Bortezomib (PS-341) 化学構造
分子量: 384.24

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Quality Control & 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 NWPyb4F1S3m2b4TvfIlkKEG|c3H5 MYO1NEDPxE1? MoXyOFghcA>? NUTKfGdCTE2VTx?= MVXLbYxteyClZXzsd{BjgSCvb4LlJJRp[W5iOUml M4HBTlExPDl7NkSz
OVCA 429 NULCPJc5TnWwY4Tpc44hSXO|YYm= NIfQVGs{ODBibl2= NULtXJoxPDhiaB?= MlnGSG1UVw>? NYr4PJY6TGm|coXweJMhcW62YXP0JI12dHSrY3XscJVt[XJidIXtc5Ihe3CqZYLvbYR{ NYS4WI5lOTB7OUm3OlY>
RPMI8226 NWHPN5VGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjLd3gyODBibl2= MV60PEBp MV;EUXNQ Ml7CTWM2OD1|MDDuUS=> M3HYWVEyOzB4NEi5
Dox40 Mm\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TvN|ExOCCwTR?= M1Ptd|Q5KGh? NYC1[ldLTE2VTx?= NUCybo02UUN3ME20NEBvVQ>? MX2xNVMxPjR6OR?=
MR20 NF7Uc2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XP[|ExOCCwTR?= MYK0PEBp M3H0[WROW09? M1;jNGlEPTB;MkCgcm0> MYGxNVMxPjR6OR?=
LR5 NYiwdII3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vaZlExOCCwTR?= NWC0emlQPDhiaB?= NXyyV2JxTE2VTx?= M1L1VGlEPTB;MkCgcm0> MkDZNVE{ODZ2OEm=
U266 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXSxNFAhdk1? MUm0PEBp NXPSNFZnTE2VTx?= NXHsW2RYUUN3ME2zJI5O M1;qVFEyOzB4NEi5
IM-9 NYfkc2xJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrjVmhsOTByIH7N NGjRe5k1QCCq Mo[5SG1UVw>? NHi4eJNKSzVyPU[gcm0> NEGwcooyOTNyNkS4PS=>
Hs Sultan MnzaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfZNVAxKG6P MV[0PEBp M3T5e2ROW09? MWPJR|UxRTJyIH7N Mnj0NVE{ODZ2OEm=
PAM-LY2 NGLNSHRHfW6ldHnvckBCe3OjeR?= MXWxNFAhdk1? MUGxNkBp MVLEUXNQ MluwTY5pcWKrdIOgUmYu|rqEIHHjeIl3[XSrb36= MXOxNVM2ODlzMx?=
PAM 212 M1HUVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXSNVAxKG6P NVHtfGZiPzJiaB?= NFzRdWdFVVOR MUHJcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? MYGxNVM2ODlzMx?=
PAM-LY2 Mk\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVf0ZZRZOTByIH7N NIDaeVg4OiCq NF:zc2pFVVOR M{G1fGlvcGmkaYTzJINmdGxidnnhZoltcXS7 NEnXTJYyOTN3MEmxNy=>
B4B8 M{f0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvONVAxKG6P MlLEO|IhcA>? MYPEUXNQ M4O4TWlvcGmkaYTzJINmdGxidnnhZoltcXS7 NUnEdo4yOTF|NUC5NVM>
B7E3 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\HfXUyODBibl2= Mlq0O|IhcA>? MWHEUXNQ NXvNfJdCUW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= Mn;nNVE{PTB7MUO=
UM-SCC-9 M1rCfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGT3[GEyODBibl2= NVPENFU6PzJiaB?= M2fUdWROW09? NHXPTWtKdmirYnn0d{Bk\WyuII\pZYJqdGm2eR?= NV64dphZOTF|NUC5NVM>
