Bortezomib (PS-341)
目录号：S1013 别名： LDP-341, MLM341
Molecular Weight(MW): 384.24
Bortezomib (PS-341)是有效的蛋白酶抑制剂，Ki为0.6 nM。它对肿瘤细胞表现出良好的选择性。
客户使用该产品的25个实验数据：
-
Immunoblot analysis of cell lysates from the indicated cell lines treated with GNE-6776 (2 μ M for 18 h), either alone or in combination with a UAE1 inhibitor MLN-7243 (5 μ M for 45 min) or the proteasome inhibitor bortezomib (5 μ M for 45 min) as indicated.
Nature, 2017, 550(7677):534-538. Bortezomib (PS-341) purchased from Selleck.
Indisulam dependent degradation of RBM39 can be blocked by bortezomib, a proteasome inhibitor. Cells were pretreated with indicated concentrations of bortezomib for 2 hours, followed by 6 hours of treatment with 2 μM indisulam. The effect of bortezomib is attenuated in a bortezomib resistant cell line.
Science, 2017, eaal3755. Bortezomib (PS-341) purchased from Selleck.
-
Wild-type mice fed as indicated were injected with vehicle (10% DMSO, pH 7.4 PBS) or bortezomib (5 mg/kg bodyweight). Livers were collected 16 hr later for quantitative PCR analysis of indicated genes (n = 4–5). *p < 0.05 bortezomib effect and #p < 0.05 Chol-Diet effect by two-way ANOVA.
Cell, 2017, 171(5):1094-1109. Bortezomib (PS-341) purchased from Selleck.
Effect of different proteasome inhibitors on dysferlin expression and on membrane resealing in cultured primary myoblasts. Primary myoblasts from patient 2 harboring a homozygous Arg555Trp DYSF mutation that were treated with the indicated amounts of bortezomib for 24 hours. Western blots of protein extracts were stained with anti-dysferlin antibodies and with anti–a-tubulin antibody as loading control.
Sci Transl Med 2015 6(250), 250ra112. Bortezomib (PS-341) purchased from Selleck.
-
Pharmacologic inhibition of the proteasome blocks proplatelet formation in murine and human megakaryocytes. Human megakaryocytes were pretreated with vehicle or bortezomib, and megakaryocytes producing proplatelets (PP) were examined. Shown are representative transmission images and representative confocal images with wheat germ agglutinin (WGA; red) and phalloidin (green) staining. Scale bars: 50 um.
J Clin Invest 2014 124(9), 3757-66. Bortezomib (PS-341) purchased from Selleck.
Effects of NF-kB inhibition on cell proliferation and apoptosis in Foxp3cKO prostate. A. Top left panels: Representative H&E staining of PIN lesions in ventral prostates of 60-week-old PBS- or bortezomib-treated Foxp3cKO littermates. Scale bar, 50 祄. Right graph: Quantification of Ki67-positive cells identified by IHC analysis (bottom left panels) as a measure of cell proliferation, performed with Scion Image software. Horizontal lines represent the average values. The p value was determined by two-tailed t test. B. Representative western blots showing p65 and nuclear p65 (N-p65) expression in prostates at 12 hours after LPS injection in 45-week-old PBS- or bortezomib-treated mice. C. Quantification of Bcl2l1 and Traf1/2 mRNA expression as a percentage of Hprt expression measured in microdissected mouse prostate epithelial cells by qPCR at 12 hours after LPS injection in 45-week-old PBS- or bortezomib-treated mice. Horizontal lines represent the average values. The p values were determined by two-tailed t test. D. Left panels: Representative images of TUNEL assays performed on prostates from PBS- or bortezomib-treated mice at 60 weeks of age. Insets show the apoptotic cells (green) in prostate glands. Scale bar, 100 祄. Right graph: Quantification of apoptotic cells in the ventral and dorsolateral prostates of PBS- or bortezomib-treated mice at 45 and 60 weeks of age. Horizontal lines represent the average values. The p value was determined by two-tailed t test. cKO, PB4-Cre4+Foxp3flox/y; wks, weeks; B/P, ratio of the mean value from bortezomib-treated mice to the mean value in PBS-treated mice. All experiments were repeated two times. Wks, weeks.
