(Rac)-Tanomastat
(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.
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- No. CAS: 179545-76-7
- Fòrmula: C23H19ClO3S
- Peso molecular:410.91
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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MMP-2 11 nM (Ki) |
MMP-3 143 nM (Ki) |
MMP-9 301 nM (Ki) |
MMP-13 1470 nM (Ki) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six- to eight-week-old female BALB/c nude mice (bearing MDA-MB-435 cells)[3]
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Dosage:100 mg/kg
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Administration:P.o.; daily for a 7-week period
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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.
Chemical Information
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No. CAS 179545-76-7
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Appearance Solid
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Peso molecular 410.91
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Fòrmula C23H19ClO3S
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SMILES
ClC1=CC=C(C=C1)C2=CC=C(C=C2)C(CC(CSC3=CC=CC=C3)C(O)=O)=O
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Synonyms
(Rac)-BAY 12-9566
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
Referencias
[1]. Leung D, et al. Protease inhibitors: current status and future prospects. J Med Chem. 2000 Feb 10;43(3):305-41. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(Rac)-Tanomastat Related Classifications
HY-12168B Related Classifications
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