Tanomastat(Synonyms: BAY 12-9566)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Tanomastat (Synonyms: BAY 12-9566)

Tanomastat (BAY 12-9566) 是一种口服生物有效的含锌羧基的非肽联苯基质金属蛋白酶 (MMPs) 抑制剂。抑制MMP-2、MMP-3、MMP-9、MMP-13 的 Ki 值分别为 11、143、301 和 1470 nM。Tanomastat 在几种实验性肿瘤模型中具有抗侵袭和抗转移活性。

Tanomastat(Synonyms: BAY 12-9566)

Tanomastat Chemical Structure

CAS No. : 179545-77-8

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生物活性

Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models[1][2][3].

IC50 & Target[1]

MMP-2

11 nM (Ki)

MMP-3

143 nM (Ki)

MMP-9

301 nM (Ki)

MMP-13

1470 nM (Ki)

体外研究
(In Vitro)

Tanomastat (BAY 12-9566) (1-10000 nM; 6 hours) prevents matrix invasion by endothelial cells in a concentration-dependent manner (IC50=840 nM), without affecting cell proliferation[2].
Tanomastat (BAY 12-9566) (1-00 µM; 5 days) inhibits tubule formation completely at 15-100 µM[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Tanomastat (BAY 12-9566) (100 mg/kg; p.o.; daily for a 7-week period) inhibits local tumor regrowth without causing any toxic effect, and inhibits the number and volume of lung metastases[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six- to eight-week-old female BALB/c nude mice (bearing MDA-MB-435 cells)[3]
Dosage: 100 mg/kg
Administration: p.o.; daily for a 7-week period
Result: Inhibited local tumor regrowth by 58% without causing any toxic effect, and inhibited the number and volume of lung metastases by 57 and 88%, respectively.

分子量

410.91

Formula

C23H19ClO3S
CAS 号

179545-77-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Leung D, et al. Protease inhibitors: current status and future prospects. J Med Chem. 2000 Feb 10;43(3):305-41.

    [2]. Gatto C, et al. BAY 12-9566, a novel inhibitor of matrix metalloproteinases with antiangiogenic activity. Clin Cancer Res. 1999 Nov;5(11):3603-7.

    [3]. Nozaki S, et al. Activity of biphenyl matrix metalloproteinase inhibitor BAY 12-9566 in a human breast cancerorthotopic model. Clin Exp Metastasis. 2003;20(5):407-12.

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