UM-SCC-11B Mm\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXixNFAhdk1? Mn;oO|IhcA>? MoHPSG1UVw>? Mm\NTY5pcWKrdIOgZ4VtdCC4aXHibYxqfHl? M3:1cFEyOzVyOUGz
H460 NXn0c4hITnWwY4Tpc44hSXO|YYm= MWKxNEDPxE1? M37yS|I1KGh? MlXVSG1UVw>? NETB[ohKdmS3Y3XzJGJkdC1{IIDoc5NxcG:{eXzheIlwdiCjbnSgZ4xm[X[jZ3WgZ49zemWuYYTl[EB4cXSqIFeyMW0heGijc3WgZZJz\XO2 NUG3e2dQOTJ2OUKxNVc>
U266 MlGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvvNHE2ODBibnevcYw> MXi0PEBp NGW3c4pFVVOR M33EfGlvcGmkaYTzJINmdGxiZ4Lve5Rp NXvQTFFrOTJ4M{G2NVk>
ARH77 Ml7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\RVVA2ODBibnevcYw> Mm\qOFghcA>? NV;renByTE2VTx?= MWnJcohq[mm2czDj[YxtKGe{b4f0bC=> M4jyXVEzPjNzNkG5
WAD-1 NVHNUGtwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXtR4s2ODBibnevcYw> NHvnVVM1QCCq NX;qVXRkTE2VTx?= NETmTpFKdmirYnn0d{Bk\WyuIHfyc5d1cA>? NX7meo9QOTJ4M{G2NVk>
U266/LR7 NFXHcHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGn6RXI2ODBibnevcYw> MmjROFghcA>? NVHMcI53TE2VTx?= MnLFTY5pcWKrdIOgZ4VtdCCpcn;3eIg> MkTONVI3OzF4MUm=
U266/dox4 Mly2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX61NFAhdmdxbXy= MWe0PEBp NVz3WnZUTE2VTx?= M3PKOWlvcGmkaYTzJINmdGxiZ4Lve5Rp Mnq5NVI3OzF4MUm=
RPMI8226/LR5 NGHUcoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfx[5JwPTByIH7nM41t MmTzOFghcA>? MYXEUXNQ MmrOTY5pcWKrdIOgZ4VtdCCpcn;3eIg> NYDtc|liOTJ4M{G2NVk>
H460 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[5PVExKM7:TR?= M3\GRVczKGh? NULwOYtFTE2VTx?= MnfPTWM2OD1zMECgcm0> MlXONVI3OzF4MkC=
H358 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmxNEDPxE1? M2O5S|czKGh? MkfNSG1UVw>? M2XWOmlEPTB;N{Cgcm0> NXj5R5lJOTJ4M{G2NlA>
H322 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVexNEDPxE1? MlG1O|IhcA>? NFzXWoxFVVOR NF7EXmlKSzVyPU[yNEBvVQ>? MVWxNlY{OTZ{MB?=
H460 NGTlUXlHfW6ldHnvckBCe3OjeR?= Mly2NVAxKG6P M{\INlI1KGh? M{LDb2ROW09? M2fUbGlv\HWlZYOgS|IuVS2yaHHz[UBienKnc4SgZY5lKHS3YoXsbY4h[XO|ZX3icJku\Gm|YYPz[Y1jdHl? MmL0NVI3OzF4MkC=
LNCap-Pro5 MXjGeY5kfGmxbjDBd5NigQ>? MXKxJO69VQ>? M3v6dFQhcA>? MmDSSG1UVw>? M4DUenN1[WKrbHn6[ZMheDV| NH7seoYyPDZzMkWzNi=>
T29 Mm\xRZBweHSxc3nzJGF{e2G7 NXPCUWNqPTBibl2= M2\Xc|Q5KGhi MX3EUXNQ MnrMTY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M1r4d|E3Pzd6MUe5
T29Kt1 M4jLemFxd3C2b4Ppd{BCe3OjeR?= M{nie|UxKG6P NG[zdZI1QCCqIB?= MVfEUXNQ M3G4d2lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NXXQWlJJOTZ5N{ixO|k>
