Regorafenib (BAY 73-4506)

Catalog No.S1178

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.

Price Stock Quantity  
USD 168 In stock
USD 120 In stock
USD 210 In stock
USD 470 In stock
USD 970 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Regorafenib (BAY 73-4506) Chemical Structure

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

Validation & Quality Control

1 customer reviews :

Quality Control & MSDS

Related Compound Libraries

VEGFR Inhibitors with Unique Features

Product Information

  • Compare VEGFR Inhibitors
    Compare VEGFR Products
  • Research Area

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)

 View  More

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
Hep3BMnLaRZBweHSxc3nzJGF{e2G7NYjY[Y55OeLCk{ZCpO69VQ>?MmHDOFghcA>?MkfnbY5pcWKrdIOgZ4VtdCCpcn;3eIg>NHfWNo4zPjN{OU[wPC=>
PLC/PRF/5 NVq4UG9iSXCxcITvd4l{KEG|c3H5NVvx[2REOeLCk{ZCpO69VQ>?MVy0PEBpMm\wbY5pcWKrdIOgZ4VtdCCpcn;3eIg>NIO5TJgzPjN{OU[wPC=>
HepG2 MmTsRZBweHSxc3nzJGF{e2G7MUWx5qCUPcLizszNMWS0PEBpNGfQPI5qdmirYnn0d{Bk\WyuIHfyc5d1cA>?NFjnbJczPjN{OU[wPC=>
HEK293NVXZOZpLTnWwY4Tpc44hSXO|YYm=NHfzO|UxNjYkgJpOwG0>NFLsZmUzNzRxNjDoNVTZelJFemWmdXPld{BIWlB5ODDlfJBz\XO|aX;uM1SzXVI2QDV6MEOy
GEOMXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2myXFAvODFvMkCg{txOM4njRlk3KGh?MX\EUXNQNFS0WIRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?NULCUINPOjV6M{izPVE>
SW48NFHZWlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M4[xTlAvODFvMkCg{txOM3jiUlk3KGh?NYnSfm17TE2VTx?=NFnhXIVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?NHTOS2QzPTh|OEO5NS=>
HT29NXvWc5M1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MnfTNE4xOS1{MDFOwG0>NH3K[4Q6PiCqM13CZWROW09?M3TzVolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzMo\ONlU5Ozh|OUG=
SW480M1\RNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M33LW|AvODFvMkCg{txONYS3NGZFQTZiaB?=NUHz[JVmTE2VTx?=NWL1bmhncW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?M3fKUFI2QDN6M{mx
SW620NEPQ[XBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NV;rWIxjOC5yMT2yNEDPxE1?NH\PUIs6PiCqMX\EUXNQM2DIbYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzM1LJZ|I2QDN6M{mx
HCT116MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M1nUe|AvODFvMkCg{txONUTaclVvQTZiaB?=M{C0U2ROW09?NUfIbY5xcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?NWm0U5hZOjV6M{izPVE>
LOVONGjIdWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Mon0NE4xOS1{MDFOwG0>NEHpZ5U6PiCqNES3NVVFVVORMV7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>NXn1VmFNOjV6M{izPVE>
HCT150NGftXYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NU\MSVJlOC5yMT2yNEDPxE1?MVe5OkBpMkfzSG1UVw>?NVvEcFRMcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?Mke5NlU5Ozh|OUG=
SW48-CRNUXXSJFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mn3jNE4xOS1{MDFOwG0>NGTtd3M6PiCqM3zrZmROW09?M3L4c4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzMnnkNlU5Ozh|OUG=
GEO-CRNVPEPWVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MXywMlAyNTJyIN88US=>MVW5OkBpMm\6SG1UVw>?M3HWT4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzMXyyOVg{QDN7MR?=
KB-31NEnqc5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NVfMT49sUUN3ME21MlXDuTBwMzDuUS=>NG\2W|kzPTd3M{O2NS=>
