(2S,3R)-N-羥基-N'-[(2S)-1-甲基氨基-1-氧代-3-苯基丙-2-基]-3-異丁基-2-(噻吩-2-基硫甲基)丁二酰胺單鈉鹽
中文名稱 | (2S,3R)-N-羥基-N'-[(2S)-1-甲基氨基-1-氧代-3-苯基丙-2-基]-3-異丁基-2-(噻吩-2-基硫甲基)丁二酰胺單鈉鹽 |
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中文同義詞 | 巴馬司他單鈉鹽;(2S,3R)-N-羥基-N'-[(2S)-1-甲基氨基-1-氧代-3-苯基丙-2-基]-3-異丁基-2-(噻吩-2-基硫甲基)丁二酰胺單鈉鹽;巴馬司他納鹽;化合物 T10461;化合物 BATIMASTAT SODIUM SALT |
英文名稱 | (2S,3R)-N-Hydroxy-N'-[(2S)-1-methylamino-1-oxo-3-phenylpropan-2-yl]-3-(2-methylpropyl)-2-(thiophen-2-ylsulfanylmethyl)butanediamide sodium salt |
英文同義詞 | (2S,3R)-N-Hydroxy-N'-[(2S)-1-methylamino-1-oxo-3-phenylpropan-2-yl]-3-(2-methylpropyl)-2-(thiophen-2-ylsulfanylmethyl)butanediamide sodium salt;Batimastat sodium salt;BB 94 sodiuM salt;BB94 sodiuM salt;BB-94 sodiuM salt;BB-94 SODIUM SALT; BB 94 SODIUM SALT; BB94 SODIUM SALT |
CAS號(hào) | 130464-84-5 |
分子式 | C23H32N3NaO4S2 |
分子量 | 501.64 |
EINECS號(hào) | |
相關(guān)類別 | |
Mol文件 | 130464-84-5.mol |
結(jié)構(gòu)式 |
(2S,3R)-N-羥基-N'-[(2S)-1-甲基氨基-1-氧代-3-苯基丙-2-基]-3-異丁基-2-(噻吩-2-基硫甲基)丁二酰胺單鈉鹽 性質(zhì)
儲(chǔ)存條件 | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
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溶解度 | 溶于二甲基亞砜 |
IC50: 3 nM (MMP-1), 4 nM (MMP-2), 4 nM (MMP-9), 6 nM (MMP-7), 20 nM (MMP-3)
Batimastat (BB-94) is a potent matrix metalloproteinase inhibitor, exhibits an unexpected mode of binding. Batimastat inhibits gelatinases A and B with IC 50 values of 4 nM and 10 nM, respectively. The IC 50 with the structurally similar collagenase Ht-d is 6 nM, which is comparable with values for MMP-1 (3 nM), MMP-8 (10 nM), and MMP-3 (20 nM). CD30 shedding from the cell line Karpas299 can effectively be blocked by the hydroxamic acidbased metalloproteinase inhibitor Batimastat (BB-94, IC 50 =230 nM).
Intraperitoneal administration of Batimastat (BB-94) effectively blocks growth of human ovarian carcinoma xenografts and murine melanoma metastasis and delays the growth of primary tumors in an orthotopic model of human breast cancer without cytotoxicity and without affecting mRNA levels. Batimastat (BB-94) is a synthetic matrix metalloproteinase inhibitor that has shown antineoplastic and antiangiogenic activity in various tumor models. Treatment with Batimastat (60 mg/kg i.p. every other day, for a total of eight injections) concomitantly with Cisplatin (4 mg/kg i.v., every 7 days for a total of three injections) completely prevents growth and spread of both xenografts, and all animals are alive and healthy on day 200. Kaplan-Meier analysis of survival (at 48 h) shows that animals treated with Batimastat (BB-94) have increased survival (95.2%) in comparison with controls (75%), and differences are almost statistically significant (p=0.064). Matrix density is analyzed in saline- or Batimastat (40 mg/kg)-pretreated animals 4 h after E 2 administration, the time point at which collagen density is observed to be at its lowest after hormone treatment.