|4-(N-(4-环己基苄基)-2-((2,3,4,5,6-五氟-N-甲苯基)磺酰氨基)乙酰氨基)-2-羟基苯甲酸|CsnPharm

CAS No.: 1334493-07-0

BP-1-102 Catalog No. CSN17200

Synonyms: BP-1-102

BP-1-102 is an orally available, small-molecule inhibitor of transcription factor STAT3.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 STAT3

Kd:504nM
描述STAT3, the protein most linked to tumorigenesis in STAT family and regarded as a target for cancer therapy, is constitutively activated in most human solid tumors and is involved in the proliferation, angiogenesis, immune evasion, and anti-apoptosis of cancer cells. BP-1-102 is a potent and selective STAT3 inhibitor with IC50 of 4.1μM (measured by fluorescence polarization), much potent to than STAT3 than Stat1 or Stat5 with IC50 values of 25-30μM. BP-1-102 could inhibit the constitutive Stat3 DNA-binding activity in MDA-MB-231, DU145, NIH-3T3/v-Src3, Panc-1 and A549 cells at concentration of 20μM for 24h and showed anti-proliferative activity dose-dependently at concentration ranging in 10-30μM for 24h. Attenuated pSTAT3-Y705 could be observed in MDA-MB-231 cells by treatment with 10μM BP-1-102 for over 1h in both cytoplasm and nuclear. Further suppression of gen expression driven STAT3, including c-Myc, Cyclin D1, Bcl-xL, Survivin and VEGF, can be observed in MDA-MB-231, DU145 and Panc-1 cells treated with 15μM BP-1-102 for 24h, as well as inhibited cell migration and invasion at concentration of 10 or 15μM for 16h accompanied by reduced KLF8 and EPSTI1 levels. Inhibition of STAT3 by 15μM BP-1-102 for 24h further blocked Stat3–NF-κB cross-talk, as shown by decreased level of nuclear pRelA and total RelA, G-CSF, sICAM, and MIF/GIF. Both oral administration every day and intravenous injection 2 or 3 days with 3mg/kg BP-1-102 suppressed tumor growth in mice bearing MDA-MB-231. Intravenous injection with 3mg/kg BP-1-102 could significantly inhibit tumor growth in mice bearing A549 cells.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
147EF cells	0.1-1 μM	Function assay	3 h	Inhibition of AKT phosphorylation in human 147EF cells at 0.1 to 1 uM after 3 hrs by Western blotting analysis	24900612
30M cells	-	Cytotoxicity assay	3 days	Cytotoxicity against human 30M cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=2 μM	24900612
DU145 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human DU145 cells after 72 hrs by MTS assay, EC50=22.7 μM	21788134

更多
动物研究
剂量
Mice: 1 mg/kg - 3 mg/kg^[2] (i.v.), 3 mg/kg^[2] (p.o.)

给药途径
i.v., p.o.

动物研究
剂量	Mice: 1 mg/kg - 3 mg/kg^[2] (i.v.), 3 mg/kg^[2] (p.o.)
给药途径	i.v., p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5959 mL
- 7.9797 mL
- 15.9594 mL
- 5 mM
- 0.3192 mL
- 1.5959 mL
- 3.1919 mL
- 10 mM
- 0.1596 mL
- 0.7980 mL
- 1.5959 mL

技术信息

CAS号

1334493-07-0

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H27F5N2O6S

运输

蓝冰

分子量

626.59

别名

BP-1-102

溶解度

DMSO	270.0 mg/mL (430.9 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	5 mg/mL	clear
PO	0.5% CMC-Na	38 mg/mL	suspension

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