HCT116 NE[yNFlCeG:ydH;zbZMhSXO|YYm= MYe1NEBvVQ>? M1rSflQ5KGhi M3f1RmROW09? NX\2OZVUUW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MVyxOlc4QDF5OR?=
HKe-3 MojDRZBweHSxc3nzJGF{e2G7 MofxOVAhdk1? MnzhOFghcCB? M2r4bWROW09? M1XNUGlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NXLNbFAxOTZ5N{ixO|k>
NB-1691 NGXTbohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSxJO69VQ>? MkTrO|IhcA>? MlmwTY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJJRwKDVn MYexO|Y5QTZ6NB?=
CHLA-255 Mn\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TzTFEh|ryP MkPLO|IhcA>? MVjJcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36geI8hOiV? NYDzc5U1OTd4OEm2PFQ>
SK-N-AS NHn6UmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnWRmFvOSEQvF2= NHvTbYM4OiCq NF\tdWlKdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44hfG9iMUCl MoXwNVc3QDl4OES=
NB-1691 Mnf4SpVv[3Srb36gRZN{[Xl? M{DYfFExKG6P MWmyOEBp MXjTbYdvcW[rY3HueIx6KHKnZIXj[ZMh[2WubIOgbY4hfGinIFewM2cyKHCqYYPl NWXmRVI6OTd4OEm2PFQ>
CHLA-255 MlK3SpVv[3Srb36gRZN{[Xl? MWCxNEBvVQ>? NH7w[IMzPCCq NVfUSWl4VW:mZYP0cJkhemWmdXPld{Bk\WyuczDpckB1cGViR{CvS|EheGijc3W= NIW3V5QyPzZ6OU[4OC=>
RPMI 8226 MkHWSpVv[3Srb36gRZN{[Xl? M{TPO|IxKG6P NYnPPWJLQCCq NGHhVW1UcWewaX\pZ4FvfGy7IHXubIFv[2W|IF7GMe67SiCjY4Tpeol1gQ>? NXP2T5g{OTl2M{[wOVA>
MM.1S MVzGeY5kfGmxbjDBd5NigQ>? MX[yNEBvVQ>? MXS4JIg> MVPTbYdvcW[rY3HueIx6KGWwaHHuZ4V{KE6ILd86RkBi[3Srdnn0fS=> NVHzdWJxOTl2M{[wOVA>
U266 M4LINWZ2dmO2aX;uJGF{e2G7 MXyyNEBvVQ>? MXq4JIg> MlXyV4lodmmoaXPhcpRtgSCnbnjhcoNmeyCQRj5OvmIh[WO2aY\peJk> M4ntPFE6PDN4MEWw
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INA6 NHv0O5RHfW6ldHnvckBCe3OjeR?= M1HwSFIxKG6P MXO4JIg> MoqxV4lodmmoaXPhcpRtgSCnbnjhcoNmeyCQRj5OvmIh[WO2aY\peJk> Mo\MNVk1OzZyNUC=
OPM2 M4LIO2Z2dmO2aX;uJGF{e2G7 M4TnXFIxKG6P MXS4JIg> NXnLcZRnW2mpbnnmbYNidnSueTDlcohidmOnczDOSk3PwkJiYXP0bZZqfHl? NXy5PGNUOTl2M{[wOVA>
RPMI 8226 NIjzXpVHfW6ldHnvckBCe3OjeR?= NVK3[Wg5OjBibl2= MYe4JIg> MXLJcoR2[2W|IFTORUB{gW62aHXzbZM> NH36PGkyQTR|NkC1NC=>
BaF/3 Ml;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrzVVcyODBibl2= NI\KTZk1QCCq MoPaTWM2OD14LkKgcm0> M3[4OVIxOzB3Nkmy
BaF/3-p210 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWexNFAhdk1? NGHmPGQ1QCCq MYjJR|UxRTRwNzDuUS=> NWC4U24{OjB|MEW2PVI>
TCC-S NX3rNIJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXCZmoyODBibl2= NEX6Tlg1QCCq MXLJR|UxRTJwODDuUS=> MYGyNFMxPTZ7Mh?=
BaF/3 M13iPWZ2dmO2aX;uJGF{e2G7 M3PJNVYhdk1? M4LtXVQ5KGh? MkDoTY5lfWOnczDhJIdz\WG2IFexJINmdGxvY4njcIUh[XK{ZYP0 NYe0RpJ6OjB|MEW2PVI>