Cancer Res 2015 75(8), 1714-24. Bortezomib (PS-341) purchased from Selleck.
-
Immunofluorescence showing HDAC4 localization in mouse primary osteoblasts treated with vehicle or PTH alone or in the presence of bortezomib. Primary osteoblasts treated with vehicle, PTH, or PTH plus bortezomib for 2 h using anti-HDAC4 and anti-b-actin antibodies.
J Cell Biol 2014 205(6), 771-80. Bortezomib (PS-341) purchased from Selleck.
Inhibition of proteasome and lysosome or silencing of VCP and co-factors lead to the accumulation of OP-puro-labeled DRIPs adjacent to or within SGs. HeLa cells were co-treated for 45 min with OP-puro and arsenite (Ars.); where indicated, cells were pretreated with bortezomib (Bort.) overnight and/or ammonium chloride (NH4Cl) for 2 h 15 min. Cells were fixed and labeled with Alexa594-Azide and anti-TIA-1.
Cell Death Differ 2014 21(12), 1838-51. Bortezomib (PS-341) purchased from Selleck.
-
Immunofluorescence analysis for Ser536 p-NF-κB cellular localization of RS4;11cells treated with CX-4945 (5 μM) and bortezomib (2.5 nM) either alone or in combination. Cells were treated, collected at 22 h and reacted with an antibody to Ser536 p-NF-κB which was revealed by a Cy3-conjugated secondary antibody. DAPI was used to label nuclei.
Oncotarget, 2015, 51: S659-S660. Bortezomib (PS-341) purchased from Selleck.
Control wild-type and Fmn2–/–oocytes observed at different stages of meiotic maturation [prophase I (Pro I), NEBD, 3 hours and 8 hours after NEBD] using anti-Fmn2. wt + Bortezo, wild-type oocytes treated with 0.1μM Bortezomib for 90 minutes before fixation. All oocytes were observed using the same settings and the images treated the same way (three independent experiments). Red arrows indicate cortical labeling. Scale bar: 10μm.
Development 2011 138, 2903-2908. Bortezomib (PS-341) purchased from Selleck.
-
Cell viability of HCT116 cells treated with a single drug or with the addition of leucovorin.
Sci Rep, 2017, 7(1):682. Bortezomib (PS-341) purchased from Selleck.
(B–C) LNCaP (B) and LNCaP-AI (C) cells were transiently transfected with sPLA2-IIa(-800)-Luc (0.5 μg). The cells were then treated with Erlotinib (20 μM), Gefitinib (20 μM), Lapatinib (20 μM), CI-1033 (8 μM), LY294002 (20 μM) and Bortezomib (20 μM) without or with EGF (100 ng/ml) for 24 h. Luciferase assay was performed according to a standard protocol with Renilla luciferase as an internal control. Data are presented as the mean (±SD) of duplicate values of a representative experiment that was independently repeated for five times.
Carcinogenesis 2010 31, 1948–1955. Bortezomib (PS-341) purchased from Selleck.
-
LNCaP-AI cells were starved in 1% stripped medium for 24 h. The cells were then treated with Erlotinib (20 μM), Gefitinib (20 μM), Lapatinib (20 μM), CI-1033 (8 μM), LY294002 (20 μM) and Bortezomib (20 μM) for 24 h. Cell culture medium was collected from each sample and subjected to ELISA for sPLA2-IIa. The condition medium samples were diluted 10 times for ELISA. Average of duplicate samples was converted to nanogram per milliliter against standard curve. The data represent one of five repeated experiments.
Carcinogenesis 2010 31, 1948–1955. Bortezomib (PS-341) purchased from Selleck.
