Bortezomib (PS-341) 化学構造
分子量: 384.24

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MSDS

製品説明

  • Compare Proteasome Inhibitors
    Proteasome製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Bortezomib (PS-341)は、強力なプロテアソーム阻害剤で、Kiが0.6nMです。
ターゲット

20S proteasome

IC50

0.6 nM (Ki) [1]

In vitro試験 Bortezomib, a boronic acid dipeptide, is a highly selective, reversible inhibitor of the 26S proteasome which primarily functions in the degradation of mis-folded proteins and is essential for the regulation of the cell cycle. Exposure to Bortezomib has been shown to stabilize p21, p27, and p53, as well as the proapoptotic Bid and Bax proteins, caveolin-1, and inhibitor κB-α, which prevents activation of nuclear factor κB-induced cell survival pathways. Bortezomib also promotes the activation of the proapoptotic c-Jun-NH2 terminal kinase, as well as the endoplasmic reticulum stress response. Alteration of the levels of these cellular proteins leads to inhibition of proliferation, migration, and promotion of apoptosis of cancer cells. [2] Bortezomib is shown to penetrate into cells and inhibit proteasome-mediated intracellular proteolysis of long-lived proteins with a concentration that inhibits 50% of the proteolysis of ∼0.1 μM. The average growth inhibition of 50% value for Bortezomib across the entire panel of 60 cancer cell lines derived from multiple human tumors from the US National Cancer Institute (NCI) is 7 nM. Treatment of PC-3 cells with Bortezomib (100 nM) for 8 h results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1. Bortezomib kills PC-3 cells at 24 and 48 hr with IC50 of 100 and 20 nM, respectively. Bortezomib induces nuclear condensation at 16–24 hr after treatment. Bortezomib treatment leads to PARP cleavage in a time-dependent manner with concentrations as low as 100 nM being effective at 24 hr. [1]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MCF-7 MVXDfZRwfG:6aXOgRZN{[Xl? NVPOTpdqPTBizszN MnP2OFghcA>? NW\vdpFSTE2VTx?= NIrRUWxMcWyuczDj[YxteyCkeTDtc5JmKHSqYX6gPVkm NIDnNZcyODR7OU[0Ny=>
OVCA 429 Mn6wSpVv[3Srb36gRZN{[Xl? NGjKfIY{ODBibl2= M1jvR|Q5KGh? NFnF[ldFVVOR NHH6ZmdFcXO{dYD0d{BqdnSjY4SgcZVtfGmlZXzseYxieiC2dX3vdkB{eGincn;p[JM> Mn7zNVA6QTl5Nk[=
RPMI8226 NXHqdHA{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HUcVExOCCwTR?= MonYOFghcA>? M4HPdGROW09? MoT2TWM2OD1|MDDuUS=> MWexNVMxPjR6OR?=
Dox40 NIrKT41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYixNFAhdk1? NXzvN4x[PDhiaB?= MmHGSG1UVw>? NXe3fWRTUUN3ME20NEBvVQ>? NG\pd2YyOTNyNkS4PS=>
MR20 Moe5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfVZ404OTByIH7N M33SUVQ5KGh? MnT0SG1UVw>? Mlm4TWM2OD1{MDDuUS=> MVqxNVMxPjR6OR?=
LR5 NFvDcGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX:xNFAhdk1? NWTaXHpFPDhiaB?= MWHEUXNQ Mo\JTWM2OD1{MDDuUS=> MUGxNVMxPjR6OR?=
U266 MoH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXL1XVVNOTByIH7N NHzWcpA1QCCq NFP1bXNFVVOR MkXnTWM2OD1|IH7N MXOxNVMxPjR6OR?=
IM-9 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDsR2cyODBibl2= MnLiOFghcA>? MWPEUXNQ M{HDZ2lEPTB;NjDuUS=> NVLWfYJuOTF|ME[0PFk>
Hs Sultan MonSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3GyWVExOCCwTR?= MVG0PEBp NFP4TlRFVVOR M3rCUWlEPTB;MkCgcm0> M3f2dFEyOzB4NEi5
PAM-LY2 NV\JOFQ1TnWwY4Tpc44hSXO|YYm= Mn7WNVAxKG6P M2X6e|EzKGh? MVnEUXNQ MmDDTY5pcWKrdIOgUmYu|rqEIHHjeIl3[XSrb36= M3nqXlEyOzVyOUGz
PAM 212 NVvhVWhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIW1[GkyODBibl2= MYK3NkBp NIO1fYtFVVOR NYniV4ZSUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= M4[yZVEyOzVyOUGz
PAM-LY2 NGXseJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\aNVAxKG6P MlrkO|IhcA>? MlHJSG1UVw>? MonrTY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? Ml7zNVE{PTB7MUO=
B4B8 NEnoNYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFyxWW4yODBibl2= NWXPTZRMPzJiaB?= MkHDSG1UVw>? MonNTY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? NF\nU3EyOTN3MEmxNy=>
B7E3 NWXJSpoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzwU4EyODBibl2= MmjuO|IhcA>? MUHEUXNQ Mlv6TY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? M{jLU|EyOzVyOUGz
UM-SCC-9 NXu4RVhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOxNFAhdk1? MWK3NkBp MXTEUXNQ M1j2V2lvcGmkaYTzJINmdGxidnnhZoltcXS7 NI\4dGMyOTN3MEmxNy=>
