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Tanomastat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Tanomastat图片
CAS NO:179545-77-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
BAY 12-9566
产品介绍
Tanomastat (BAY 12-9566) 是一种口服生物有效的含锌羧基的非肽联苯基质金属蛋白酶(MMPs)抑制剂。抑制MMP-2、MMP-3、MMP-9、MMP-13 的Ki值分别为 11、143、301 和 1470 nM。Tanomastat 在几种实验性肿瘤模型中具有抗侵袭和抗转移活性。
生物活性

Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenylmatrix metalloproteinases(MMPs)inhibitor with a Zn-binding carboxyl group. TheKivalues are 11, 143, 301, and 1470 nM forMMP-2,MMP-3,MMP-9,MMP-13respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models[1][2][3].

IC50& Target[1]

MMP-2

11 nM (Ki)

MMP-3

143 nM (Ki)

MMP-9

301 nM (Ki)

MMP-13

1470 nM (Ki)

体外研究
(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].

体内研究
(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.
分子量

410.91

性状

Solid

Formula

C23H19ClO3S

CAS 号

179545-77-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month