中文名称:

331862-41-0

中文同义词:

NOTCH抑制剂(IMR-1A);化合物IMR-1A

英文名称:

IMR-1A

英文同义词:

IMR-1A;IMR1A;IMR 1A;IMR-1A;IMR-1A, >98%;Acetic acid, 2-[2-methoxy-4-[(4-oxo-2-thioxo-5-thiazolidinylidene)methyl]phenoxy]-

CAS号:

331862-41-0

分子式:

C13H11NO5S2

分子量:

325.36

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

331862-41-0.mol

密度 

1.55±0.1 g/cm3(Predicted)

储存条件 

Inert atmosphere,2-8°C

酸度系数(pKa)

3.10±0.10(Predicted)

生物活性

IMR-1A 是IMR-1的酸性代谢产物，是一种 Notch 的有效的抑制剂，IC50值为0.5 μM，Kd值为2.9 μM。IMR-1A 具有抗肿瘤活性。

靶点

Target Value Notch (Cell-free assay) 0.5 μM Notch (Cell-free assay) 2.9 μM(Kd)

Target

Value

Notch (Cell-free assay)

0.5 μM

Notch (Cell-free assay)

2.9 μM(Kd)

体内研究

IMR-1A (2 mg/kg (i.v.) and 100 mg/kg (i.p)) exhibits low systematic plasma clearance (CL = 7 mL/min/kg) with terminal elimination half-life (T1/2) of 2.22 h following a single i.v. administration. The normal liver blood flow in mice is 90 mL/min/kg and the Vss (volume of distribution) is ~4-fold. Plasma concentrations is quantifiable up to 24 h with Tmax of 0.50 h after i.p. administration. Animal Model: Male C57 BL/6 mice Dosage: 2 mg/kg (i.v.) and 100 mg/kg (i.p) Administration: I.v. and i.p. Result: Exhibited low systematic plasma clearance (CL = 7 mL/min/kg) with terminal elimination half-life (T1/2) of 2.22 h following a single i.v. administration and plasma concentrations is quantifiable up to 24 h with Tmax of 0.50 h after i.p. administration.

Animal Model:

Male C57 BL/6 mice

Dosage:

2 mg/kg (i.v.) and 100 mg/kg (i.p)

Administration:

I.v. and i.p.

Result:

Exhibited low systematic plasma clearance (CL = 7 mL/min/kg) with terminal elimination half-life (T1/2) of 2.22 h following a single i.v. administration and plasma concentrations is quantifiable up to 24 h with Tmax of 0.50 h after i.p. administration.