BaF/3-p210 Ml;FSpVv[3Srb36gRZN{[Xl? NFLzUY83KG6P M365SlQ5KGh? MVrJcoR2[2W|IHGgd4xq\2i2IFexJINmdGxvY4njcIUh[XK{ZYP0 MkD2NlA{ODV4OUK=
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Raji NWf3TZhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfFNUDPxE1? MkXENlQhcA>? NXv3T2ZrWmWmdXPld{Bk\WyuII\pZYJqdGm2edMg NWDKWlhnOjFzN{C5PFg>
LCL-1 M{nCfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL2U4QyOSEQvF2= NG\tfZUzPCCq MnLFVoVlfWOnczDj[YxtKH[rYXLpcIl1gcLi Mn\hNlEyPzB7OEi=
LCL-2 NIG4blZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TvVlEh|ryP MYKyOEBp M1foV3Jm\HWlZYOgZ4VtdCC4aXHibYxqfHoEoB?= NXnjNZRWOjFzN{C5PFg>
BJAB MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDYNUDPxE1? Mn7xNlQhcA>? NFnFU5BT\WS3Y3XzJINmdGxidnnhZoltcXS7wrC= MYOyNVE4ODl6OB?=
SNT-13 M2jZb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzMNUDPxE1? NXq5U3A2OjRiaB?= NHzzfY1T\WS3Y3XzJINmdGxidnnhZoltcXS7wrC= NVnBbnpCOjFzN{C5PFg>
SNT-16 NUHB[WY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LReFEh|ryP NHrmZlMzPCCq NEXIboZT\WS3Y3XzJINmdGxidnnhZoltcXS7wrC= M2rWdlIyOTdyOUi4
Jurkat NFnDeWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDlR2IyKM7:TR?= NI\5ZYIzPCCq MWHS[YR2[2W|IHPlcIwhfmmjYnnsbZR6yqB? NXLWRZNWOjFzN{C5PFg>
KAI-3 MkTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TsVlEh|ryP M1TLVFI1KGh? MmPlVoVlfWOnczDj[YxtKH[rYXLpcIl1gcLi NHX2PXYzOTF5MEm4PC=>
SNK-6 NF30PFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\EO|Eh|ryP NWrwOZo5OjRiaB?= MYrS[YR2[2W|IHPlcIwhfmmjYnnsbZR6yqB? MmHVNlEyPzB7OEi=
KHYG-1 Mn;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfDfpIyKM7:TR?= Ml\RNlQhcA>? NH[zVnJT\WS3Y3XzJINmdGxidnnhZoltcXS7wrC= M2rVOFIyOTdyOUi4
SNT-16 NIrWb2VCeG:ydH;zbZMhSXO|YYm= NX[3d4ZnOSEQvF2= M{PROVYhcA>? MnLDTY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M365e|IyOTdyOUi4
Jurkat Mle2RZBweHSxc3nzJGF{e2G7 MXexJO69VQ>? MnjROkBp NU[1W4E4UW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MlLPNlEyPzB7OEi=
KAI-3 Mof1RZBweHSxc3nzJGF{e2G7 MYexJO69VQ>? NGC5dm83KGh? Ml2xTY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MYWyNVE4ODl6OB?=
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SNT-16 NFnRTppCdnSrdnnyZYwhSXO|YYm= MX2xJO69VQ>? NV3pb2tDOjRiaB?= NEHMW4lKdmS3Y3XzJIx6fGmlIHnu[oVkfGmxbjDv[kBGSlZ? NHL1SpgzOTF5MEm4PC=>
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HH NF3JXGVHfW6ldHnvckBCe3OjeR?= MVqxNFAhdk1? Ml3nNlQhcA>? MkX5SG1UVw>? M{TqcYRwf26{ZXf1cIF1\XNiVFfGMe6zOSCjbnSgTWwuOTJiZYjwdoV{e2mxbh?= M{DyUFI2PjhzM{O1
