(Rac)-Tanomastat

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(Rac)-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。

CAS NO:

179545-76-7

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

(Rac)-BAY 12-9566

产品介绍

Rac)-Tanomastat ((Rac)-BAY 12-9566) 是 Tanomastat 的外消旋体。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K_i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

(Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenylmatrix metalloproteinases(MMPs)inhibitor with a Zn-binding carboxyl group. TheK_ivalues 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

Formula

C₂₃H₁₉ClO₃S

CAS 号

179545-76-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.