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Delanzomib

Delanzomib

产品编号 T6027   CAS 847499-27-8
别名: 德兰佐米, CEP-18770

Delanzomib (CEP-18770) 是一种强效的具有口服活性的蛋白酶体的胰凝乳蛋白酶样活性抑制剂,IC50为 3.8 nM。它抑制NF-κB 活性,诱导癌细胞凋亡,具有很强的抗血管生成和抗癌活性。

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Delanzomib Chemical Structure
Delanzomib, CAS 847499-27-8
规格 价格/CNY 货期 数量
1 mg ¥ 389 现货
2 mg ¥ 558 现货
5 mg ¥ 965 现货
10 mg ¥ 1,560 现货
25 mg ¥ 3,170 现货
50 mg ¥ 4,650 现货
100 mg ¥ 6,630 现货
1 mL * 10 mM (in DMSO) ¥ 997 现货
产品目录号及名称: Delanzomib (T6027)
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纯度: 99.46%
纯度: 95.52%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Delanzomib (CEP-18770) is an orally active inhibitor of the chymotrypsin-like activity of proteasome (IC50: 3.8 nM). It only marginally inhibits the tryptic and peptidylglutamyl activities of the proteosome.
靶点活性 Chymotrypsin-like proteasome:3.8 nM
体外活性 CEP-18770 demonstrates marginal prevention of the tryptic and peptidyl gultamyl activities of the protesome. The IC50 values of CEP-18770 are similar to those of bortezomib, with the chymotryptic and caspase-like activities being inhibited at low-nanomolar concentrations.[1] CEP-18770 inhibits A2780 ovarian cancer cells, PC3 prostate cancer, H460, LoVo colon cancer, RPMI8226 multiple myeloma cancer and HS-Sultan anaplastic non-Hodgkin lymphoma with IC50 values of 13.7, 22.2, 34.2 11.3, 5.6 and 8.2 nM, respectively.[1] CEP-18770 blocks the ubiquitin-proteasome pathway in several MM and in the chronic myelogenous leukemia cell line, K562. CEP-18770 causes an accumulation of ubiquitinated proteins over 4 to 8 hours with a profile similar to that observed after bortezomib treatment.[1] IκBα degradation is completely blocked by pretreatment with CEP-18770. CEP-18770 significantly inhibits high levels of NF-κB activity in both RPMI-8226 and U266 cells. The time- and concentration-dependent suppression of NF-kB DNA-binding activity in MM cell lines by CEP-18770 leads to a decrease of expression of several NF-κB-modulated genes mediating the growth and survival of tumor cells including IkBα itself, the X-chromosome-linked inhibitor-of-apoptosis protein (XIAP), the pro-inflammatory cytokines TNF-α and interleukin-1β (IL-1β), the intracellular adhesion molecule (ICAM1), and the pro-angiogeneic factor vascular endothelial growth factor. [1] The expression of these NF-κB–mediated genes and their modulation by bortezomib are associated with more favorable Clinicalal responsiveness to this agent, highlighting their potential prognostic value in response to CEP-18770 exposure.
体内活性 CEP-18770 reveals sustained dose-related relative tumor weight inhibition. CEP-18770 leads to dose-related complete tumor regressions, as compared to bortezomib treatment, which results in a 50% incidence of CR at its maximally tolerated dose (MTD) of 1.2 mg/kg intravenously. [1] In contrast to bortezomib, CEP-18770 reveals dose-related increase in the incidence of tumor-free mice by the completion of these studies (120 days after tumor transplantation). Oral administration of CEP-18770 produces a marked decrease in tumor weight and notable dose-related incidence of complete tumor regression with minimal changes in animal body weight over the course of the 120 day studies. [1]When compared to bortezomib, equiactive doses of CEP-18770 reveal a greater and more sustained dose-related inhibition of tumor proteasome activity, corresponding temporarily with maximum induction of caspase-3 and 7 activity.[1] The maximum apoptotic signal is 2.5 fold greater for CEP-18770 versus bortezomib. In contrast, proteasome inhibition profiles of CEP-18870 and bortezomib are comparable in the normal peripheral mouse tissues examined (liver, lungs, whole blood, and brain [no activity]) in both their magnitude and their duration.[1] No proteasome inhibition is detected in brain tissue at any time point for either CEP-18770 or bortezomib. In MM xenograft models, the addition of CEP-18770 to melphalan completely preventes the growth of both melphalan-sensitive or melphalan-resistant tumours. [1] The combination of CEP-18770 and bortezomib leads to complete regression of bortezomib-sensitive tumours and markedly delays progression of bortezomib-resistant tumours compared to treatment with either agent alone. Single agent CEP-18770 PO also shows marked anti-MM effects in these xenograft models[1]
激酶实验 Probing proteasome activity in cell extracts: Human multiple myeloma cells are washed twice with cold phosphate-buffered saline, pelleted and lysed with one volume of glass beads (<106 microns, acid-washed) and an equal volume of homogenization buffer (50 mM Tris (pH 7.4), 1 mM dithiothreitol, 5 mM MgCl2, 2 mM ATP and 250 mM sucrose) by vortexing at high speed for 15-30 min at 4 °C. Beads, membrane fractions, nuclei and cell debris are then removed from the supernatant by centrifugation at 16,000 g for 5 min. The protein content of extracts is quantitated using the Bradford assay. Proteasome activity is assayed as described below. Equal amounts (typically 60 g) of protein are denatured by boiling in reducing sample buffer, separated by 12.5% SDS-PAGE and electrotransferred onto polyvinylidene difluoride (PVDF) membranes. Immunoblotting is performed using a dansyl-sulfonamidohexanoyl polyclonal antibody (1:7,500, rabbit) and horseradish peroxidase–coupled goat or swine anti-rabbit secondary antibody followed by enhanced chemiluminescence.
细胞实验 HMEC and TEC cells are seeded into 24-well plates at a density of 104 cells/well in DMEM supplemented with 5% FCS. After incubation with proteasome inhibitors (48 hours), cells are washed, air dried, and stained with crystal violet as described. Cell number is determined, in duplicate samples, on the basis of a standard curve obtained with known cell numbers. All experiments are performed in triplicate. In vitro formation of capillary-like structures is studied on cells (4 × 104 cells/well in DMEM supplemented with 5% FCS. After incubation with proteasome inhibitors (48 hours), cells are washed (cells/well in 24-well plates) and seeded onto Matrigel-coated wells in DMEM containing 0.25% BSA. HMEC and TEC cells (5 × 103 per well), suspended in 200 μL DMEM with 5% FCS (positive control), serum-free medium (negative control), are layered onto the Matrigel surface in the presence or absence of proteasome inhibitor CEP-18770. Cells are observed with a inverted microscope and experimental results are then recorded after a 6-hour incubation at 37 °C. Data is analyzed, as the mean (× 1 SD) of total length of capillary-like structures, by the Micro-Image system and is expressed as mm/field by the computer analysis system in 5 different fields at 100 × magnification in duplicated wells for 4 different experiments. (Only for Reference)
别名 德兰佐米, CEP-18770
分子量 413.28
分子式 C21H28BN3O5
CAS No. 847499-27-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 77 mg/mL (186.3 mM)