Hut-78 NEL2VlFOcWe{YYTpc44hSXO|YYm= M2ryWlExOCCwTR?= M17hd|I1KGh? NYmzPVRGTE2VTx?= NHj1XGxT\WS3Y3XzJINmdGxibXnndoF1cW:wIHL5JFgx6oDVOUCl NHX4fYwzPTZ6MUOzOS=>
HH MmX1UYloemG2aX;uJGF{e2G7 NHnTS|MyODBibl2= MlLaNlQhcA>? M1fEWWROW09? M4PPcnJm\HWlZYOgZ4VtdCCvaXfyZZRqd25iYomgPFDjiJN7MTW= MYCyOVY5OTN|NR?=
U937 MYrGeY5kfGmxbjDBd5NigQ>? NYjxfFFCOTByIH7N NV\ufoZwPiCq NY\VN4JkUW6mdXPld{BKVC16IHX4dJJme3Orb36gbY4hVFCVLYP0bY12dGG2ZXSgWVk{PyCvYXPyc5Bp[Wencx?= Mmm4NlU4QTF2N{e=
human PBMC NYjP[YxJTnWwY4Tpc44hSXO|YYm= NX23WVVNOTByIH7N Mn:2NlQhcA>? MYjJcoR2[2W|IFnMMVghemWuZXHz[S=> MlXkNlU4QTF2N{e=
ES6 MoW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnnOJhKSzVyPUCuNFAzOSCwTR?= MnrJV2FPT0WU
SK-UT-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwMU[zJI5O NIfyXZFUSU6JRWK=
SH-4 NUPIPHFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFL4PIVKSzVyPUCuNVc{KG6P NE\jWXlUSU6JRWK=
TE-9 NYTLNGN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\2TWM2OD1yLkG4NkBvVQ>? NHTLWlVUSU6JRWK=
A253 MnLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYf6[ohnUUN3ME2wMlIxQCCwTR?= NVPJR5RXW0GQR1XS
no-10 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLh[2YzUUN3ME2wMlIyKG6P NVPBXYM5W0GQR1XS
MMAC-SF NEC0dG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPLTWM2OD1yLkKxOkBvVQ>? MX;TRW5ITVJ?
A101D MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLVRm1pUUN3ME2wMlIzPSCwTR?= NVTP[odoW0GQR1XS
NTERA-S-cl-D1 NXjXeZRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzhTWM2OD1yLkK0N{BvVQ>? NGrUW|FUSU6JRWK=
8-MG-BA M3jG[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PRdGlEPTB;MD6yOUBvVQ>? NXrBfnlwW0GQR1XS
KNS-42 NHnkdVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TDUGlEPTB;MD6yOVghdk1? NUPqd3kyW0GQR1XS
LXF-289 M4n6U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInBOFJKSzVyPUCuNlY6KG6P NV:zdI1KW0GQR1XS
OVCAR-4 MnGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;vXWlEPTB;MD6yPFkhdk1? NVPidmtUW0GQR1XS
LOUCY M3nub2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTBwMkmzJI5O M2rIW3NCVkeHUh?=
BB65-RCC M{\pNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHuTWM2OD1yLkOwOEBvVQ>? MnLRV2FPT0WU
D-542MG NHTad2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwM{K5JI5O NWnvNHZLW0GQR1XS
ONS-76 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1r2eWlEPTB;MD6zN{BvVQ>? NIHGUZpUSU6JRWK=
BB30-HNC M33jTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoK4TWM2OD1yLkOzOUBvVQ>? MXzTRW5ITVJ?