KB-G2NXrESmJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3vqPWlEPTB;OT6xxtExNjFibl2=MmHmNlU4PTN|NkG=
LLC-PK1M4fscWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NGPaSGJKSzVyPUSyMlDDuTNwMjDuUS=>NFH4NHUzPTd3M{O2NS=>
LLC-PK1/MRP2MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2m3VmlEPTB;OEKuOOKyOi55IH7NM1TZOFI2PzV|M{[x
HEK293MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MX3JR|UxRTFzLkFCtVEvOiCwTR?=M{XuSlI2PzV|M{[x
HEK293/OATP1B1M1:w[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NWLtN|J6UUN3ME22MlLDuTBwMzDuUS=>MlTENlU4PTN|NkG=
HROC18Mm\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M4LYZWlEPTB;MT6zJO69VQ>?NXjOVGJROjV|MEm5NVQ>
HROC24MlHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2XQTmlEPTB;ND62JO69VQ>?M365RVI2OzB7OUG0
HROC43Mnu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NF;PdItKSzVyPUWuN{DPxE1?MknoNlU{ODl7MUS=
HROC46M3XUUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NEnBUm1KSzVyPUKuOEDPxE1?NH;lOnMzPTNyOUmxOC=>
RJ345NFK2RZZHfW6ldHnvckBCe3OjeR?=M{j6TFAvPS93IN88US=>NGX5dIkzPCCqMl\4SG1UVw>?NXznNVVKcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9vMW[yOVI2Ozl7NB?=
RJ348MnLaSpVv[3Srb36gRZN{[Xl?NYX3[FFqOC53L{Wg{txONYnWWJJ{OjRiaB?=M1fNcWROW09?NYfL[W9ucW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9vNVm3UolGOjV{NUO5PVQ>
MCF-7MlToSpVv[3Srb36gRZN{[Xl?M3\zTFAvPS93IN88US=>MVuyOEBpNVnCXoQ2TE2VTx?=MmHybY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;uM3LLWlI2OjV|OUm0
MDA-MB-231NFnsU|dHfW6ldHnvckBCe3OjeR?=NX[4bldZOC53L{Wg{txOM2q0VFI1KGh?NYLpTo5RTE2VTx?=MkLVbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;uMlS4NlUzPTN7OUS=
HT15Mk\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MVKxMVIxKM7:TR?=MmD5OFghcA>?M371[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzMYGyOVA4OTBzOB?=
DLD1M1HHdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M122eFEuOjBizszNMWm0PEBpM1jmeIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzNEPNUnozPTB5MUCxPC=>
HT-29NXe0bJdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MXuxMVIxKM7:TR?=M2rIWVQ5KGh?MVzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>NHy4TmszPTB5MUCxPC=>
Hct-116MlfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NXrWVGhkOS1{MDFOwG0>MYq0PEBpMXvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>NVfSNZNNOjVyN{GwNVg>
HT15M3XZemFxd3C2b4Ppd{BCe3OjeR?=NVjlcnl5OS1zMDFOwG0>MUW0PEBpNYe5N4R[cW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzMmXqNlUxPzFyMUi=
DLD1MkTkRZBweHSxc3nzJGF{e2G7M1W3S|EuOTBizszNMnX2OFghcA>?NY[5XYRNcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzNIrJW3IzPTB5MUCxPC=>
HT-29NEj2e45CeG:ydH;zbZMhSXO|YYm=MXqxMVExKM7:TR?=NYrXWHpEPDhiaB?=M4PLV4lv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>MlTUNlUxPzFyMUi=
Hct-116MVvBdI9xfG:|aYOgRZN{[Xl?M3e1R|EuOTBizszNMYS0PEBpNX7Ic4hIcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVzMl;WNlUxPzFyMUi=
GBM5M{\qVGFxd3C2b4Ppd{BCe3OjeR?=NX7ne5hyOC534pETNU4x6oDLzszNNYHKfoRXOjRiaB?=NFTDeGFFVVORM{X3ZYlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=>M2ryXFI1QTFzMkG1
GBM6MoPzRZBweHSxc3nzJGF{e2G7NGm3VHcxNjYkgKOxMlDjiIoQvF2=Ml2yNlQhcA>?NHPRV4RFVVORMkDYbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYToMVeyOFkyOTJzNR?=
