Merck
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安全信息

B5437

Sigma-Aldrich

苯达莫司汀 盐酸盐 水合物

≥98% (HPLC)

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别名:
1H-Benzimidazole-2-butanoic acid, 5-[bis(2-chloroethyl)amino]-1-methyl monohydrochloride, Treanda
经验公式（希尔记法）:
C16H21Cl2N3O2·HCl · xH2O
分子量:
394.72 (anhydrous basis)
MDL编号:
MFCD16879055
PubChem化学物质编号:
329773260
NACRES:
NA.77

检测方案

≥98% (HPLC)

形式

powder

储存条件

desiccated

颜色

off-white

溶解性

H2O: >30 mg/mL

创始人

Teva

储存温度

room temp

SMILES字符串

O.Cl.Cn1c(CCCC(O)=O)nc2cc(ccc12)N(CCCl)CCCl

InChI

1S/C16H21Cl2N3O2.ClH.H2O/c1-20-14-6-5-12(21(9-7-17)10-8-18)11-13(14)19-15(20)3-2-4-16(22)23;;/h5-6,11H,2-4,7-10H2,1H3,(H,22,23);1H;1H2

InChI key

TWBJYCLUHINEDN-UHFFFAOYSA-N

一般描述

Bendamustine comprises 2-chloroethylamine alkylating group, a butyric acid side chain and a benzimidazole ring in its structure and is a nitrogen mustard. It is catabolized in the liver by the enzyme cytochrome P450 1A2 into γ hydroxyl-bendamustine and N-desmethyl-bendamustine.

应用

Bendamustine hydrochloride hydrate has been used as:
  • a chemotherapy agent for chronic lymphocytic leukemia (CLL) samples to monitor spliced and unspliced gene expression
  • an inhibitor to E3 ubiquitin-protein ligase RNF3 (HOIP) in matrix-assisted laser desorption ionization time-of-flight mass spectrometry (MALDI-TOF) assay
  • a cytotoxic chemotherapeutic drug in high-throughput screening to test interaction with BAY87-2243

生化/生理作用

Bendamustine is a therapeutic agent employed in treating lymphomas and chronic lymphocytic leukemia. It may be useful in central nervous system (CNS) malignancies treatment regimen due to its penetration capacity into brain tissue. Bendamustine is a promising candidate for non-Hodgkin lymphoma and Hodgkin lymphoma therapies.
Bendamustine hydrochloride is a DNA-alkylator with a distinct pattern of activity. Bendamustine activates DNA-damage stress response and apoptosis; inhibits mitotic checkpoints; and induces mitotic catastrophe.

特点和优势

This compound is a featured product for Apoptosis research. Click here to discover more featured Apoptosis products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by Teva. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

象形图

Skull and crossbonesHealth hazard
GHS06,GHS08

警示用语：

Danger

危险分类

Acute Tox. 3 Oral - Carc. 2 - Muta. 2 - Repr. 2

储存分类代码

6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

dust mask type N95 (US), Eyeshields, Faceshields, Gloves

法规信息

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Elinor A Chapman et al.
Oncotarget, 8(61), 102948-102964 (2017-12-22)
The functional significance of AKT in chronic lymphocytic leukemia (CLL) remains unclear. Given the importance of non-malignant T cells in regulating clonal expansion in CLL, we investigated the role of AKT in T cell-mediated cytoprotection and proliferation using an established
Manoj K Kashyap et al.
Haematologica, 100(7), 945-954 (2015-04-12)
RNA splicing plays a fundamental role in human biology. Its relevance in cancer is rapidly emerging as demonstrated by spliceosome mutations that determine the prognosis of patients with hematologic malignancies. We report studies using FD-895 and pladienolide-B in primary leukemia
Sheridan M Hoy
Drugs, 72(14), 1929-1950 (2012-09-07)
Bendamustine (Levact®) is an alkylating agent consisting of three structural elements: a 2-chloroethylamine alkylating group; a butyric acid side chain; and a benzimidazole ring. Although its precise mechanism of action is as yet unknown, it appears to exert its antineoplastic
Optimal use of bendamustine in hematologic disorders: treatment recommendations from an international consensus panel-an update
Cheson BD, et al.
Leukemia Lymphoma, 57(4), 766-782 (2016)
Therasa Kim et al.
BMC cancer, 18(1), 729-729 (2018-07-11)
A relatively high proportion of patients diagnosed with primary CNS lymphoma will experience recurrent disease, yet therapy options are limited in salvage therapy. This is the first study to evaluate a bendamustine-based combination regimen for the treatment of relapsed/refractory PCNSL
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Discover Bioactive Small Molecules for Apoptosis

Apoptosis, or programmed cell death (PCD), is a selective process for the removal of unnecessary, infected or transformed cells in various biological systems. As it plays a role in the homeostasis of multicellular organisms, apoptosis is tightly regulated through two principal pathways by a number of regulatory and effector molecules.

Discover Bioactive Small Molecules for Cell Cycle Research

n proliferating cells, the cell cycle consists of four phases. Gap 1 (G1) is the interval between mitosis and DNA replication that is characterized by cell growth. Replication of DNA occurs during the synthesis (S) phase, which is followed by a second gap phase (G2) during which growth and preparation for cell division occurs. Together, these three stages comprise the interphase phase of the cell cycle. Interphase is followed by the mitotic (M) phase.

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