中文名称:

N/A

中文同义词:

转录因子STAT3小分子抑制剂(BP-1-102);BP-1-102游离态;化合物BP-1-102

英文名称:

BP-1-102

英文同义词:

BP-1-102;4-(N-(4-Cyclohexylbenzyl)-2-(2,3,4,5,6-pentafluoro-N-methylphenylsulfonamido)acetamido)-2-hydr;STAT3 Inhibitor XVIII, BP-1-102;BP-1-102; BP1-102; BP 1-102.;4-(N-(4-cyclohexylbenzyl)-2-(2,3,4,5,6-pentafluoro-N-methylphenylsulfonamido)acetamido)-2-hydroxybenzoic acid;STAT3 Inhibitor XVIII;STAT3 INHIBITOR XVIII;BP1-102;BP 1-102;Benzoic acid, 4-[[(4-cyclohexylphenyl)methyl][2-[methyl[(2,3,4,5,6-pentafluorophenyl)sulfonyl]amino]acetyl]amino]-2-hydroxy-

CAS号:

1334493-07-0

分子式:

C29H27F5N2O6S

分子量:

626.59

EINECS号:

相关类别:

细胞生物学试剂;API

Mol文件:

1334493-07-0.mol

沸点 

749.2±70.0 °C(Predicted)

密度 

1.474±0.06 g/cm3(Predicted)

储存条件 

Inert atmosphere,Store in freezer, under -20°C

酸度系数(pKa)

3.15±0.10(Predicted)

生物活性

BP-1-102 是有口服活性的转录因子 Stat3 的小分子抑制剂，其 IC50 值为 6.8 μM。

靶点

STAT3 6.8 μM (IC 50 )

STAT3 6.8 μM (IC 50 )

体外研究

BP-1-102 binds Stat3 with an affinity K D of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro , with an IC 50 value of 6.8±0.8 μM. It blocks Stat3-phospho-tyrosine peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8.

体内研究

Mice therapeutically given BP-1-102, an orally bioavailable compound targeting STAT3/NF-kB activation and cross-talk, exhibit reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas. BP-1-102 is orally bioavailable and that the agent accumulates in tumor tissues at levels sufficient to inhibit aberrantly active Stat3 functions and inhibit tumor growth.