GBM12NXjC[2plSXCxcITvd4l{KEG|c3H5MXKwMlXjiJNzLkFihKnPxE1?M1zF[|I1KGh?MX;EUXNQNXGzUphQcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRpNE\UPVUzPDlzMUKxOS=>
GBM14 M4e0RmFxd3C2b4Ppd{BCe3OjeR?=NYfsfZJqOC534pETNU4x6oDLzszNM3XsO|I1KGh?MYrEUXNQNHT6e2JqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg>MmLZNlQ6OTF{MUW=
Hep3BNXXnRpZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MUmx5qCUOi53wrFOwG0>M2jSOlI1NzR6L{eyJIg>NELWOWxqdmirYnn0d{Bk\WyuIHfyc5d1cA>?NFqyfG4zPDh6NUi5NC=>
PLC/PRF/5 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mn36NgKBmzJwNdMg{txOM3q2c|I1NzR6L{eyJIg>NI\EZpFqdmirYnn0d{Bk\WyuIHfyc5d1cA>?NGrJW2UzPDh6NUi5NC=>
HepG2 NVLve3k{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVWx5qCUOi53wrFOwG0>MnL6NlQwPDhxN{KgbC=>NV3xN2FFcW6qaXLpeJMh[2WubDDndo94fGh?MWGyOFg5PTh7MB?=
HCT116 MU\GeY5kfGmxbjDBd5NigQ>?MU[xNE8zOC92MDFOwG0>M4n6XlI1KGh?MnLwbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIH3SUmEh\XiycnXzd4lwdiCrbjDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XJ?M{\T[FI1PzZ|NkGx
Lim2405M4LUZWZ2dmO2aX;uJGF{e2G7NUHOXZR6PDBizszNMUiyOEBpMlLWbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{NX3qUXpWOjR5NkO2NVE>
LoVoM3npTGZ2dmO2aX;uJGF{e2G7MlT4OFAh|ryPMWmyOEBpNXTjW3J4cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m|NHuyN20zPDd4M{[xNS=>
Lim1215M1X5[WZ2dmO2aX;uJGF{e2G7M4LNTVQxKM7:TR?=M1y1WVI1KGh?M4jUVIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>?MkDONlQ4PjN4MUG=
SW48NULBcolMTnWwY4Tpc44hSXO|YYm=NIHYOnY1OCEQvF2=NFzmXJIzPCCqM2LJUIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>?MYiyOFc3OzZzMR?=
RKO MnHTSpVv[3Srb36gRZN{[Xl?NWLJT2c6PDBizszNMkjMNlQhcA>?M3;DV4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>?MWKyOFc3OzZzMR?=
SW837Mn[0SpVv[3Srb36gRZN{[Xl?Mm\WOFAh|ryPNFXzN28zPCCqNE\wbW1qdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?Ml\6NlQ4PjN4MUG=
SW1463M2HUO2Z2dmO2aX;uJGF{e2G7MojaOFAh|ryPMoj5NlQhcA>?M4ja[Ilv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>?MVKyOFc3OzZzMR?=
SW480NFXQU|VHfW6ldHnvckBCe3OjeR?=NHvXPHM1OCEQvF2=M3XBW|I1KGh?NXnsZ2kycW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m|MX:yOFc3OzZzMR?=
Vaco432M3fEc2Z2dmO2aX;uJGF{e2G7Ml7tOFAh|ryPNV3pTmtDOjRiaB?=MVfpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM>NIDud2YzPDd4M{[xNS=>
Vaco400NHO3XVlHfW6ldHnvckBCe3OjeR?=NID0[lU1OCEQvF2=MkPvNlQhcA>?M{Lufolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>?NF7tRpIzPDd4M{[xNS=>
DLD1NGTORVRHfW6ldHnvckBCe3OjeR?=NHvDTJE1OCEQvF2=M4HFZlI1KGh?MnnMbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{M4rl[lI1PzZ|NkGx
HT29 M{nPSmZ2dmO2aX;uJGF{e2G7M{fle|QxKM7:TR?=NVnDfJNtOjRiaB?=MmTLbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{M3y1SlI1PzZ|NkGx
PLC/PRF/5 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NITZNG0y6oDVNdM1US=>MWmyOE81QC95MjDoM4TLTYlvcGmkaYTzJINmdGxiZ4Lve5RpNYi0TFM{OjNzNkmxOFg>
HepG2Ml;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NITlNWgy6oDVNdM1US=>M17VZlI1NzR6L{eyJIg>Mo\HbY5pcWKrdIOgZ4VtdCCpcn;3eIg>M4rLcFI{OTZ7MUS4
Hep3B NWLzZoZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NH3HeJMy6oDVNdM1US=>MkTuNlQwPDhxN{KgbC=>M{fa[YlvcGmkaYTzJINmdGxiZ4Lve5RpMnvLNlMyPjlzNEi=

