产品
编 号：F747078
分子式：C23H19ClO3S
分子量：410.91
分子式：C23H19ClO3S
分子量：410.91
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CAS No: 179545-76-7
产品详情
生物活性：
(Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. 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.
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.
体外研究：
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.Tanomastat (BAY 12-9566) (1-00 μM; 5 days) inhibits tubule formation completely at 15-100 μM.
(Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. 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.
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.
体外研究：
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.Tanomastat (BAY 12-9566) (1-00 μM; 5 days) inhibits tubule formation completely at 15-100 μM.
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