UM-SCC-11B NUfIVXlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjIVJlrOTByIH7N MofnO|IhcA>? NWLFSW85TE2VTx?= NH;O[IpKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= NGG0R2QyOTN3MEmxNy=>
H460 M17CbmZ2dmO2aX;uJGF{e2G7 MWexNEDPxE1? M2DvVVI1KGh? NXnVbXh4TE2VTx?= NXvnUVAzUW6mdXPld{BD[2xvMjDwbI9{eGixconsZZRqd25iYX7kJINt\WG4YXflJINwenKnbHH0[YQhf2m2aDDHNk1OKHCqYYPlJIFzemW|dB?= MVmxNlQ6OjFzNx?=
U266 NFmzRWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\VOVAxKG6pL33s M4ixPVQ5KGh? M2fVeWROW09? NGiyW3ZKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NEnnc28yOjZ|MU[xPS=>
ARH77 NWTycJBLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXYV5ZnPTByIH7nM41t M2rtW|Q5KGh? MmHKSG1UVw>? MoLvTY5pcWKrdIOgZ4VtdCCpcn;3eIg> NXzpcIpYOTJ4M{G2NVk>
WAD-1 NX;U[YZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV21NFAhdmdxbXy= M{HJT|Q5KGh? Ml;0SG1UVw>? NIHLSodKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NUfMNmRmOTJ4M{G2NVk>
U266/LR7 M13YU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX21NFAhdmdxbXy= M3T2XFQ5KGh? MWXEUXNQ NEC3[4lKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NIDETWsyOjZ|MU[xPS=>
U266/dox4 NE\TTItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fEclUxOCCwZz;tcC=> MVe0PEBp NY\VbIw6TE2VTx?= MXfJcohq[mm2czDj[YxtKGe{b4f0bC=> Mnj4NVI3OzF4MUm=
RPMI8226/LR5 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPYUIF[PTByIH7nM41t NV7F[nVyPDhiaB?= MkfNSG1UVw>? M3OxZ2lvcGmkaYTzJINmdGxiZ4Lve5Rp M1XIelEzPjNzNkG5
H460 NWjtN3VOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moj6NVAh|ryP Mkf3O|IhcA>? Mnf4SG1UVw>? NYXDVIg4UUN3ME2xNFAhdk1? MlXVNVI3OzF4MkC=
H358 M4K1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXGxNEDPxE1? NGO0Npg4OiCq NH3DeVRFVVOR M2\pWWlEPTB;N{Cgcm0> MmTBNVI3OzF4MkC=
H322 M1T0TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fmZVExKM7:TR?= NUn3UXdSPzJiaB?= MmHISG1UVw>? NEPyRWtKSzVyPU[yNEBvVQ>? Mo\YNVI3OzF4MkC=
H460 MUjGeY5kfGmxbjDBd5NigQ>? NFzHOVMyODBibl2= NUK2U2JjOjRiaB?= NIX0WpFFVVOR MUHJcoR2[2W|IFeyMW0ueGijc3WgZZJz\XO2IHHu[EB1fWK3bHnuJIF{e2WvYnz5MYRqe2G|c3XtZox6 NITUPI0yOjZ|MU[yNC=>
LNCap-Pro5 MormSpVv[3Srb36gRZN{[Xl? MUixJO69VQ>? M4XtR|QhcA>? NGfQe2pFVVOR NHi0XldUfGGkaXzpfoV{KHB3Mx?= MlrGNVQ3OTJ3M{K=
T29 M4\LUmFxd3C2b4Ppd{BCe3OjeR?= MXS1NEBvVQ>? M1fOTFQ5KGhi MorMSG1UVw>? NUHkTWJ2UW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NHG4bYEyPjd5OEG3PS=>
T29Kt1 MULBdI9xfG:|aYOgRZN{[Xl? MYS1NEBvVQ>? MXi0PEBpKA>? NXPCfFZNTE2VTx?= MVTJcoR2[2W|IHPlcIwh[XCxcITvd4l{ NXnjR4JFOTZ5N{ixO|k>
HCT116 MmjBRZBweHSxc3nzJGF{e2G7 NXzteoZrPTBibl2= M{P3OFQ5KGhi M4\rSWROW09? MnjETY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MnfRNVY4PzhzN{m=
HKe-3 NIPufodCeG:ydH;zbZMhSXO|YYm= NGe4U|c2OCCwTR?= M2XPTVQ5KGhi M4DzSGROW09? NF;JbolKdmS3Y3XzJINmdGxiYYDvdJRwe2m| NHzkd28yPjd5OEG3PS=>
NB-1691 M{KzfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:xJO69VQ>? Ml7OO|IhcA>? NYDTbmFOUW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKHSxIEWl MkPrNVc3QDl4OES=
CHLA-255 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XyNVEh|ryP MnLWO|IhcA>? NGfsbpJKdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44hfG9iMjW= MXuxO|Y5QTZ6NB?=
SK-N-AS Ml3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorONUDPxE1? MlvVO|IhcA>? NV\oOJc2UW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKHSxIEGwKS=> NEHNVmQyPzZ6OU[4OC=>
NB-1691 NULqdmVTTnWwY4Tpc44hSXO|YYm= M4naclExKG6P M3;6PFI1KGh? MWPTbYdvcW[rY3HueIx6KHKnZIXj[ZMh[2WubIOgbY4hfGinIFewM2cyKHCqYYPl M2rleFE4Pjh7Nki0
CHLA-255 NHT6TlJHfW6ldHnvckBCe3OjeR?= NGe3W|cyOCCwTR?= M1X5SFI1KGh? NXLsVGVkVW:mZYP0cJkhemWmdXPld{Bk\WyuczDpckB1cGViR{CvS|EheGijc3W= M3\telE4Pjh7Nki0
RPMI 8226 NXrQT5FqTnWwY4Tpc44hSXO|YYm= M1jYR|IxKG6P NEj6Xos5KGh? MXjTbYdvcW[rY3HueIx6KGWwaHHuZ4V{KE6ILd86RkBi[3Srdnn0fS=> M2fQeVE6PDN4MEWw
MM.1S M2rCfWZ2dmO2aX;uJGF{e2G7 NETKbFgzOCCwTR?= NFjVVXY5KGh? MXrTbYdvcW[rY3HueIx6KGWwaHHuZ4V{KE6ILd86RkBi[3Srdnn0fS=> MlnmNVk1OzZyNUC=
U266 MonHSpVv[3Srb36gRZN{[Xl? MnTBNlAhdk1? NXPwfIVZQCCq M2[3WHNq\26rZnnjZY51dHliZX7oZY5k\XNiTl[t{tpDKGGldHn2bZR6 Mnm5NVk1OzZyNUC=
OPM1 NVXIfFBxTnWwY4Tpc44hSXO|YYm= M3zxN|IxKG6P NXrXXppuQCCq NFjofotUcWewaX\pZ4FvfGy7IHXubIFv[2W|IF7GMe67SiCjY4Tpeol1gQ>? MXmxPVQ{PjB3MB?=