PS-341 impairs FPV replication in A549 cells. (A and B)A549 cells were either pretreated for 1 h with different concentrations of PS-341 or with solvent only or were left untreated. Then, cells were infected with FPV at an MOI of 0.001 (A) or 0.05 (B). After virus inoculation cells were posttreated with different concentrations of PS-341. (A) At 24 h p.i. supernatants were obtained and progeny virus titers were measured by standard plaque assay. (B)Proteasome activity and the ability of PS-341 to inhibit the proteasome was determined 24 h p.i. (C) A549 cells were pretreated with 50 nM PS-341 or solvent or left untreated for 1 h. Afterwards cells were infected with FPV at an MOI of 0.0005. Subsequent to virus inoculation cells were posttreated with 50 nM PS-341 or solvent or left untreated. After the indicated times p.i.supernatants were obtained and progeny virus titers were determined by standard plaque assay. Arrow bars in all experiments represent standard deviations of three independent experiments.
J Virol 2010 84, 9439–9451. Bortezomib (PS-341) purchased from Selleck.
-
Early steps of viral replication within the first replication cycle are affected. (A) For time-of-addition kinetics analysis, A549 cells were either left untreated or were pretreated for 10 h or 1 h with 50 nM PS-341 before infection and additionally posttreated after infection. Cells were infected with FPV at an MOI of 0.005. After virus inoculation cells were posttreated with 50 nM PS-341. Then the proteasome inhibitor was added after virus inoculation (10 h, 1 h, and 30 min) or it was added at the different times p.i. as indicated (1 h, 2 h, 4 h, 6 h, and 8 h; cells were not pretreated before infection). At 9 h p.i. supernatants were obtained and progeny virus titers were determined by standard plaque assay. Shown is one representative experiment out of three independent experiments. (B) A549 cells were pretreated with 50 nM PS-341 or left untreated for 1 h. Afterwards cells were infected with avian FPV or human PR8 at an MOI of 1. Subsequent to virus inoculation cells were posttreated with 50 nM PS-341 or left untreated. After the indicated times p.i. cells were lysed and analyzed by Western blotting for accumulation of viral proteins polymerase PB1 and matrix protein M1. Cellular protein ERK2 served as a control to demonstrate equal amounts of protein loading. Shown is one representative blot out of three independent experiments.
J Virol 2010 84, 9439–9451. Bortezomib (PS-341) purchased from Selleck.
A549 cells were treated with PS-341 at 50 nM for the indicated times or left untreated. Western blotting was performed with total cell lysates, using phospho-specific antibodies against JNK and the transcription factors c-Jun and ATF-2 or loading controls, respectively.
J Virol 2010 84, 9439–9451. Bortezomib (PS-341) purchased from Selleck.
-
Western blot of extracts of infected cells treated with different proteasome inhibitors at different concentrations, reacted with the indicated antibodies. p53 was used to monitor proteasome inhibition, and actin was used as a loading control.
J Virol 2011 85, 2781–2792. Bortezomib (PS-341) purchased from Selleck.
Time window treatment with proteasome inhibitors. (A) Scheme of the experiment performed with MA104 cells exposed to virus (OSU; MOI, 3) for 1 h and analyzed at the starting point and endpoint of the indicated time window treatments with DMSO, MG132, or bortezomib. (B) Western blot of cellular lysates derived from cells infected for the indicated time periods and treated with the proteasome inhibitors or DMSO. NI, noninfected cells. Blots were reacted with the indicated antibodies; p53 was used to monitor proteasome inhibition, and actin was used as a loading control.
J Virol 2011 85, 2781–2792. Bortezomib (PS-341) purchased from Selleck.
-
Fluorescence analysis of viroplasm formation on NSP5-EGFP cells infected with rotavirus (OSU; MOI, 3) and treated or not treated with MG132 (10 M) or bortezomib (10 M) at different times p.i., as indicated. Cells were analyzed at the starting points (1 h, 3 h, 5 h, 7 h) and endpoints (9 h) of the inhibitor’s window treatment.
