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Batimastat (BB-94)

现货
Catalog No.
A2577
MMP抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,050.00
现货
1mg
¥ 500.00
现货
5mg
¥ 1,000.00
现货
10mg
¥ 1,500.00
现货
25mg
¥ 2,500.00
现货

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Background

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),  Mr 72,000 type IV collagenase (IC50 = 4 nM), Mr 92,000 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

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

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

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

文献引用

Chemical Properties

Physical AppearanceA solid
StorageStore at 4°C
M.Wt477.64
Cas No.130370-60-4
FormulaC23H31N3O4S2
SynonymsBatimastat,BB-94
Solubility≥23.88mg/mL in DMSO
Chemical Name(2S,3R)-N1-hydroxy-3-isobutyl-N4-((S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl)-2-((thiophen-2-ylthio)methyl)succinamide
SDFDownload SDF
Canonical SMILESCNC([C@@H](NC([C@@H]([C@H](CSC1=CC=CS1)C(NO)=O)CC(C)C)=O)CC2=CC=CC=C2)=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验:

细胞系

C170HM2和AP5LV细胞系

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

96 h;3.0 μg/ml

应用

在batimastat存在时的细胞增殖实验用MTT吸光度法进行评估。在无血清和含scrum培养基中培养的C170HM2和AP5LV细胞中,batimastat对细胞生长没有显著影响。

动物实验:

动物模型

人结肠癌原位移植裸鼠模型

剂量

30 mg/kg;i.p.

应用

BB-94引起原发肿瘤的中位重量从对照组中的293 mg(范围: 1141~124 mg)减少到BB-94治疗组中的144 mg(范围: 424~38 mg)(P < 0.001),并显著减少肿瘤侵入邻近组织的发生率,从对照组中发生率为67%(12/18)减少到BB-94治疗组中的35%(7/20)。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Watson S A, Morris T M, Robinson G, et al. Inhibition of organ invasion by the matrix metalloproteinase inhibitor batimastat (BB-94) in two human colon carcinoma metastasis models[J]. Cancer research, 1995, 55(16): 3629-3633.

[2] Wang X, Fu X, Brown P D, et al. Matrix metalloproteinase inhibitor BB-94 (batimastat) inhibits human colon tumor growth and spread in a patient-like orthotopic model in nude mice[J]. Cancer research, 1994, 54(17): 4726-4728.

生物活性

描述 Batimastat (BB-94)是一种有效的广谱基质金属蛋白酶(matrix metalloprotease,MMP)抑制剂,作用于MMP-1、MMP-2、MMP-9、MMP-7和MMP-3,IC50值分别为3 nM、4 nM、4 nM、6 nM和20 nM。
靶点 MMP-1 MMP-2 MMP-9 MMP-7 MMP-3  
IC50 3 nM 4 nM 4 nM 6 nM 20 nM  

质量控制

化学结构

Batimastat

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