INA6 NWfX[WxvTnWwY4Tpc44hSXO|YYm= NUnDUoRsOjBibl2= NX\DTnFrQCCq MlWzV4lodmmoaXPhcpRtgSCnbnjhcoNmeyCQRj5OvmIh[WO2aY\peJk> M4fRdFE6PDN4MEWw
OPM2 MXLGeY5kfGmxbjDBd5NigQ>? M2foZlIxKG6P MojSPEBp MnXBV4lodmmoaXPhcpRtgSCnbnjhcoNmeyCQRj5OvmIh[WO2aY\peJk> NU\wcY1VOTl2M{[wOVA>
RPMI 8226 MVnGeY5kfGmxbjDBd5NigQ>? MVGyNEBvVQ>? Mof3PEBp MWnJcoR2[2W|IFTORUB{gW62aHXzbZM> NYLkPGVLOTl2M{[wOVA>
BaF/3 M2Tidmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTkNVAxKG6P NHLCOWQ1QCCq M1X6UmlEPTB;Nj6yJI5O MnizNlA{ODV4OUK=
BaF/3-p210 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWixNFAhdk1? M{DpcFQ5KGh? NF[4WGNKSzVyPUSuO{BvVQ>? MWOyNFMxPTZ7Mh?=
TCC-S NH\RVINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DCVlExOCCwTR?= M3vSVlQ5KGh? M1L1b2lEPTB;Mj64JI5O M{jLS|IxOzB3Nkmy
BaF/3 NInnXFlHfW6ldHnvckBCe3OjeR?= MUG2JI5O MWe0PEBp MU\JcoR2[2W|IHGg[5Jm[XRiR{GgZ4VtdC2leXPs[UBienKnc4S= M4H1dVIxOzB3Nkmy
BaF/3-p210 NWqxO4pzTnWwY4Tpc44hSXO|YYm= NXu0dnN{PiCwTR?= NFv6Ro01QCCq NWjGc3hJUW6mdXPld{BiKHOuaXfoeEBIOSClZXzsMYN6[2ynIHHydoV{fA>? MYWyNFMxPTZ7Mh?=
BaF/3-p210 NY\OVXBSTnWwY4Tpc44hSXO|YYm= M3zIW|Yhdk1? M4PRNFI1KGh? NXrTVItGWmWmdXPld{B1cGVicHjvd5Bpd3K7bHH0bY9vKGGwZDD0bIUh[WO2aY\peJkhd2ZiUnK= NF;6[JEzODNyNU[5Ni=>
Raji NX\0Wo1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDGNUDPxE1? M1uwPFI1KGh? NFTEWHhT\WS3Y3XzJINmdGxidnnhZoltcXS7wrC= M{nrfFIyOTdyOUi4
LCL-1 NHy3UWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3r2[lEh|ryP MXSyOEBp MVPS[YR2[2W|IHPlcIwhfmmjYnnsbZR6yqB? MWeyNVE4ODl6OB?=
LCL-2 MlLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlX1NUDPxE1? MoLkNlQhcA>? MnfLVoVlfWOnczDj[YxtKH[rYXLpcIl1gcLi Mnj3NlEyPzB7OEi=
BJAB NHrq[VBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnYVGwyKM7:TR?= MX2yOEBp MnPOVoVlfWOnczDj[YxtKH[rYXLpcIl1gcLi M3:yWFIyOTdyOUi4
SNT-13 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PEVFEh|ryP MnLYNlQhcA>? NH3KR3FT\WS3Y3XzJINmdGxidnnhZoltcXS7wrC= M1rpSlIyOTdyOUi4
SNT-16 MkfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvRNXkyKM7:TR?= NXjKWnV1OjRiaB?= Mnn5VoVlfWOnczDj[YxtKH[rYXLpcIl1gcLi M1nUTFIyOTdyOUi4
Jurkat M2DPNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoP3NUDPxE1? Mm\GNlQhcA>? NEH3V|BT\WS3Y3XzJINmdGxidnnhZoltcXS7wrC= NHi0bGgzOTF5MEm4PC=>
KAI-3 NIDsZ5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{j1fFEh|ryP M1LtU|I1KGh? NEe0R2FT\WS3Y3XzJINmdGxidnnhZoltcXS7wrC= NEn0UXQzOTF5MEm4PC=>
SNK-6 MonzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DGeVEh|ryP MorwNlQhcA>? NVjtSGVTWmWmdXPld{Bk\WyuII\pZYJqdGm2edMg Mn3qNlEyPzB7OEi=
KHYG-1 NYjuPGtnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXz5UFdFOSEQvF2= M{jsSFI1KGh? MoT6VoVlfWOnczDj[YxtKH[rYXLpcIl1gcLi MV2yNVE4ODl6OB?=
SNT-16 NFvzRYRCeG:ydH;zbZMhSXO|YYm= NGjCd24yKM7:TR?= NGPmd|I3KGh? MVHJcoR2[2W|IHPlcIwh[XCxcITvd4l{ NGPnZnAzOTF5MEm4PC=>
Jurkat M4G2N2Fxd3C2b4Ppd{BCe3OjeR?= MnPmNUDPxE1? NFv2[Jg3KGh? MVLJcoR2[2W|IHPlcIwh[XCxcITvd4l{ Mo\BNlEyPzB7OEi=
KAI-3 M4jkbmFxd3C2b4Ppd{BCe3OjeR?= Mm\mNUDPxE1? MYG2JIg> MV\JcoR2[2W|IHPlcIwh[XCxcITvd4l{ NHPlfVkzOTF5MEm4PC=>
KHYG-1 NIXSUotCeG:ydH;zbZMhSXO|YYm= NV\ETI5XOSEQvF2= MV:2JIg> NHP0TpZKdmS3Y3XzJINmdGxiYYDvdJRwe2m| NI\KdJMzOTF5MEm4PC=>
SNT-13 M2jXZ2FvfGm4aYLhcEBCe3OjeR?= NX6zSnRpOSEQvF2= Mnf6NlQhcA>? MVjJcoR2[2W|IHz5eIlkKGmwZnXjeIlwdiCxZjDFRnY> NUnWRpdwOjFzN{C5PFg>
SNT-16 M2LsWGFvfGm4aYLhcEBCe3OjeR?= Ml\MNUDPxE1? NV;3bpBlOjRiaB?= NEXFZ3lKdmS3Y3XzJIx6fGmlIHnu[oVkfGmxbjDv[kBGSlZ? MnLvNlEyPzB7OEi=
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SNK-6 MnG1RY51cX[rcnHsJGF{e2G7 NEjETXUyKM7:TR?= Mk[3NlQhcA>? NUTKU5R1UW6mdXPld{BtgXSrYzDpcoZm[3Srb36gc4YhTUKY M3fVZlIyOTdyOUi4
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BLM MVnBdI9xfG:|aYOgRZN{[Xl? M1[zZ|ExKG6P M1L0dlI1KGh? Mnu5TY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NFO0d4szOzB5OUC4Ny=>
A375 MoPyRZV1d3CqYXf5JGF{e2G7 NI\rOXQyOCCwTR?= NXLkRlRROTJiaB?= NX32OoQ3UW6mdXPld{Bnd3KvYYTpc44hd2ZiYYX0c5Bp[Wexc3;t[ZM> M3XIcVI{ODd7MEiz
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H1299 M3qwR2Fxd3C2b4Ppd{BCe3OjeR?= NYTmOIJKQDBibl2= MVWyOEBp NWToU3E5TE2VTx?= M1TBNHNmdnOrdHn6[ZMhVlOFTFOgZ4VtdHNidH:gUXNENWSncnn2[YQhcUN7LXnu[JVk\WRiYYDvdJRwe2m| MnTsNlU{OjN4OUO=
