Tanomastat

Product NameTanomastat
CAS179545-77-8
MFC23H19ClO3S
MW410.91
EINECS
MOL File179545-77-8.mol

Chemical Properties

Melting point	110-110.5°C
Boiling point	620.1±55.0 °C(Predicted)
Density	1.33±0.1 g/cm3(Predicted)
storage temp.	Sealed in dry,2-8°C
solubility	Acetone (Slightly), Chloroform (Slightly), Ethyl Acetate (Slightly)
form	Solid
pka	4.01±0.23(Predicted)
color	White to Off-White
CAS DataBase Reference	179545-77-8

Usage And Synthesis

Chemical Properties

White Solid

Uses

A Matrix Metalloproteinase inhibitor. An angiogenesis inhibitor.Optical Rotation +82° (C 1.5 acetone).

Uses

Tanomastat is an orally available, non-peptidic inhibitor of matrix metalloproteinase-2 (MMP-2), MMP-3, and MMP-9 (Kis = 11, 143, and 301 nM, respectively). It is active in various animal models of tumor metastasis and has been used in a phase III clinical trial in pancreatic, SCLC, NSCLC, and ovarian cancer patients.

Uses

A Matrix Metalloproteinase inhibitor. An angiogenesis inhibitor. Optical Rotation +82(C 1.5 acetone)

Definition

ChEBI: Tanomastat is an organochlorine compound and a member of biphenyls.

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.

IC 50

MMP-2: 11 nM (Ki); MMP-3: 143 nM (Ki); MMP-9: 301 nM (Ki); MMP-13: 1470 nM (Ki)