179545-76-7

179545-76-7 structure

Name: (Rac)-Tanomastat
Chemical Name: (Rac)-Tanomastat
CAS Number: 179545-76-7
Molecular Formula: C₂₃H₁₉ClO₃S
Molecular Weight: 410.91
Catalog: Signaling Pathways Metabolic Enzyme/Protease MMP
Create Date: 2022-10-18 06:30:32
Modify Date: 2024-01-10 12:02:55
(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[1][2][3].

Name	(Rac)-Tanomastat

Description	(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[1][2][3].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> MMP
Target	MMP-2:11 nM (Ki) MMP-3:143 nM (Ki) MMP-9:301 nM (Ki) MMP-13:1470 nM (Ki)
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].
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]. 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.
References	[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. [4]. Harold Clinton Eugene Kluender, et al. Substituted 4-biarylbutyric or 5-biarylpentanoic acids and derivatives as matrix metalloprotease inhibitiors. WO1996015096A1.

Molecular Formula	C₂₃H₁₉ClO₃S
Molecular Weight	410.91

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