J Virol 2011 85, 2781–2792. Bortezomib (PS-341) purchased from Selleck.
Quantification of the accumulation of viroplasms in infected NSP5 -EGFP/MA104 cells. At different times p.i., cells were treated for 4 h with DMSO or the indicated proteasome inhibitor and the number of viroplasms/cell was quantified at the starting (1 h, 3 h, 5 h; white bars) and endpoints (5 h, 7 h, 9 h) of treatment.
J Virol 2011 85, 2781–2792. Bortezomib (PS-341) purchased from Selleck.
-
The stable cell line HepAD38 was incubated for 18 h in the presence of the indicated amount of Bortezomib. The medium was removed and replaced by medium containing Bortezomib dissolved in PBS. In case of the control cells the same amount of PBS was added to the medium. 4 h later this procedure was repeated and again 14 h later the supernatant was collected. The amount of viral particles was quantified by real time PCR. HBV-genome quantification was done using COBAS® AmpliPrep/COBAS® TaqMan® HBV test (Roche Diagnostics GmbH, Mannheim, Germany) according to the manufacturer’s instructions. The assay shows relative values (the value for untreated control cells was arbitrarily set as 1) that are based on three independent experiments. The cell viability was analyzed by MTT assays. For does up to 50 nM no significant effect on cell viability was observed within 18h, for 100 nM the proportion of metabolically active cells was reduced to 83%.
J Biol Chem 2010 285, 41074-41086. Bortezomib (PS-341) purchased from Selleck.
HLC-1 cells were treated with IFN-gamma (30 ng/ml) and Bortezomib (0-10 nM) for 3 h. After washing with PBS, the cells were cultured for another 45 h in the fresh medium. After 48 h incubation, PD-L1 expression was analysed by flow cytometry (n =3).
Int Immunopharmacol, 2018, 54:39-45. Bortezomib (PS-341) purchased from Selleck.
-
Proteasome inhibition effect on biotinylation of MHC-Iα. (a) WB-ra of cellular extracts of HEK293 cells co-transfected with BAP-MHC-Ia and cyt-BirA (control) and, where indicated, with US2 or US11 in the absence (2) or presence of MG132 (MG; 50 μM for 4 h) or Bortezomib(Bort.; 50 μM for 4 h).
PLoS One 2011 6, e23712. Bortezomib (PS-341) purchased from Selleck.
KKU-M213 was treated with BTZ as indicated. Total cell lysate ( a) and nuclear extract (b) were prepared. Actin and γ -tubulin were loading controls for total and nuclear proteins, respectively.
2011 Mireia Vila Gasull University of Porto. Bortezomib (PS-341) purchased from Selleck.
-
Mireia Vila Gasull University of Porto. 2011;Mireia Vila Gasull . Bortezomib (PS-341) purchased from Selleck.