KS-1 M{fxU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTBwM{Sgcm0> M4DKSXNCVkeHUh?=
A388 NH3iV2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jrb2lEPTB;MD6zOVYhdk1? M3HxV3NCVkeHUh?=
ES8 Mkm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHP[lVFUUN3ME2wMlQhdk1? M1:4OXNCVkeHUh?=
MZ2-MEL NHPQN3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LufWlEPTB;MD60NFchdk1? NEL4c4pUSU6JRWK=
HCC2998 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\GNGxJUUN3ME2wMlQyOiCwTR?= MlvtV2FPT0WU
D-247MG NIXKc4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHraXnZKSzVyPUCuOFE{KG6P NGjyZplUSU6JRWK=
ACN MmP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XJVWlEPTB;MD60NVchdk1? MnfnV2FPT0WU
LB2518-MEL NWrpXWNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;pV4lxUUN3ME2wMlQzPSCwTR?= NHrpNndUSU6JRWK=
ES1 NWTQcVhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPHRYNKSzVyPUCuOFMhdk1? NYHB[XViW0GQR1XS
HCE-T MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTBwNEO5JI5O NVfiWW1ZW0GQR1XS
OS-RC-2 NYPEOZE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXW3O4IzUUN3ME2wMlQ1KG6P NH;CSIxUSU6JRWK=
MFH-ino MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\OTWM2OD1yLkS0N{BvVQ>? NGDucJFUSU6JRWK=
OCUB-M NXHFbXZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVO1PVFLUUN3ME2wMlQ1PyCwTR?= MljkV2FPT0WU
CP66-MEL MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTBwNEezJI5O NXy3Z4ZxW0GQR1XS
LB771-HNC NUjo[mpiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DXbmlEPTB;MD60O|Qhdk1? Ml;sV2FPT0WU
DSH1 M2nrOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7sfWpLUUN3ME2wMlQ5KG6P MlnsV2FPT0WU
HUTU-80 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;UPIFnUUN3ME2wMlU{OyCwTR?= M3TudXNCVkeHUh?=
CESS Mk\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nsXGlEPTB;MD61N|ghdk1? M1m0OnNCVkeHUh?=
NCI-H747 NFvncGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTBwNUO5JI5O MXXTRW5ITVJ?
HT-144 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDBeJdKSzVyPUCuOVc3KG6P NUP2bINWW0GQR1XS
COLO-829 MnPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTBwNkG0JI5O MUjTRW5ITVJ?
A4-Fuk MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofZTWM2OD1yLk[yN{BvVQ>? NXzKc4xOW0GQR1XS
GI-ME-N M4q3cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvqXlB6UUN3ME2wMlY{PCCwTR?= MXzTRW5ITVJ?
LB831-BLC NVqzRWR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\jWJdKSzVyPUCuOlQyKG6P NGHWSZpUSU6JRWK=
HOP-62 M4\VU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTETWM2OD1yLk[0O{BvVQ>? NYPrbZVZW0GQR1XS
BB49-HNC NHLNb2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlT2TWM2OD1yLk[1NkBvVQ>? Mlv4V2FPT0WU
D-336MG NHXjfJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvrTWM2OD1yLk[1O{BvVQ>? MYnTRW5ITVJ?
TK10 NHrkcXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTFbo1KSzVyPUCuOlc6KG6P NVTQU|JVW0GQR1XS
Ramos-2G6-4C10 NXrKWHlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjINW5KSzVyPUCuOlk{KG6P Mmr2V2FPT0WU
LB373-MEL-D M13i[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LrfWlEPTB;MD63JI5O M1vvXnNCVkeHUh?=
SF126 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTBwN{CxJI5O M2j2SXNCVkeHUh?=
UACC-257 M{e4UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwN{Ggcm0> M33UPHNCVkeHUh?=
KINGS-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwN{KyJI5O Mo\NV2FPT0WU
LS-513 MnW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwN{O5JI5O Mn7sV2FPT0WU
GI-1 NHHYVFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;YTWM2OD1yLke2OEBvVQ>? NIT3SopUSU6JRWK=
ES7 NGn4ZmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwN{[2JI5O M3TlfHNCVkeHUh?=
LB2241-RCC M{TPXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;0fmlxUUN3ME2wMlgxPCCwTR?= MVnTRW5ITVJ?
