYm=MkK2NgKBmzYEoN88US=>M1L5cFQ5KGh?M3Pa[olvcGmkaYTzJINmdGxiZ4Lve5RpNWTRSWtzOjZ|Mkm2NFg>
HEK293MX3GeY5kfGmxbjDBd5NigQ>?MVewMlXjiIoQvF2=NXP0bItIOi92L{[gbC=>NH:wXmJz\WS3Y3XzJGdTWDd6IHX4dJJme3Orb36=NHL2Z4szPTh3OECzNi=>
GEONFPtUJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MnzHNE4xOS1{MDFOwG0>MV:5OkBpMVvEUXNQMVTpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>NEnIblYzPTh|OEO5NS=>
SW48M4rFbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3uxZVAvODFvMkCg{txONXTPdoljQTZiaB?=NHrze2pFVVORMXXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>NYP4dIdYOjV6M{izPVE>
HT29NV3FNYVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1TIUVAvODFvMkCg{txONGfqZ|M6PiCqM1;hNmROW09?NUnXfId2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?MnfYNlU5Ozh|OUG=
SW480M4\CSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NGG3XWoxNjBzLUKwJO69VQ>?MWK5OkBpMmfoSG1UVw>?M4jFWIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzNV;pUGE3OjV6M{izPVE>
SW620M1fT[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHjaU3ExNjBzLUKwJO69VQ>?MYS5OkBpMWPEUXNQMXfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>NE\vZWczPTh|OEO5NS=>
HCT116MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGrxbVkxNjBzLUKwJO69VQ>?NV7zTI9jQTZiaB?=NFTO[ldFVVORMn36bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>NULhVnROOjV6M{izPVE>
LOVOM1vYT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4T1PVAvODFvMkCg{txOMYO5OkBpMXjEUXNQNE\BWZdqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?MXqyOVg{QDN7MR?=
HCT150MmnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MU[wMlAyNTJyIN88US=>MmTZPVYhcA>?MU\EUXNQMljybY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>NYTtclIzOjV6M{izPVE>
SW48-CRM1zNcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NUPjWoV1OC5yMT2yNEDPxE1?M1Tpdlk3KGh?NFXSVXVFVVORNGrGZo9qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?NWeyNJJ[OjV6M{izPVE>
GEO-CRMVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MVuwMlAyNTJyIN88US=>NHHScVc6PiCqNVLEPXdHTE2VTx?=MlO3bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>MnLuNlU5Ozh|OUG=
KB-31NVLTd2JOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3e4W2lEPTB;NT61xtExNjNibl2=MnuzNlU4PTN|NkG=
KB-G2M3LvVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NYjySYdLUUN3ME25MlHDuTBwMTDuUS=>NH;Rd2MzPTd3M{O2NS=>
LLC-PK1M4\kTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnjyTWM2OD12Mj6wxtE{NjJibl2=NVHuNYh3OjV5NUOzOlE>
LLC-PK1/MRP2MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXXlb4NlUUN3ME24Nk41yrF{Lkegcm0>NI\n[2EzPTd3M{O2NS=>
HEK293M4H1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MX7JR|UxRTFzLkFCtVEvOiCwTR?=MVmyOVc2OzN4MR?=
HEK293/OATP1B1MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MYnJR|UxRTZwMtMxNE4{KG6PM13sO|I2PzV|M{[x
HROC18Mn\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NUTsTI1XUUN3ME2xMlMh|ryPMlPSNlU{ODl7MUS=
HROC24MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NF\GSlJKSzVyPUSuOkDPxE1?MWeyOVMxQTlzNB?=
HROC43MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MofaTWM2OD13LkOg{txOMV6yOVMxQTlzNB?=
HROC46NFm5c5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M17hcmlEPTB;Mj60JO69VQ>?MYSyOVMxQTlzNB?=
RJ345M4DWT2Z2dmO2aX;uJGF{e2G7MYCwMlUwPSEQvF2=NUjHUGxnOjRiaB?=MYrEUXNQMljnbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;uNF:5ZZQzPTJ3M{m5OC=>
RJ348MUHGeY5kfGmxbjDBd5NigQ>?NW\JbYU3OC53L{Wg{txOMkC1NlQhcA>?NGLM[3NFVVORM4[1O4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=>MoXoNlUzPTN7OUS=
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MDA-MB-231NW\0OlNUTnWwY4Tpc44hSXO|YYm=M37WdFAvPS93IN88US=>M3;Ib|I1KGh?MWHEUXNQM4DpWIlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=>MV2yOVI2Ozl7NB?=
HT15NVXBUIVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M2\QTVEuOjBizszNMUe0PEBpMYLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>MViyOVA4OTBzOB?=
DLD1M3\hZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVWxMVIxKM7:TR?=NFXXT5c1QCCqM4LXWIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzMmTENlUxPzFyMUi=
HT-29MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M4W0XFEuOjBizszNNEP0SIg1QCCqM{DsUolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzNUO3d3A1OjVyN{GwNVg>
