(S)-4-(4'-氯联苯-4-基)-4-氧代-2-(苯硫基甲基)丁酸
- CAS号:179545-77-8
- 英文名:Tanomastat
- 中文名:(S)-4-(4'-氯联苯-4-基)-4-氧代-2-(苯硫基甲基)丁酸
- CBNumber:CB0506810
- 分子式:C23H19ClO3S
- 分子量:410.91
- MOL File:179545-77-8.mol
- 熔点 :110-110.5°C
- 沸点 :620.1±55.0 °C(Predicted)
- 密度 :1.33±0.1 g/cm3(Predicted)
- 储存条件 :Sealed in dry,2-8°C
- 溶解度 :Acetone (Slightly), Chloroform (Slightly), Ethyl Acetate (Slightly)
- 形态 :Solid
- 酸度系数(pKa) :4.01±0.23(Predicted)
- 颜色 :White to Off-White
- CAS 数据库 :179545-77-8
(S)-4-(4'-氯联苯-4-基)-4-氧代-2-(苯硫基甲基)丁酸性质、用途与生产工艺
- 生物活性 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。
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靶点
MMP-2
11 nM (Ki)
MMP-3
143 nM (Ki)
MMP-9
301 nM (Ki)
MMP-13
1470 nM (Ki)
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体外研究
Tanomastat (BAY 12-9566) (1-10000 nM; 6 hours) prevents matrix invasion by endothelial cells in a concentration-dependent manner (IC 50 =840 nM), without affecting cell proliferation.
Tanomastat (BAY 12-9566) (1-00 µM; 5 days) inhibits tubule formation completely at 15-100 µM. -
体内研究
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.
Animal Model: Six- to eight-week-old female BALB/c nude mice (bearing MDA-MB-435 cells) 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. -
用途
A Matrix Metalloproteinase inhibitor. An angiogenesis inhibitor. Optical Rotation +82℃ (C 1.5 acetone).
- 公司名称：TORONTO
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- 国家：加拿大
- 产品数：6038
- 优势度：71