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HH M1fDT2Z2dmO2aX;uJGF{e2G7 MkXmNVAxKG6P NFq5VG8zPCCq MYHEUXNQ M1vuVoRwf26{ZXf1cIF1\XNiVFfGMe6zOSCjbnSgTWwuOTJiZYjwdoV{e2mxbh?= M2S1clI2PjhzM{O1
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U937 MoWzSpVv[3Srb36gRZN{[Xl? NUDvWW5WOTByIH7N M3\nSlYhcA>? MYjJcoR2[2W|IFnMMVgh\XiycnXzd4lwdiCrbjDMVHMue3SrbYXsZZRm\CCXOUO3JI1i[3KxcHjh[4V{ MnPLNlU4QTF2N{e=
human PBMC MYTGeY5kfGmxbjDBd5NigQ>? M{PmclExOCCwTR?= M{jxflI1KGh? NYD0ZW8{UW6mdXPld{BKVC16IILlcIVie2V? NYPkd|hKOjV5OUG0O|c>
ES6 NHv5V|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nGWGlEPTB;MD6wNFIyKG6P MmG1V2FPT0WU
SK-UT-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHDWYdKSzVyPUCuNVY{KG6P MkXsV2FPT0WU
SH-4 NXTuOYh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3Wdo5KSzVyPUCuNVc{KG6P NHXqOHdUSU6JRWK=
TE-9 NVzvO|hjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnK1TWM2OD1yLkG4NkBvVQ>? MmjFV2FPT0WU
A253 NFXCeIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEi5RnFKSzVyPUCuNlA5KG6P MUTTRW5ITVJ?
no-10 NW\aVmNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULXSohFUUN3ME2wMlIyKG6P M1j0THNCVkeHUh?=
MMAC-SF MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHmyNWtKSzVyPUCuNlE3KG6P NWnHZmFFW0GQR1XS
A101D NUPKW2dQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;yc2VKSzVyPUCuNlI2KG6P MULTRW5ITVJ?
NTERA-S-cl-D1 NFmySYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTBwMkSzJI5O MXzTRW5ITVJ?
8-MG-BA NWjqNZMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXYTWM2OD1yLkK1JI5O M1rXeHNCVkeHUh?=
KNS-42 NFPW[2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoL1TWM2OD1yLkK1PEBvVQ>? NYLRSJMxW0GQR1XS
LXF-289 NVz1VGlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHzNmFHUUN3ME2wMlI3QSCwTR?= MnP1V2FPT0WU
OVCAR-4 NGrzU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVftfGJGUUN3ME2wMlI5QSCwTR?= NUXvdmh5W0GQR1XS
LOUCY MnXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{i3SmlEPTB;MD6yPVMhdk1? MkDJV2FPT0WU
BB65-RCC M{nl[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLwTWM2OD1yLkOwOEBvVQ>? NVntUmFrW0GQR1XS
D-542MG NIDxZ2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\DT|BKSzVyPUCuN|I6KG6P NETTXW5USU6JRWK=
ONS-76 NEnBO3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{C2ZmlEPTB;MD6zN{BvVQ>? M3L0UXNCVkeHUh?=
BB30-HNC M3T6fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwM{O1JI5O NXO5eIJKW0GQR1XS
KS-1 NWjvNlVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonNTWM2OD1yLkO0JI5O NYjoUHBTW0GQR1XS
A388 M3f0eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3BTWM2OD1yLkO1OkBvVQ>? MYHTRW5ITVJ?
ES8 MlriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7LSlZKSzVyPUCuOEBvVQ>? NECwfI1USU6JRWK=
MZ2-MEL MnS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\UTWM2OD1yLkSwO{BvVQ>? MYjTRW5ITVJ?
HCC2998 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHSTWM2OD1yLkSxNkBvVQ>? M1;aRXNCVkeHUh?=
D-247MG MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFO1fXhKSzVyPUCuOFE{KG6P NFiz[GJUSU6JRWK=
ACN MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTBwNEG3JI5O M{\XPHNCVkeHUh?=
LB2518-MEL NELObYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIC2bVdKSzVyPUCuOFI2KG6P MYHTRW5ITVJ?
ES1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTBwNEOgcm0> MVnTRW5ITVJ?
HCE-T Mmr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTBwNEO5JI5O Mk\qV2FPT0WU
OS-RC-2 NIDzUmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3mxT2lEPTB;MD60OEBvVQ>? MXrTRW5ITVJ?
MFH-ino MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HpeWlEPTB;MD60OFMhdk1? MojCV2FPT0WU
OCUB-M NYPqVGdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Hi[mlEPTB;MD60OFchdk1? NILVdXNUSU6JRWK=
CP66-MEL M1PPN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLveFlzUUN3ME2wMlQ4OyCwTR?= MorVV2FPT0WU
LB771-HNC NUTyfpNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\rTWM2OD1yLkS3OEBvVQ>? NIDS[GlUSU6JRWK=
DSH1 NHzLRWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvtVHRiUUN3ME2wMlQ5KG6P NHXNdIxUSU6JRWK=
HUTU-80 NFvOWpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvvTWM2OD1yLkWzN{BvVQ>? M1nIUXNCVkeHUh?=
CESS M{O1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfEcnJHUUN3ME2wMlU{QCCwTR?= NYrWO4diW0GQR1XS
NCI-H747 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHJXFhYUUN3ME2wMlU{QSCwTR?= MWnTRW5ITVJ?