Hct-116NIWweIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MkK3NU0zOCEQvF2=M{OxNlQ5KGh?NXfGWYF2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?M1jwNFI2ODdzMEG4
HT15MXzBdI9xfG:|aYOgRZN{[Xl?NVXVeHhHOS1zMDFOwG0>Mnv1OFghcA>?MWnpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=NX;MTGdGOjVyN{GwNVg>
DLD1NGj2eY1CeG:ydH;zbZMhSXO|YYm=MkjqNU0yOCEQvF2=M37iSlQ5KGh?MVjpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=MYCyOVA4OTBzOB?=
HT-29MnLuRZBweHSxc3nzJGF{e2G7M17od|EuOTBizszNMlr4OFghcA>?M2HFbIlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>NWnuXFA6OjVyN{GwNVg>
Hct-116Mmq0RZBweHSxc3nzJGF{e2G7MmnVNU0yOCEQvF2=NU\PfJhUPDhiaB?=NFzTZ3dqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>Mnj4NlUxPzFyMUi=
GBM5NHPEeWdCeG:ydH;zbZMhSXO|YYm=MUKwMlXjiJNzLkFihKnPxE1?NIW5SFkzPCCqMWnEUXNQMWrpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi=M{HNVVI1QTFzMkG1
GBM6NG\ifJBCeG:ydH;zbZMhSXO|YYm=NVXNe|ROOC534pETNU4x6oDLzszNMkXTNlQhcA>?NXPKNIFDTE2VTx?=MXTpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi=M2e1[lI1QTFzMkG1
GBM12MmPNRZBweHSxc3nzJGF{e2G7MoToNE426oDVMT6w5qCK|ryPMWWyOEBpM1PNRmROW09?Mk\IbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYToMWWyOFkyOTJzNR?=
GBM14 NXPHPXNbSXCxcITvd4l{KEG|c3H5NUPSbnNYOC534pETNU4x6oDLzszNM1ThWFI1KGh?MX;EUXNQMkLwbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYToNHLBdY4zPDlzMUKxOS=>
Hep3BM1X3VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MYKx5qCUOi53wrFOwG0>M33ZRlI1NzR6L{eyJIg>Ml76bY5pcWKrdIOgZ4VtdCCpcn;3eIg>NVzhSZB6OjR6OEW4PVA>
PLC/PRF/5 M4r2WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUmx5qCUOi53wrFOwG0>M3XHb|I1NzR6L{eyJIg>NVTJT|ZVcW6qaXLpeJMh[2WubDDndo94fGh?NXPOOmpoOjR6OEW4PVA>
HepG2 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NX\BR4RFOeLCk{KuOeKh|ryPMmjUNlQwPDhxN{KgbC=>NUf6do5RcW6qaXLpeJMh[2WubDDndo94fGh?Ml:1NlQ5QDV6OUC=
HCT116 NX2xWmhTTnWwY4Tpc44hSXO|YYm=NHnVclUyOC9{MD:0NEDPxE1?Mn3XNlQhcA>?NILkcIdqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgcXJPSSCneIDy[ZN{cW:wIHnuJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JI1idm6nch?=M2\HSlI1PzZ|NkGx
Lim2405Mnz5SpVv[3Srb36gRZN{[Xl?MkjwOFAh|ryPM{HTdVI1KGh?MkW3bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{NEP0O5ozPDd4M{[xNS=>
LoVoNFm5cmVHfW6ldHnvckBCe3OjeR?=MnOxOFAh|ryPM4P4PVI1KGh?NVLuUW44cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m|NIn5XYMzPDd4M{[xNS=>
Lim1215MWjGeY5kfGmxbjDBd5NigQ>?NXLRSWpEPDBizszNNHXKS5QzPCCqMljYbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{NGXMOVUzPDd4M{[xNS=>
SW48NV;VNJJZTnWwY4Tpc44hSXO|YYm=NH\yXpA1OCEQvF2=MVuyOEBpM{[ycolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>?NIHvcIEzPDd4M{[xNS=>
RKO NUPLfGZZTnWwY4Tpc44hSXO|YYm=NXLROoJzPDBizszNMmC1NlQhcA>?MkjUbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{M1nBOVI1PzZ|NkGx
SW837NG\jcHpHfW6ldHnvckBCe3OjeR?=MorXOFAh|ryPNY\NdXZrOjRiaB?=NEDvT45qdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?M2TYXVI1PzZ|NkGx
SW1463NXvoZZl4TnWwY4Tpc44hSXO|YYm=NGDNOpY1OCEQvF2=Ml7ZNlQhcA>?MYfpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM>Mlu5NlQ4PjN4MUG=
SW480NUTmSpZ4TnWwY4Tpc44hSXO|YYm=MVO0NEDPxE1?NI\yb4ozPCCqM{LnZ4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>?M1LEeFI1PzZ|NkGx
Vaco432M{\hdmZ2dmO2aX;uJGF{e2G7M{fVdlQxKM7:TR?=MXyyOEBpNULVeo94cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m|NX;sXpVZOjR5NkO2NVE>
Vaco400Mmj0SpVv[3Srb36gRZN{[Xl?NV7YOVJJPDBizszNNFKzNYMzPCCqNX\zelVkcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m|M2WxTFI1PzZ|NkGx
DLD1MVTGeY5kfGmxbjDBd5NigQ>?NVHhSYh1PDBizszNNGLBSYUzPCCqNGXSVVlqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?MV[yOFc3OzZzMR?=
HT29 NXy5XYJ7TnWwY4Tpc44hSXO|YYm=MYC0NEDPxE1?M4HsSlI1KGh?NEfnNGRqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?M3e5XVI1PzZ|NkGx
PLC/PRF/5 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NVPLclY5OeLCk{ZCuW0>NGTFUnAzPC92OD:3NkBpNELRVohqdmirYnn0d{Bk\WyuIHfyc5d1cA>?NY\P[mlkOjNzNkmxOFg>
HepG2MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MXGx5qCUPcL3TR?=Mnn0NlQwPDhxN{KgbC=>MWjpcohq[mm2czDj[YxtKGe{b4f0bC=>M1vrTFI{OTZ7MUS4
Hep3B NVvVblYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NIrhSFUy6oDVNdM1US=>NXnST4NJOjRxNEivO|IhcA>?M2LlPYlvcGmkaYTzJINmdGxiZ4Lve5RpMU[yN|E3QTF2OB?=