D-263MG MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnsTWM2OD1yLkiwO{BvVQ>? MlnRV2FPT0WU
SW684 M2jOWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTBwOEKxJI5O MULTRW5ITVJ?
ML-2 Ml:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PHe2lEPTB;MD64NlEhdk1? NFHrVIZUSU6JRWK=
SK-LMS-1 NGjm[GZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{X1bGlEPTB;MD64OVQhdk1? NUnmXmNkW0GQR1XS
TE-5 Mn;aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTBwOE[1JI5O M2DBN3NCVkeHUh?=
QIMR-WIL MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jneWlEPTB;MD64PFkhdk1? MUTTRW5ITVJ?
NCI-H1355 NWrTcXc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDqTWM2OD1yLki5OUBvVQ>? NGDlW45USU6JRWK=
SNB75 NICyV4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;pbIZGUUN3ME2wMlkyOiCwTR?= NF3nT4NUSU6JRWK=
RXF393 NXe4RpQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPn[YdQUUN3ME2wMlkyPCCwTR?= M4HLRXNCVkeHUh?=
IST-MEL1 Ml;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHjOYFKSzVyPUCuPVE4KG6P NUDXW4hoW0GQR1XS
SF268 MonHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwOUKzJI5O MYfTRW5ITVJ?
KALS-1 NIXBbGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;LbJBKSzVyPUCuPVI2KG6P NVPtZ2Z{W0GQR1XS
HC-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTjTWM2OD1yLkm3OUBvVQ>? NF;WenhUSU6JRWK=
SW872 MkjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTBwOUm2JI5O Mnr3V2FPT0WU
PSN1 Mmf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTFwMEGgcm0> MYfTRW5ITVJ?
TE-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnr4TWM2OD1zLkCzJI5O MWjTRW5ITVJ?
TE-10 M4LDT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3W1OWlEPTB;MT6wN{BvVQ>? NH7yR5dUSU6JRWK=
RKO MnHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTFwME[gcm0> MonYV2FPT0WU
LC-2-ad M2\Gc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjRemRKSzVyPUGuNFghdk1? MYjTRW5ITVJ?
SK-MM-2 NGD4Z3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrTXXRKSzVyPUGuNFkhdk1? NEjnSlBUSU6JRWK=
VA-ES-BJ MnnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4K1N2lEPTB;MT6wPUBvVQ>? Mln0V2FPT0WU
MZ7-mel Ml\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXmyZXBzUUN3ME2xMlA6KG6P MUDTRW5ITVJ?
D-392MG MoTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTFwMTDuUS=> M1LwNnNCVkeHUh?=
CCRF-CEM MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPqTWM2OD1zLkGzJI5O M33FeXNCVkeHUh?=
EM-2 NHznU2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUn5[G1bUUN3ME2xMlE3KG6P NF7xOVlUSU6JRWK=
HAL-01 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonGTWM2OD1zLkG4JI5O MX;TRW5ITVJ?
TE-8 M3fifGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\STm0yUUN3ME2xMlE6KG6P NWDsVG1mW0GQR1XS
NCI-H1882 NI\oeZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDOc25KSzVyPUGuNkBvVQ>? NGLydlJUSU6JRWK=
Daudi MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTFwMkKgcm0> NU\0UXZlW0GQR1XS
BL-41 M4fidmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17TWGlEPTB;MT6yOUBvVQ>? NXPFeVFDW0GQR1XS
SR NWP0Rmt{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWfBWZZsUUN3ME2xMlI2KG6P NGPXVXFUSU6JRWK=
KM12 MojsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[1TWM2OD1zLkK3JI5O NF70PG5USU6JRWK=
K5 MkfxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXBTWM2OD1zLkK4JI5O NGO5TZhUSU6JRWK=
A3-KAW NXXmTFNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TXcGlEPTB;MT6yPEBvVQ>? MWDTRW5ITVJ?