HT-144 NGG4SmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojYTWM2OD1yLkW3OkBvVQ>? MVPTRW5ITVJ?
COLO-829 M3vIeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTBwNkG0JI5O M2\QN3NCVkeHUh?=
A4-Fuk MmjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmj6TWM2OD1yLk[yN{BvVQ>? Mn3EV2FPT0WU
GI-ME-N NIfrVYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTBwNkO0JI5O NV:xeGpmW0GQR1XS
LB831-BLC NUf1RW4{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVT1c3hsUUN3ME2wMlY1OSCwTR?= NYL3SYZJW0GQR1XS
HOP-62 NYXJNoxpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3SwdWlEPTB;MD62OFchdk1? M3LpbXNCVkeHUh?=
BB49-HNC NEnxWFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjYSZFtUUN3ME2wMlY2OiCwTR?= MVTTRW5ITVJ?
D-336MG NVvZN5IyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwNkW3JI5O NHHYXYdUSU6JRWK=
TK10 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTMPHNKSzVyPUCuOlc6KG6P M{[4fHNCVkeHUh?=
Ramos-2G6-4C10 M1;0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7iTWM2OD1yLk[5N{BvVQ>? NV3tSJJDW0GQR1XS
LB373-MEL-D MoPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwNzDuUS=> MU\TRW5ITVJ?
SF126 NX3S[GVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTBwN{CxJI5O NYTrVVRMW0GQR1XS
UACC-257 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTBwN{Ggcm0> NYPX[4hZW0GQR1XS
KINGS-1 NYnoUm57T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3T3UGlEPTB;MD63NlIhdk1? NWXLOWd1W0GQR1XS
LS-513 NXv2UpUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIGze5lKSzVyPUCuO|M6KG6P MWnTRW5ITVJ?
GI-1 NV3jd5FDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTpTWM2OD1yLke2OEBvVQ>? NX75PIVxW0GQR1XS
ES7 NUO1WGo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrofolKSzVyPUCuO|Y3KG6P NHK1OYFUSU6JRWK=
LB2241-RCC MnnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfaOXBKSzVyPUCuPFA1KG6P MYHTRW5ITVJ?
D-263MG M4PiVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfHTWM2OD1yLkiwO{BvVQ>? M3rUW3NCVkeHUh?=
SW684 MnX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTBwOEKxJI5O NXnvZmNlW0GQR1XS
ML-2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTBwOEKxJI5O MkXVV2FPT0WU
SK-LMS-1 M{TBemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXMN4FKSzVyPUCuPFU1KG6P M2\qeXNCVkeHUh?=
TE-5 M4\IVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn2wTWM2OD1yLki2OUBvVQ>? MWLTRW5ITVJ?
QIMR-WIL MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTBwOEi5JI5O MV3TRW5ITVJ?
NCI-H1355 M1O0W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4SxW2lEPTB;MD64PVUhdk1? M2[yNnNCVkeHUh?=
SNB75 M2\hXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zWNGlEPTB;MD65NVIhdk1? MnPGV2FPT0WU
RXF393 NWK5fpVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrFTWM2OD1yLkmxOEBvVQ>? NH7sVHdUSU6JRWK=
IST-MEL1 NEHJWppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDsenc6UUN3ME2wMlkyPyCwTR?= Mlq2V2FPT0WU
SF268 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfTTWM2OD1yLkmyN{BvVQ>? NXXSWWw2W0GQR1XS
KALS-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTBwOUK1JI5O NF6yPVNUSU6JRWK=
HC-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LSOWlEPTB;MD65O|Uhdk1? MkjnV2FPT0WU
SW872 NIDqbmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37LWGlEPTB;MD65PVYhdk1? MYrTRW5ITVJ?
PSN1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWSzZ2M4UUN3ME2xMlAyKG6P MoDzV2FPT0WU
TE-1 NXi1OZJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTFwMEOgcm0> NF\qTWZUSU6JRWK=
TE-10 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonmTWM2OD1zLkCzJI5O MV;TRW5ITVJ?
RKO MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTFwME[gcm0> NHXUb4JUSU6JRWK=
LC-2-ad NFnUT3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\qXoFVUUN3ME2xMlA5KG6P NHnmPVlUSU6JRWK=
SK-MM-2 MknPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HodWlEPTB;MT6wPUBvVQ>? MULTRW5ITVJ?
VA-ES-BJ NIPTUJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnhWJE1UUN3ME2xMlA6KG6P MkDMV2FPT0WU
MZ7-mel NEfabZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTFwMEmgcm0> MVXTRW5ITVJ?
D-392MG NEXoboVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFi3NJRKSzVyPUGuNUBvVQ>? MXrTRW5ITVJ?
CCRF-CEM M2LHXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\ETWM2OD1zLkGzJI5O MY\TRW5ITVJ?
