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德兰佐米 /Delanzomib {[allProObj[0].p_purity_real_show]}

货号：A800043 同义名： CEP-18770

Delanzomib is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 3.8 nM, with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome.

Delanzomib 化学结构 CAS号：847499-27-8
Delanzomib 化学结构
CAS号：847499-27-8
Delanzomib 3D分子结构
CAS号：847499-27-8
Delanzomib 化学结构 CAS号：847499-27-8
Delanzomib 3D分子结构 CAS号：847499-27-8
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Delanzomib 纯度/质量文件 产品仅供科研

货号：A800043 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 20S proteasome ↓ Proteasome ↓ 其他靶点 纯度
Ixazomib ++++

20S proteasome, IC50: 3.4 nM

20S proteasome, Ki: 0.93 nM

 		99%+
Delanzomib +++

Chymotrypsin-like proteasome, IC50: 3.8 nM

 		98%
Celastrol +

20S proteasome, IC50: 2.5 μM

 		98%
MLN9708 +++

20S proteasome, IC50: 3.4 nM

20S proteasome, Ki: 0.93 nM

 		99%
Bortezomib ++++

20S proteasome, Ki: 0.6 nM

 		98%
Oprozomib ++

20S proteasome LMP7, IC50: 82 nM

20S proteasome β5, IC50: 36 nM

 		99%+
Epoxomicin ✔ 99%
PI-1840 ++

Chymotrypsin-like proteasome, IC50: 27 nM

 		98%
VR23 +++

Trypsin-like proteasomes, IC50: 1 nM

Chymotrypsin-like proteasomes, IC50: 3 μM

 		98%
Carfilzomib ++

Proteasome, IC50: 5 nM

 		98%
(R)-MG-132 +

Proteasome, IC50: 100 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Delanzomib 生物活性

靶点

  • 20S proteasome

    Chymotrypsin-like proteasome, IC50:3.8 nM
描述 The ubiquitin-proteasome pathway plays a key role in protein processing and degradation, regulating crucial transduction pathways for cell growth and survival, including cell-cycle control, transcriptional regulation, cellular stress responses, and antigen presentation. Delanzomib (CEP-18770) is an orally active proteasome inhibitor that has potency against chymotrypsin-like proteasome activity with IC50 value of 3.8 nM[2]. In vitro, treatment with 20 nM delanzomib suppressed nuclesar factor-κB (NF-κB) mediated transcription and induced apotosis in multiple myeloma cell lines CMA-03, H929, KMM1, KMS11, KMS18, KMS27, SKMM1, U266 and RPMI-8226. Delanzomib can inhibit cell proliferation, including A2780, PC3, H460 SC, LoVo, RPMI8226 and HS-Sultan cell lines, with IC50 values of 13.7 nM, 22.2 nM, 34.2 nM, 11.3 nM, 5.6 nM and 8.2 nM, respectively. These data indicated that delanzomib exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors, and bone marrow–derived stromal cells[2]. In vivo, delanzomib demonstrated dose-related inhibition of tumor proteasome activity in RPMI-8266 tumor-bearing SCID mice. Oral administration of delanzomib at 10 mg/kg twice a week resulted in a significant reduction of tumor weight and oral administration of delanzomib at 13 mg/kg resulted in complete tumor regression in RPMI-8226 subcutaneous xenograft SCID mice modelPiva R, Ruggeri B, Williams M, et al. CEP-18770: A novel, orally active proteasome inhibitor with a tumor-selective pharmacologic profile competitive with bortezomib. Blood, 2008, 111(5): 2765-2775.|https://www.ncbi.nlm.nih.gov/pubmed/18057228}. Treatment with delanzomib either 3 mg/kg once or twice weekly intravenously or orally at 10 mg/kg suppressed the development and gression of renal tissue renal tissue damage and extended the survival of the NZBWF1 mice with fatal lupus nephritis{{Seavey M M, Lu L D, Stump K L, et al. Novel, orally active, proteasome inhibitor, delanzomib (CEP-18770), ameliorates disease symptoms and glomerulonephritis in two preclinical mouse models of SLE. International Immunopharmacology, 2012, 12(1): 257-270.|http://www.ncbi.nlm.nih.gov/pubmed/22178195.
作用机制 Delanzomib reversible inhibits P2 threonine boronic acid of the 26S mammalian proteasome[3].