DMSO: 77 mg/mL (186.3 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.4197 mL 12.0983 mL 24.1967 mL 60.4917 mL
5 mM 0.4839 mL 2.4197 mL 4.8393 mL 12.0983 mL
10 mM 0.242 mL 1.2098 mL 2.4197 mL 6.0492 mL
20 mM 0.121 mL 0.6049 mL 1.2098 mL 3.0246 mL
50 mM 0.0484 mL 0.242 mL 0.4839 mL 1.2098 mL
100 mM 0.0242 mL 0.121 mL 0.242 mL 0.6049 mL

计算器

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分子量计算器
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参考文献

1. Piva R,et al. Blood. 2008,111(5),2765-2775. 2. Sanchez E, et al. Br J Haematol. 2010,148(4),569-581. 3. Berkers CR, et al. Nat Methods. 2005,2(5),357-362.

文献引用

1. Chen X, Chen Y, Ou Y, et al. Bortezomib inhibits NLRP3 inflammasome activation and NF-κB pathway to reduce psoriatic inflammation. Biochemical Pharmacology. 2022, 206: 115326.
cpm-1285 Resveratrol SP2509 Anticancer agent 106 Anticancer agent 105 Ara-SH PP5-IN-1 JNJ-1013

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 抗癌活性化合物库 抗抑郁症化合物库 抗乳腺癌化合物库 HIF-1化合物库 ReFRAME 相关化合物库 细胞凋亡化合物库 抗前列腺癌化合物库 药物功能重定位化合物库

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
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给药体积
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第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Delanzomib 847499-27-8 Apoptosis NF-Κb Proteases/Proteasome Ubiquitination NF-κB Proteasome 德兰佐米 Inhibitor CEP 18770 CEP-18770 anti-cancer Nuclear factor-κB Nuclear factor-kappaB chymotrypsin-like antiangiogenic inhibit CEP18770 inhibitor

 

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