CMK M1\Qd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmL0TWM2OD1zLkK5JI5O MnWxV2FPT0WU
Calu-6 NVrBcoRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mle3TWM2OD1zLkK5JI5O MX7TRW5ITVJ?
IST-SL2 NIexZWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jwfGlEPTB;MT6zNUBvVQ>? MnLLV2FPT0WU
OPM-2 NFz6e4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzvTWM2OD1zLkOzJI5O MV;TRW5ITVJ?
DU-4475 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHnNWJQUUN3ME2xMlM3KG6P M2TKdXNCVkeHUh?=
ECC12 MmnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTFwM{egcm0> M334SnNCVkeHUh?=
L-540 M{Ozc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPW[HVRUUN3ME2xMlM4KG6P NV[xSmJiW0GQR1XS
CAS-1 MmXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTFwM{egcm0> NXS0OZlLW0GQR1XS
PF-382 M1XZNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3pe2t1UUN3ME2xMlQ4KG6P MVvTRW5ITVJ?
LS-411N M2rtd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXlTWM2OD1zLkWzJI5O Mor6V2FPT0WU
NCI-H69 NVOySmtwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TDWWlEPTB;MT61OEBvVQ>? NID2cVRUSU6JRWK=
NB12 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGizfoRKSzVyPUGuOVYhdk1? MYfTRW5ITVJ?
HEL NWjPXYRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{C5XWlEPTB;MT62NUBvVQ>? MYPTRW5ITVJ?
GCIY NFLUe4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17QWWlEPTB;MT62NkBvVQ>? MnuyV2FPT0WU
EHEB MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIm3emJKSzVyPUGuOlchdk1? NGjMW|JUSU6JRWK=
TGBC1TKB NYPIVYxOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHn0fZhKSzVyPUGuO|Ehdk1? Mmj2V2FPT0WU
KURAMOCHI MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkG2TWM2OD1zLkeyJI5O NYTCbnVKW0GQR1XS
U-266 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHObJhbUUN3ME2xMlc3KG6P MWTTRW5ITVJ?
LC4-1 MlrxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLZTWM2OD1zLke5JI5O MnvHV2FPT0WU
NCI-H2126 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjvb3pKSzVyPUGuPEBvVQ>? M4nBUXNCVkeHUh?=
NCI-H1092 NH3aTHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrlb3lKSzVyPUGuPEBvVQ>? M{T5TnNCVkeHUh?=
GB-1 NGnPVGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmX2TWM2OD1zLkixJI5O NYS4[XJMW0GQR1XS
MV-4-11 M1;3Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTFwOEKgcm0> Mn[wV2FPT0WU
Becker NH;zV5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjuWm9EUUN3ME2xMlg{KG6P Mk[yV2FPT0WU
MPP-89 NX;yOpJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTFwOEmgcm0> M1ztW3NCVkeHUh?=
BE-13 MknqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLzTWM2OD1zLkmzJI5O MojaV2FPT0WU
697 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITXTVZKSzVyPUGuPVkhdk1? M{DtOXNCVkeHUh?=
NKM-1 NYHabI83T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTJibl2= NX7peIhFW0GQR1XS
NB13 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jCVGlEPTB;MjDuUS=> MlPPV2FPT0WU
LS-123 M3q0Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnyzTWM2OD1{LkCyJI5O NH7KdHFUSU6JRWK=
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NCI-H1522 M{DSe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjSTWM2OD1|MEeuNFUhdk1? M4\KVHNCVkeHUh?=
SCH M{POcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrMRnNCUUN3ME2zNlIvOjJibl2= Mo\5V2FPT0WU
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CA46 Ml\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TGTGlEPTB;M{ezMlY{KG6P NXu0OXhkW0GQR1XS
NCI-H1963 NIDrTHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPYVpFVUUN3ME2zPFYvOTlibl2= Mn3SV2FPT0WU
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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 2年-20℃
6月-80℃in solvent
別名 LDP-341, MLM341
溶解度 (25°C) * In vitro DMSO 76 mg/mL (197.79 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
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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