EM-2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2GyfWlEPTB;MT6xOkBvVQ>? M3\zZnNCVkeHUh?=
HAL-01 M2P0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTFwMUigcm0> MX7TRW5ITVJ?
TE-8 NWq5bYxpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\IcmlEPTB;MT6xPUBvVQ>? M3T1NHNCVkeHUh?=
NCI-H1882 NHrIUHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLwcZZbUUN3ME2xMlIhdk1? MXHTRW5ITVJ?
Daudi MmHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnf2TWM2OD1zLkKyJI5O MojYV2FPT0WU
BL-41 M4PDSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrTTWM2OD1zLkK1JI5O M1\sW3NCVkeHUh?=
SR MlL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfoTWM2OD1zLkK1JI5O MoDMV2FPT0WU
KM12 NVLYWZViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;wZW9KSzVyPUGuNlchdk1? M{[xT3NCVkeHUh?=
K5 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTFwMkigcm0> MWDTRW5ITVJ?
A3-KAW NFq5SXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TkWGlEPTB;MT6yPEBvVQ>? M4TEeXNCVkeHUh?=
CMK Mk\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXteZZKSzVyPUGuNlkhdk1? M2Wwd3NCVkeHUh?=
Calu-6 M2Cyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zEZ2lEPTB;MT6yPUBvVQ>? NFrkZWtUSU6JRWK=
IST-SL2 NWjJXohGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzyeodKSzVyPUGuN|Ehdk1? NWXVXmt{W0GQR1XS
OPM-2 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmexTWM2OD1zLkOzJI5O MmDUV2FPT0WU
DU-4475 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTudXgyUUN3ME2xMlM3KG6P MnTpV2FPT0WU
ECC12 NEj5TlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTFwM{egcm0> MVnTRW5ITVJ?
L-540 M4TKSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjXVJhKSzVyPUGuN|chdk1? NUi0enBkW0GQR1XS
CAS-1 MornS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\yd5ZUUUN3ME2xMlM4KG6P M1X5OHNCVkeHUh?=
PF-382 M3rVcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPIUGNKSzVyPUGuOFchdk1? MUXTRW5ITVJ?
LS-411N NVq2bXc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTFwNUOgcm0> NHvpTJFUSU6JRWK=
NCI-H69 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHJOIVKSzVyPUGuOVQhdk1? MnzXV2FPT0WU
NB12 NF3rU4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTFwNU[gcm0> M{\aRXNCVkeHUh?=
HEL NYrJ[Yd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYC2e3hZUUN3ME2xMlYyKG6P MkHnV2FPT0WU
GCIY M1\x[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoSzTWM2OD1zLk[yJI5O NXXWV5B3W0GQR1XS
EHEB NIWwUVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rQUmlEPTB;MT62O{BvVQ>? NGm4eI5USU6JRWK=
TGBC1TKB NV\BOWh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M322cmlEPTB;MT63NUBvVQ>? MVfTRW5ITVJ?
KURAMOCHI MkKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTFwN{Kgcm0> NHfqZlNUSU6JRWK=
U-266 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTzTWM2OD1zLke2JI5O NWLkNJZzW0GQR1XS
LC4-1 NXX6WVJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M132O2lEPTB;MT63PUBvVQ>? NILsS4tUSU6JRWK=
NCI-H2126 NVrkPJlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\UXlNKSzVyPUGuPEBvVQ>? NF7hRohUSU6JRWK=
NCI-H1092 NW\Xe2N3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7UTWM2OD1zLkigcm0> MV3TRW5ITVJ?
GB-1 NVXsbot{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzVS3VKSzVyPUGuPFEhdk1? MXTTRW5ITVJ?
MV-4-11 NIDLN2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHlTWM2OD1zLkiyJI5O NFrMUoxUSU6JRWK=
Becker MlXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DYdWlEPTB;MT64N{BvVQ>? NGf4ZmNUSU6JRWK=
MPP-89 M{jtdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTFwOEmgcm0> NEfmfJpUSU6JRWK=
BE-13 Ml3US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzkTWM2OD1zLkmzJI5O MXPTRW5ITVJ?
697 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTFwOUmgcm0> MW\TRW5ITVJ?
NKM-1 M4jMU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkX2TWM2OD1{IH7N MYjTRW5ITVJ?
NB13 NXLIVoV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfMU|hQUUN3ME2yJI5O M1vZ[3NCVkeHUh?=
LS-123 M2nPSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXtbVFKSzVyPUKuNFIhdk1? NFXQ[olUSU6JRWK=
NB17 MoDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\RU2lEPTB;Mj6wOEBvVQ>? NF2zcW9USU6JRWK=
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... Click to View More Cell Line Experimental Data

