(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.
For research use only. We do not sell to patients.
- CAS No.: 179545-76-7
- Formula: C23H19ClO3S
- Molecular Weight:410.91
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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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CAS No. 179545-76-7
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Appearance Solid
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Molecular Weight 410.91
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
References
[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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