... Click to View More Cell Line Experimental Data

In vivo Regorafenib reveals potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages in breast MDA-MB-231 and renal 786-O carcinoma models. Regorafenib prevents not only the growth of syngeneic primary 4T1 breast tumors growing orthotopically in the fat pad, but also suppresses the formation of tumor metastasis in the lung. [1]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Kinase assays In vitro assays using recombinant VEGFR2 (murine aa785–aa1367), VEGFR3 (murine aa818–aa1363), PDGFRβ (aa561–aa1106), Raf-1 (aa305–aa648) and BRafV600E (aa409–aa765) kinase domains are performed. Initial in vitro kinase inhibition profiling is performed at a fixed 1 μM Regorafenib concentration. Inhibitory concentration of 50% (IC50) values are determined from selected responding kinases, e.g., VEGFR1 and RET. TIE2 kinase inhibition is measured with a homogeneous time-resolved fluorescence (HTRF) assay using a recombinant fusion protein of glutathione-S-transferase, the intracellular domain of TIE2 and the peptide biotin-Ahx-EPKDDAYPLYSDFG as substrate.

Cell Assay: [1]

Cell lines GIST 882 and TT cells
Concentrations 5 nM-10 μM
Incubation Time 96 hours
Method For proliferation assays, GIST 882 and TT cells are grown in RPMI medium containing L-glutamine, and MDA-MB-231, HepG2 and A375 cells in DMEM always containing 10% hiFBS. Cells are trypsinized, plated at 5×104 cells/well in 96-well plates in complete media containing 10% FBS and grown overnight at 37 °C. The next day, vehicle or Regorafenib serially diluted in complete growth media to between 10 μM and 5 nM final concentrations, and 0.2% DMSO, is added and incubation is continued for 96 hours. Cell proliferation is quantified.

Animal Study: [1]

Animal Models Female athymic NCr nu/nu mice with Colo-205, MDA-MB-231 or 786-O
Formulation PEG400/125 mM aqueous methanesulfonic acid (80/20) or polypropylene glycol/PEG400/Pluronic F68 (42.5/42.5/15 + 20% Aqua)
Dosages 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Wilhelm SM, et al. Int J Cancer, 2011, 129(1), 245-255.

[2] Heng DY, et al. Ther Adv Med Oncol, 2010, 2(1), 39-49.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-01-10)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02439723 Not yet recruiting Metastatic Solid Malignancies|Locally Advanced Solid Malignancies AHS Cancer Control Alberta|Cross Cancer Institute March 2016 Phase 1
NCT02581059 Not yet recruiting Colorectal Cancer|Palliative Care Hoosier Cancer Research Network|Bayer November 2015 Phase 2
NCT02383433 Not yet recruiting Metastatic Pancreatic Adenocarcinoma Case Comprehensive Cancer Center|National Cancer Institut  ...more Case Comprehensive Cancer Center|National Cancer Institute (NCI) November 2015 Phase 2
NCT02638766 Recruiting Gastrointestinal Stromal Tumors Grupo Espanol de Investigacion en Sarcomas|Bayer November 2015 Phase 2
NCT02619435 Recruiting Advanced Colorectal Cancer National Cancer Institute, Naples November 2015 Phase 2

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Chemical Information

Download Regorafenib (BAY 73-4506) SDF
Molecular Weight (MW) 482.82
Formula

C21H15ClF4N4O3

CAS No. 755037-03-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms Fluoro-Sorafenib
Solubility (25°C) * In vitro DMSO 97 mg/mL (200.9 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea

Customer Product Validation (1)


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Source J Cell Physiol, 2015, 230(9): 2281-98. Regorafenib (BAY 73-4506) purchased from Selleck
Method Trypan Blue & Live/Dead Assays
Cell Lines Hepatoma cells
Concentrations 0.5 µM
Incubation Time 24 h
Results Sildenafil interacted with regorafenib to kill hepatoma cells, regardless of whether the tumor cell expressed CD95.

Product Use Citation (10)

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