In vivo試験 The anticancer effects of bortezomib as a single agent have been demonstrated in xenograft models of multiple myeloma, adult T-cell leukemia, lung, breast, prostate, pancreatic, head and neck, and colon cancer, and in melanoma. [2] Oral bortezomib 1.0 mg/ kg daily for 18 days causes tumor growth delays, as well as a decrease in the number of metastases in the Lewis lung cancer model. Bortezomib at a single dose of up to 5 mg/kg significantly decreased the surviving fraction of breast tumor cells. Bortezomib 1.0 mg/kg administrated weekly for 4 weeks reduces tumor growth by 60% in murine xenograft models of prostate cancer. 1.0 mg/kg Bortezomib administration for 4 weeks results in a 72% or 84% reduction in pancreatic cancer murine xenografts growth, as well as an increase in tumor cell apoptosis. 1.0 mg/kg Bortezomib treatment results in significant inhibition of human plasmacytoma xenograft growth, increase in tumor cells apoptosis and overall survival, and a decrease in tumor angiogenesis. [3]
臨床試験 A phase I study of weekly subcutaneous Bortezomib in patients with steroid-refractory or -dependent chronic graft versus host disease is currently in recruiting.
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[4]

Kinetic Methods In a typical kinetic run, 2.00 mL of assay buffer (20 mM HEPES, 0.5 mM EDTA, 0.035% SDS, pH 7.8) and Suc-Leu-Leu-Val-Tyr-AMC in DMSO are added to a 3 mL fluorescence cuvette, and the cuvette is placed in the jacketed cell holder of a fluorescence spectrophotometer. Reaction temperature is maintained at 37℃ by a circulating water bath. After the reaction solution has reached thermal equilibrium (5 minutes), 1 μL−10 μL of the stock enzyme solution is added to the cuvette. Reaction progress is monitored by the increase in fluorescence emission at 440 nm (λex= 380 nm) that accompanies cleavage of AMC from peptide-AMC substrates.

