Bortezomib (PS-341)

Catalog No.S1013 Synonyms: Velcade, LDP-341, MLM341, NSC 681239

For research use only.

Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.

Bortezomib (PS-341) Chemical Structure

CAS No. 179324-69-7

Selleck's Bortezomib (PS-341) has been cited by 801 publications

Purity & Quality Control

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Biological Activity

Description Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.
Targets
NF-κB [6]
()
20S proteasome [1]
(Cell-free assay)
0.6 nM(Ki)
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1838 NVrL[HR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnL6TWM2OD12MUi2MlMzKM7:TR?= NGDVZpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OjVyNEGvK|5USU6JRWK8M4E,
IMR-5 MkD3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NESybpBKSzVyPUO0NFkvPjJizszN M1PuSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
TE-441-T MkPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{[ye2lEPTB;MkWyNU44KM7:TR?= NWX2cYd2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzJ3MESxM{c,W0GQR1XSQE9iRg>?
U-698-M MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfwU41KSzVyPUKyOlIvOTVizszN MoHhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|I2ODRzLze+V2FPT0WUPD;hQi=>
COLO-824 NE\PT5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTF{NkGuO|gh|ryP NE[4eJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OjVyNEGvK|5USU6JRWK8M4E,
P31-FUJ MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzhTWM2OD1zMUGyMlc2KM7:TR?= NX;VVZpMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzJ3MESxM{c,W0GQR1XSQE9iRg>?
KY821 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnX[4ZKSzVyPUGwN|YvODRizszN Mnm5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|I2ODRzLze+V2FPT0WUPD;hQi=>
RPMI-8866 NUHJOFJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PHSGlEPTB;MUCwOk4zQCEQvF2= M{W1flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
TC-YIK NGPGZ4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPxRVhKSzVyPUe4NU4xOSCwTR?= M1XaVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
MS-1 MmrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTd3OT60NkBvVQ>? M3nzTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
DMS-153 NY\R[2g4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFW4UFhKSzVyPUe0Ok45OyCwTR?= NG\ZcYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OjVyNEGvK|5USU6JRWK8M4E,
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CPC-N NFLjUI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vWVGlEPTB;NECzMlc4KG6P NFzhbWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OjVyNEGvK|5USU6JRWK8M4E,
COLO-668 NIX3RmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTvTWM2OD12MEOuOVchdk1? M37tZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFMzPTB2MT:nQnNCVkeHUkyvZV4>
NCI-H226 MlrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjF[WxSUUN3ME20NFMvOjNibl2= NHHNRVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OjVyNEGvK|5USU6JRWK8M4E,
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NCI-H1963 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjvTWM2OD1|OE[uNVkhdk1? NHr2VnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{OjVyNEGvK|5USU6JRWK8M4E,
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RAW 264.7 NUHW[|RWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fVcFExOCCwTR?= NHnUdpY1QCCq MWjS[YR2[2W|IHPlcIwhfmmjYnnsbZR6yqB? NInQRmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkSyO|E2PCd-MkK0NlcyPTR:L3G+
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SNK-6 NHrGO4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVGxJO69VQ>? NVXSOItTOjRiaB?= NVzXPVVuWmWmdXPld{Bk\WyuII\pZYJqdGm2edMg Mnq3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFzN{C5PFgoRjJzMUewPVg5RC:jPh?=
KAI-3 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFP2WFMyKM7:TR?= NFrKc3ozPCCq MmfyVoVlfWOnczDj[YxtKH[rYXLpcIl1gcLi MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTF5MEm4PEc,OjFzN{C5PFg9N2F-
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Glioma (HF2876) M2nXVmN6fG:2b4jpZ4l1gSCjc4PhfS=> MkPrO|IhcHK| NXjNTWhOTUN3MDC9JFAvODByNzFOwG0> NWDE[WdNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPFg3QTlpPkK2Nlg5Pjl7PD;hQi=>
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Glioma (HF3013) M3zuVmN6fG:2b4jpZ4l1gSCjc4PhfS=> MnfXO|IhcHK| Mn7zSWM2OCB;IECuNFAxPyEQvF2= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ6OE[5PUc,OjZ{OEi2PVk9N2F-
Glioma (HF2381) M3zmVmN6fG:2b4jpZ4l1gSCjc4PhfS=> Mni5O|IhcHK| M1O1UmVEPTBiPTCwMlAxODdizszN NFjjeFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK4PFY6QSd-Mk[yPFg3QTl:L3G+
Glioma (HF2790) M2HsfWN6fG:2b4jpZ4l1gSCjc4PhfS=> NEPhW4M4OiCqcoO= MX\FR|UxKD1iMD6wNFA4KM7:TR?= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ6OE[5PUc,OjZ{OEi2PVk9N2F-
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Molt4 M1OxTWZ2dmO2aX;uJIF{e2G7 MVfFR|UxKD1iMD6wNlEh|ryP NHrHcFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkWwN|M1QSd-MkK1NFM{PDl:L3G+
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fibroblast NH7FRmhyUFSVIHHzd4F6 M1f3OpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiClb370do9tKEiqIIfpcIQhfHmyZTDmbYJzd2KuYYP0JINmdGy| NXLlVWtbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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fibroblast MWTxTHRUKGG|c3H5 MlixdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgZ49vfHKxbDDIbEB4cWymIIT5dIUh\mmkcn;icIF{fCClZXzsdy=> MlvNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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OHS-50 NXfmbnlOeUiWUzDhd5NigQ>? NHvMNlhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBQUFNvNUCgZ4VtdHN? NWXoSVBLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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Rh41 MkLPdWhVWyCjc4PhfS=> MlnudWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog1OSClZXzsdy=> NVHY[GZNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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TC32 M4DVfZFJXFNiYYPzZZk> NX;heIpNeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? NIDxboE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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Saos-2 NEf5T3dyUFSVIHHzd4F6 MXTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTZY9{NTJiY3XscJM> NUPqb2F4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 NFLsc2ZyUFSVIHHzd4F6 NUm0ZnR2eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiT4L0bI9od26jbDCzSEB3cWGkaXzpeJkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz MmDlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD NIHsTJdyUFSVIHHzd4F6 NUjlTZF4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiT4L0bI9od26jbDCzSEB3cWGkaXzpeJkhe2O{ZXXuJIZweiCURDDj[Yxtew>? NYL3VHdORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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SUP-B15 M4m3NGZ2dmO2aX;uJIF{e2G7 MYSxJJRwKDFyMDDuUS=> NGjVS2kzPCCqcoO= M1jTe2lvcGmkaYTpc44hd2ZicILveIVie2:vZTDpckBqdWG2aX7pZk1z\XOrc4ThcpQhcHWvYX6gV3VRNUJzNTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBkdGWjdnXkJHBCWlBiZYjwdoV{e2mxbjDheEAyKHSxIEGwNEBvVSCjZoTldkAzPCCqcoOgZpkhcW2vdX7vZoxwfCCjc4PhfS=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN4NUi5Nkc,OzB|NkW4PVI9N2F-
SEM NH;lfHBHfW6ldHnvckBie3OjeR?= NV\Pe|U4OSC2bzCxNFAhdk1? NV;xXYtuOjRiaILz NVfmfnpUUW6qaXLpeIlwdiCxZjDwdo91\WG|b33lJIlvKGi3bXHuJHNGVSClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDjcIVifmWmIGDBVnAh\XiycnXzd4lwdiCjdDCxJJRwKDFyMDDuUUBi\nSncjCyOEBpenNiYomgbY1ufW6xYnzveEBie3OjeR?= NFfZVVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO2OVg6Oid-M{CzOlU5QTJ:L3G+
SEM NGK1fINHfW6ldHnvckBie3OjeR?= NIPCe5YyOCCwTR?= MXixPEBpenN? NUXCZXRCUW6qaXLpeIlwdiCxZjDwdo91\WG|b33lJIlvKGi3bXHuJHNGVSClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDh[4dz\XOxbXWgZYNkfW23bHH0bY9vKGG2IEGwJI5OKGGodHXyJFE5KGi{czDifUBjgSCIQVPTJIFv[Wy7c3nz M4PEOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5|MEO2OVg6OjxxYU6=
SEM M1z6fGZ2dmO2aX;uJIF{e2G7 M{K2XFExKG6P NG\wO5QyQCCqcoO= MnrLTY5pcWKrdHnvckBw\iCycn;0[YF{d22nIHnuJIh2dWGwIGPFUUBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCjZ3fy[ZNwdWViYXPjeY12dGG2aX;uJIF1KDFyIH7NJIFnfGW{IEG4JIhzeyCkeTDmcJVwemW|Y3XuZ4UhdWmlcn;zZ49xcWNibXX0bI9l M3vDRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{[1PFkzLz5|MEO2OVg6OjxxYU6=
HepG2 NYjVcIRCS2WubDD2bYFjcWyrdImgZZN{[Xl? M1i5RWhmeEd{IHPlcIx{KH[rYXLpcIl1gSCzSGTTJIZweiCcaXvhJJZqenW|IHnubIljcXSxcoO= NY[5VGZ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{OyNlk2PDVpPkOzNlI6PTR3PD;hQi=>
Assay
Methods Test Index PMID
Western blot phospho-PERK / ATF-4 ; GRP-78 / GADD-34 ; pro-caspase-12 / pro-caspase-3 ; pro-caspase-9 ; p-IκBα / IκBα ; COX-2 / cIAP2 15509775 20335171 24085292
Immunofluorescence Vimentin ; Ubiquitin 19010849
Growth inhibition assay Cell viability 20571067
ELISA IL-8 24085292
In vivo

