产品说明书

BP-1-102

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Chemical Structure| 1334493-07-0 同义名 : -
CAS号 : 1334493-07-0
货号 : A772321
分子式 : C29H27F5N2O6S
纯度 : 99%+
分子量 : 626.591
MDL号 : MFCD29477477
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(55.86 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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

生物活性
靶点

  • STAT3

    STAT3, Kd:504 nM
描述 BP-1-102 binds to Stat3 with an affinity KD of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro, with an IC50 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 KLF-8[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.60mL

0.32mL

0.16mL

7.98mL

1.60mL

0.80mL

15.96mL

3.19mL

1.60mL
参考文献

[1]Zhang X, et al. Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts. Proc Natl Acad Sci U S A. 2012 Jun 12;109(24):9623-8.

[2]De Simone V, et al. Th17-type cytokines, IL-6 and TNF-α synergistically activate STAT3 and NF-kB to promote colorectal cancer cell growth. Oncogene. 2015 Jul;34(27):3493-503.