細胞アッセイ:

[5]

細胞株 Human multiple myeloma cells line U266
濃度 ~10 μM
反応時間 2 days
実験の流れ

The inhibitory effect of Bortezomib on cell growth is assessed by measuring MTT dye absorbance of the cells. Cells from 48-hour cultures are pulsed with 10 μL of 5 mg/mL MTT to each well for the last 4 hour of 48-hour cultures, followed by 100 μL of isopropanol containing 0.04 N HCl. Absorbance is measured at 570 nm using a spectrophotometer.

動物実験:

[3]

動物モデル Human plasmacytoma xenografts RPMI 8226
製剤 Saline
投薬量 1 mg/kg
投与方法 i.v. twice weekly for 4 weeks, then once weekly

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

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
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

参考

化学情報

Download Bortezomib (PS-341) SDF
分子量 384.24
化学式

C19H25BN4O4

CAS No. 179324-69-7
保管 3年-20℃
2年-80℃in solvent
別名 LDP-341, MLM341
溶解度 (25°C) * In vitro DMSO 76 mg/mL (197.79 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/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.
化学名 B-​[(1R)​-​3-​methyl-​1-​[[(2S)​-​1-​oxo-​3-​phenyl-​2-​[(2-​pyrazinylcarbonyl)​amino]​propyl]​amino]​butyl]​-boronic acid

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Frequently Asked Questions

  • Question 1
    On your website, it is mentioned that Bortezomib should be prepared at a concentration of 5 mg/ml in 2% DMSO/30% PEG300/ddH2O for in vivo use. But on the product sheet we received with the compound, it is mentioned: 5mg/ml in 0.5% methylcellulose, 0.2% tween 80. So which is the correct preparation buffer?

    Answer: S1013 Bortezomib in 2% DMSO+30% PEG 300+ddH2O at 5 mg/ml is a clear solution, and it in 0.5% methylcellulose+0.2% Tween 80 is a suspension. Please choose the suitable vehicle according to your administration route. When you prepare the clear solution, please dissolve Bortezomib in DMSO first, make sure it dissolves well, warm it up to 45 degree and/or sonicate if necessary, then add PEG, mix well, and finally add water.

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Tags: Bortezomib (PS-341)を買う | Bortezomib (PS-341)供給者 | Bortezomib (PS-341)を購入する | Bortezomib (PS-341)費用 | Bortezomib (PS-341)生産者 | オーダーBortezomib (PS-341) | Bortezomib (PS-341)代理店
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