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]

Protocol (from reference)

Kinase Assay:

[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.

Cell Research:

[5]

  • Cell lines: Human multiple myeloma cells line U266
  • Concentrations: ~10 μM
  • Incubation Time: 2 days
  • Method:

    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.

  • (Only for Reference)
Animal Research:

[3]

  • Animal Models: Human plasmacytoma xenografts RPMI 8226
  • Dosages: 1 mg/kg
  • Administration: i.v. twice weekly for 4 weeks, then once weekly
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 76 mg/mL
(197.79 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+30% PEG 300+ddH2O
For best results, use promptly after mixing.

5mg/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

Molecular Weight 384.24
Formula

C19H25BN4O4

CAS No. 179324-69-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles B(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04656951 Recruiting Drug: Daratumumab Multiple Myeloma University of Cologne|Janssen-Cilag G.m.b.H June 1 2021 Phase 2
NCT04915248 Active not recruiting Drug: Daratumumab|Drug: Bortezomib|Drug: Dexamethasone Plasmablastic Lymphoma Fondazione Italiana Linfomi ONLUS|Janssen-Cilag S.p.A. March 18 2021 Phase 2
NCT04570631 Recruiting Drug: Eftozanermin alfa|Drug: Bortezomib|Drug: Dexamethasone Multiple Myeloma AbbVie November 5 2020 Phase 1
NCT03993262 Recruiting Drug: Bortezomib|Drug: Placebo Autoimmune Encephalitis Jena University Hospital May 13 2020 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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
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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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