... 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.

view more

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02835924 Not yet recruiting Metastatic Colorectal Cancer Spanish Cooperative Group for the Treatment of Digestive  ...more Spanish Cooperative Group for the Treatment of Digestive Tumours (TTD)|Bayer July 2016 Phase 2
NCT02795156 Not yet recruiting Non-small Cell Lung Carcinoma|Urothelial Carcinoma|Gastrointestinal Carcinoma, Non-colon|Upper Aerodigestive Tract Carcinoma SCRI Development Innovations, LLC|Foundation Medicine|Boe  ...more SCRI Development Innovations, LLC|Foundation Medicine|Boehringer Ingelheim|Bayer July 2016 Phase 2
NCT02664077 Recruiting Stage III (IIIB or IIIC) Colon Cancer NSABP Foundation Inc|Bayer June 2016 Phase 3
NCT02383433 Recruiting Metastatic Pancreatic Adenocarcinoma Case Comprehensive Cancer Center|National Cancer Institut  ...more Case Comprehensive Cancer Center|National Cancer Institute (NCI) June 2016 Phase 2
NCT02773524 Not yet recruiting Gastro-Oesophageal Cancer Australasian Gastro-Intestinal Trials Group|Canadian Canc  ...more Australasian Gastro-Intestinal Trials Group|Canadian Cancer Trials Group June 2016 Phase 3

view more

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
2 years -80℃in solvent
Synonyms Fluoro-Sorafenib
Solubility (25°C) * In vitro DMSO 97 mg/mL (200.9 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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

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.

Tel: +1-832-582-8158 Ext:3

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

* Indicates a Required Field

Related VEGFR Products

  • SU5402

    SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.

  • Erlotinib

    Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  • R428 (BGB324)

    R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).

  • Axitinib

    Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.

    Features:Superior as second-line therapy relative to sorafenib (current standard-of-care).

  • Cabozantinib (XL184, BMS-907351)

    Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively.

  • Nintedanib (BIBF 1120)

    Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.

  • Vandetanib (ZD6474)

    Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay.

  • Lenvatinib (E7080)

    Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Phase 3.

  • Pazopanib

    Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.

  • Pazopanib HCl (GW786034 HCl)

    Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.

    Features:A multi-kinase inhibitor.

Recently Viewed Items

Tags: buy Regorafenib (BAY 73-4506) | Regorafenib (BAY 73-4506) ic50 | Regorafenib (BAY 73-4506) price | Regorafenib (BAY 73-4506) cost | Regorafenib (BAY 73-4506) solubility dmso | Regorafenib (BAY 73-4506) purchase | Regorafenib (BAY 73-4506) manufacturer | Regorafenib (BAY 73-4506) research buy | Regorafenib (BAY 73-4506) order | Regorafenib (BAY 73-4506) mouse | Regorafenib (BAY 73-4506) chemical structure | Regorafenib (BAY 73-4506) mw | Regorafenib (BAY 73-4506) molecular weight | Regorafenib (BAY 73-4506) datasheet | Regorafenib (BAY 73-4506) supplier | Regorafenib (BAY 73-4506) in vitro | Regorafenib (BAY 73-4506) cell line | Regorafenib (BAY 73-4506) concentration | Regorafenib (BAY 73-4506) nmr
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us