MMP-9-IN-1

中文名称:

MMP-9-IN-1

中文同义词:

英文名称:

MMP-9-IN-1

英文同义词:

MMP-9-IN-1;OUN87710;Acetamide, N-[4-(difluoromethoxy)phenyl]-2-[(1,6-dihydro-6-oxo-4-propyl-2-pyrimidinyl)thio]-

CAS号:

502887-71-0

分子式:

C16H17F2N3O3S

分子量:

369.39

EINECS号:

相关类别:

API

Mol文件:

502887-71-0.mol

储存条件 

Inert atmosphere,2-8°C

生物活性

MMP-9-IN-1 (OUN87710)是一种 matrix metalloproteinase-9 (MMP-9) 的特异性抑制剂。MMP-9-IN-1 可选择性地靶向MMP-9的血红素(PEX)域，Kd值为2.1 μM。

靶点

Target Value MMP-9 (Cell-free assay) 2.1 μM(Kd)

Target

Value

MMP-9 (Cell-free assay)

2.1 μM(Kd)

体外研究

MMP-9-IN-1 (compound 2; 100 μM; 14 hours) does not cause notable cytotoxicity. MMP-9-IN-1 (compound 2; 10 μM) significantly inhibits cell proliferation of HT-1080 and MDA-MB-435 cells. Cell Cytotoxicity Assay Cell Line: COS-1 monkey epithelial cell lines Concentration: 100 μM Incubation Time: 24 hours Result: Treatment did not cause notable cytotoxicity. Cell Proliferation Assay Cell Line: HT-1080 and MDA-MB-435 cancer cells expressing endogenous MMP-9 Concentration: 10 μM Incubation Time: 9 days Result: Significant inhibition of cell proliferation.

Cell Line:

COS-1 monkey epithelial cell lines

Concentration:

100 μM

Incubation Time:

24 hours

Result:

Treatment did not cause notable cytotoxicity.

Cell Line:

HT-1080 and MDA-MB-435 cancer cells expressing endogenous MMP-9

Concentration:

10 μM

Incubation Time:

9 days

Result:

Significant inhibition of cell proliferation.

体内研究

MMP-9-IN-1 (compound 2; 20 mg/kg; intraperitoneal and intratumoral injection alternately; 6 days/week; for 14 weeks) results in a profound delay in tumor growth in NCR-Nu mice bearing MDA-MB-435/GFP tumor. MMP-9-IN-1 inhibits cancer cell metastasis in vivo. Animal Model: 4-5 week-old female NCR-Nu mice bearing MDA-MB-435/GFP tumor Dosage: 20 mg/kg Administration: Intraperitoneal and intratumoral injection alternately; 6 days/week; for 14 weeks, Result: Resulted in a profound delay in tumor growth. Inhibited cancer cell metastasis.

Animal Model:

4-5 week-old female NCR-Nu mice bearing MDA-MB-435/GFP tumor

Dosage:

20 mg/kg

Administration:

Intraperitoneal and intratumoral injection alternately; 6 days/week; for 14 weeks,

Result:

Resulted in a profound delay in tumor growth. Inhibited cancer cell metastasis.