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Batimastat(BB-94)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Batimastat(BB-94)图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
Batimastat (BB-94) 是一种有效的广谱 MMP 抑制剂,对 MMP-1、MMP-2、MMP-9、MMP-7 和 MMP-3 的 IC50 分别为 3、4、4、6 和 20 nM。

Cell lines

C170HM2 and AP5LV cell lines

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Reaction Conditions

96 h; 3.0 μg/ml

Applications

In vitro proliferation in the presence of batimastatwas assessed by the MTT absorbance assay. The effect of batimastat on the in vitro growth of C170HM2 and AP5LV in both serum-free and scrum-containing culture media was determined three times. Batimastat had no significant effect on the growth of either cell line.

Animal models

Orthotopic transplant model of human colon cancer in nude mice

Dosage form

30 mg/kg; i.p.

Applications

Treatment with BB-94 caused a significant reduction in the median weight of the primary tumor from 293 mg(range, 1141 to 124 mg) in the control group to 144 mg (range, 424 to 38 mg) in the BB-94 treated group (P< 0.001) and resulted in a marked reduction in the incidence of tumor invasion of adjacent tissue, from 12 of 18 mice in the control group (67%) to 7 of 20 mice in the BB-94 treated group (35%).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

Batimastat (also known as BB-49), [4-(N-hydroxyamino)-2R-isobutyl-3S-(thiopen-2-ylthiomethyl)-succinyl-L-phenylalanine-N-methylamide, is a potent and synthetic inhibitor of a broad spectrum of matrix metalloproteinases (MMPs), including interstitial collagenase (IC50= 3 nM), stromelysin (IC50= 20 nM), Mr72,000 type IV collagenase (IC50= 4 nM), Mr92,000 type IV collagenase (IC50= 4 nM), and matrilysin (IC50= 6 nM). It is a low-molecular-weight (MW = 478) and peptide-like collagen substrate analogue consisting of a peptide backbone and a hydroxamic acid group which bind to MMPs and the catalytically active zinc atom respectively. Batimastat exhibits antineoplastic and antiangiogenic activity in various tumor models, including ovarian carcinoma xegnografts and human colon tumor.

Reference

[1].Bernard Davies, Peter D. Brown, Nick East, Michael J. Crimmin, and Frances R. Balkwill. A synthetic matrix metalloproteinase inhibitor decreases tumor burden and prolongs survival of mice bearing human ovarian carcinoma xenografts. Cancer Research 1993; 53: 2087-2091
[2].X. Wang, X. Fu, P.D. Brown, M. J. Crimmin, and R. M. Hoffman. Matrix metalloproteinase inhibitor BB-94 (batimastat) inhibits human colon tumor growth and spread in a patient-like orthotopic model in nude mice. Cancer Research 1994; 54: 4726-4728
[3].Raffaella Giavazzi, Angela Garofalo, Cristina Ferri, Valeria Lucchini, Elisabeth A. Bone, Stefania Chiari, Peter D. Brown, M. Ines Nicoletti, and Giulia Taraboletti. Batimastat, a synthetic inhibitor of matrix metalloproteinases, potentiates the antitumor activity of cisplatin in ovarian carcinoma xgenografts. Clinical Cancer Research 1998; 4: 985-992