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生物活性
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.
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体外研究
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体内研究
30% Propylene glycol, 5% Tween 80, 65% D5W(5%葡萄糖水溶液)
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激酶实验
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细胞实验
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动物实验
30 毫克/毫升 腹腔注射
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不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
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例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
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参考文献
[1] Chirivi RG, et al. Int J Cancer, 1994, 58(3), 460-464.
[2] Davies, B., et al. 1993. Cancer Res. 53: 2087-2091.
[3] Wang, X., et al. 1994. Cancer Res. 54: 4726-4728.
[4] Kohn, E.C. and Liotta, L.A. 1995. Cancer Res. 55: 1856-1862.
分子式
C23H31N3O4S2 |
分子量
477.64 |
CAS号
130370-60-4 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
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DMSO
100 mM |
Water
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Ethanol
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体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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