产品安全说明书
Proteasome抑制剂选择性比较
生物活性
| 产品描述 | Bortezomib (PS-341)是有效的蛋白酶抑制剂，Ki为0.6 nM。它对肿瘤细胞表现出良好的选择性。 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 体外研究 |
Bortezomib，一种硼酸二肽，是一种26S蛋白酶体的高选择性可逆抑制剂，其作用于错误折叠蛋白的降解，并且对细胞周期的调控是必要的。暴露于Bortezomib能够稳定p21，p27，和p53，以及促凋亡Bid和Bax蛋白，微囊蛋白-1，和抑制剂κB-α，这防止了核因子κB诱导的细胞存活途径的激活。Bortezomib也会促进促凋亡c-Jun-NH2末端激酶，以及内质网应激反应的激活。这些细胞蛋白水平的改变导致对增殖，迁移的抑制，和癌细胞凋亡的促进。[2] Bortezomib能够渗透到细胞，并抑制蛋白酶体介导的细胞内长寿蛋白水解，抑制50%蛋白质水解的浓度为∼0.1 μM。Bortezomib对衍生自美国国家癌症研究所(NCI)多重人类肿瘤的一组60个癌细胞系的IC50值为7 nM。PC-3细胞用Bortezomib (100 nM)处理8小时导致细胞积聚在G2-M期，相应的G1期细胞数量减少。Bortezomib在24和48小时杀死PC-3细胞，IC50分别为100和20 nM。Bortezomib治疗16-24小时后诱导细胞核缩合。Bortezomib在低至100 nM浓度下以时间依赖的方式导致PARP裂解，在处理24小时后产生效果。[1] |
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Cell Data |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 体内研究 | Bortezomib单一用药的抗癌作用已在多发性骨髓瘤的异种移植模型，成人白血病，肺癌，乳腺癌，前列腺癌，胰腺癌，头颈癌，和结肠癌，以及在黑色素瘤中得到证实。[2]在Lewis肺癌模型中，口服bortezomib (1.0 mg/ kg，每天)，服用18天引起肿瘤生长延迟，并减少转移数量。Bortezomib单一用药， 高达5 mg/kg剂量时显著降低乳腺癌细胞的存活率。在前列腺癌小鼠异种移植模型中，Bortezomib (1.0 mg/kg，每周一次)用药4周减少60%肿瘤生长。1.0 mg/kg Bortezomib给药4周导致胰腺癌小鼠异种移植物生长减少72%或84%，并导致肿瘤细胞凋亡增加。1.0 mg/kg Bortezomib显著抑制人浆细胞瘤异种移植物生长，增加肿瘤细胞凋亡和总存活率，并减少肿瘤血管生成。[3] |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
| 激酶实验： |
+ 展开
动力学法: 在典型的动力学试验中，2.00 mL试验缓冲液(20 mM HEPES，0.5 mM EDTA，0.035% SDS，pH 7.8) 和 Suc-Leu-Leu-Val-Tyr-AMC溶于DMSO，加入3 mL荧光比色皿中，并将比色皿放置于荧光分光光度计的夹套细胞皿座。反应温度通过循环水浴维持在37℃。反应溶液达到热平衡后(5 分钟)，1 μL−10 μL储存酶溶液加入培养皿。伴随AMC 从多肽AMC底物裂解的反应进程通过440 nm (λex= 380 nm)下荧光发射的增加监测。 |
|---|---|
| 细胞实验： |
+ 展开
|
| 动物实验： |
+ 展开
|
溶解度 (25°C)
| 体外 | DMSO | 76 mg/mL (197.79 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | Insoluble | |
| 体内 |
从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 2% DMSO+30% PEG 300+ddH2O |
5mg/mL |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 384.24 |
|---|---|
| 化学式 | C19H25BN4O4 |
| CAS号 | 179324-69-7 |
| 稳定性 | powder |
| in solvent | |
| 别名 | LDP-341, MLM341 |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
临床试验信息
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03829020 | Not yet recruiting | Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma | Mayo Clinic|National Cancer Institute (NCI) | March 1 2019 | Phase 1 |
| NCT03617484 | Recruiting | Mantle Cell Lymphoma | University of Michigan Rogel Cancer Center | March 2019 | Phase 2 |
| NCT03617484 | Recruiting | Mantle Cell Lymphoma | University of Michigan Rogel Cancer Center | March 2019 | Phase 2 |
| NCT03878524 | Not yet recruiting | Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia | OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation | March 14 2019 | Phase 1 |
| NCT03829020 | Not yet recruiting | Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma | Mayo Clinic|National Cancer Institute (NCI) | March 1 2019 | Phase 1 |
| NCT03878524 | Not yet recruiting | Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia | OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation | March 14 2019 | Phase 1 |
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
常见问题及建议解决方法
-
问题 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?
-
回答：
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.