Delanzomib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00572637 Solid Tumors ... 展开 >>Lymphoma, Non-Hodgkin 收起 << Phase 1 Completed - Italy ... 展开 >> Europen Institute of Oncology Milano, Italy, 20141 Switzerland IOSI - Oncology Institute of Southern Switzerland - Ospedale S. Giovanni Bellinzona, Switzerland, 6500 Kantonsspital St. Gallen St. Gallen, Switzerland, 9007 收起 <<
NCT01348919 Multiple Myeloma Phase 1 Phase 2 Terminated - United States, Georgia ... 展开 >> Teva Investigational Site 1 Augusta, Georgia, United States United States, Kentucky Teva Investigational Site 3 Lexington, Kentucky, United States United States, Texas Teva Investigational Site 2 Houston, Texas, United States New Zealand Teva Investigational Site 201 Auckland, New Zealand Teva Investigational Site 204 Auckland, New Zealand Teva Investigational Site 200 Christchurch, New Zealand Teva Investigational Site 206 Hamilton, New Zealand Teva Investigational Site 205 Newtown, New Zealand Teva Investigational Site 202 Palmerston North, New Zealand Teva Investigational Site 203 Takapuna, New Zealand 收起 <<
NCT01023880 Multiple Myeloma Phase 1 Phase 2 Terminated - United States, Arizona ... 展开 >> Mayo Clinic- Scottsdale Scottsdale, Arizona, United States United States, Arkansas University of Arkansas for Medical Sciences Little Rock, Arkansas, United States United States, California Stanford Heme Group Palo Alto, California, United States University of California, San Francisco San Francisco, California, United States United States, District of Columbia Washington Cancer Institute Washington, District of Columbia, United States United States, Illinois Northwestern University Medical School Chicago, Illinois, United States United States, Michigan Henry Ford Health System Protocol Review Committee Detroit, Michigan, United States Sparrow Regional Cancer Center Lansing, Michigan, United States United States, Missouri Washington University School of Medicine St. Louis, Missouri, United States United States, New Jersey John Theurer Cancer Center Hackensack, New Jersey, United States United States, North Carolina Duke University Medical Center Durham, North Carolina, United States United States, Pennsylvania University of Pennsylvania Philadelphia, Pennsylvania, United States United States, Wisconsin Medical College of Wisconsin Milwaukee, Wisconsin, United States 收起 <<

Delanzomib 参考文献

[1]Sanchez E, Li M, et al. The proteasome inhibitor CEP-18770 enhances the anti-myeloma activity of bortezomib and melphalan. Br J Haematol. 2010 Feb;148(4):569-81.

[2]Piva R, Ruggeri B, Williams M, et al. CEP-18770: A novel, orally active proteasome inhibitor with a tumor-selective pharmacologic profile competitive with bortezomib. Blood, 2008, 111(5): 2765-2775.

[3]Seavey M M, Lu L D, Stump K L, et al. Novel, orally active, proteasome inhibitor, delanzomib (CEP-18770), ameliorates disease symptoms and glomerulonephritis in two preclinical mouse models of SLE. International Immunopharmacology, 2012, 12(1): 257-270.

Delanzomib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.10mL

2.42mL

1.21mL

24.20mL

4.84mL

2.42mL

Delanzomib 技术信息

CAS号847499-27-8
分子式C21H28BN3O5
分子量 413.275
别名 CEP-18770
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C
溶解度

DMSO: 105 mg/mL(254.07 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Delanzomib | CEP-18770 | Proteasome | AmBeed-信号通路专用抑制剂 | Delanzomib 纯度/质量文件 | Delanzomib 亚型比较 | Delanzomib 生物活性 | Delanzomib 临床数据 | Delanzomib 参考文献 | Delanzomib 实验方案 | Delanzomib 技术信息

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