Home JAK/STAT STAT inhibitor BP-1-102

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BP-1-102 STAT inhibitor

Cat.No.S7769

BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor, binds Stat3 with an affinity Kd of 504 nM and blocks Stat3-phospho-tyrosine (pTyr) peptide interactions and Stat3 activation at 4-6.8 μM.
BP-1-102 STAT inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 626.59

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Quality Control

Batch: Purity: 99.72%
99.72

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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
OCI-AML2 cells Cytotoxicity assay 72 h Cytotoxicity against human OCI-AML2 cells assessed as cell viability after 72 hrs by MTS assay, IC50=10 μM
MDA468 cells Cytotoxicity assay Cytotoxicity against human MDA468 cells after 72 hrs by MTS assay, EC50=10.9 μM
JJN-3 cells Cytotoxicity assay 72 h Cytotoxicity against human JJN-3 cells after 72 hrs by MTS assay, EC50=16.7 μM
DU145 cells Cytotoxicity assay 72 h Cytotoxicity against human DU145 cells after 72 hrs by MTS assay, EC50=22.7 μM
147EF cells Function assay 0.1-1 μM 3 h Inhibition of AKT phosphorylation in human 147EF cells at 0.1 to 1 uM after 3 hrs by Western blotting analysis
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (159.59 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 626.59 Formula

C29H27F5N2O6S

 Storage (From the date of receipt)
CAS No. 1334493-07-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN(CC(=O)N(CC1=CC=C(C=C1)C2CCCCC2)C3=CC(=C(C=C3)C(=O)O)O)S(=O)(=O)C4=C(C(=C(C(=C4F)F)F)F)F

Mechanism of Action

Targets/IC50/Ki
STAT3
504 nM(Kd)
In vitro

BP-1-102 binds Stat3 with an affinity (KD) of 504 nM, blocks Stat3-phospho-tyrosine (pTyr) peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. This compound-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, which is identified as a Stat3 target gene that promotes Stat3-mediated breast tumor cell migration and invasion. Treatment of breast cancer cells with this chemical further blocks Stat3–NF-κB cross-talk, the release of granulocyte colony-stimulating factor, soluble intercellular adhesion molecule 1, macrophage migration-inhibitory factor/glycosylation-inhibiting factor, interleukin 1 receptor antagonist, and serine protease inhibitor protein 1, and the phosphorylation of focal adhesion kinase and paxillin, while enhancing E-cadherin expression. It inhibits Stat3 DNA-binding activity in vitro, with an IC50 value of 6.8±0.8 μM and preferentially inhibits Stat3-Stat3, over Stat1-Stat3, Stat1-Stat1, or Stat5-Stat5 DNA-binding activity. This agent has little or no effect on phospho-Shc, Src, Jak-1/2, Erk1/2, or Akt levels.
In vivo

Intravenous or oral gavage delivery of BP-1-102 furnishes micromolar or microgram levels in tumor tissues and inhibits growth of human breast and lung tumor xenografts and modulates Stat3 activity, Stat3 target genes, and soluble factors in vivo. This compound selectively suppresses growth, survival, malignant transformation, migration, and invasion of malignant cells harboring constitutively active stat3. It is detectable at micromolar concentrations in plasma and in micrograms in tumor tissues.
References

Applications

Methods Biomarkers Images PMID
Western blot p-STAT3 / STAT3 c-Myc / Cyclin D1 / Survivin
S7769-WB1
30720080

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