BP-1-102

For research use only.

Catalog No.S7769

24 publications

BP-1-102 Chemical Structure

CAS No. 1334493-07-0

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.

Selleck's BP-1-102 has been cited by 24 publications

Purity & Quality Control

Choose Selective STAT Inhibitors

Biological Activity

Description 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.
Targets
STAT3 [1]
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. 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, which is identified as a Stat3 target gene that promotes Stat3-mediated breast tumor cell migration and invasion. Treatment of breast cancer cells with BP-1-102 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. BP-1-102 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. BP-1-102 has little or no effect on phospho-Shc, Src, Jak-1/2, Erk1/2, or Akt levels[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
30M cells NGjaU2ZEgXSxdH;4bYNqfHliYYPzZZk> NXnteVNTOyCmYYnz MVvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjCzNG0h[2WubIOgZZN{\XO|ZXSgZZMh[2WubDD2bYFjcWyrdImgZYZ1\XJiMzDkZZl{KGK7IFHsZY1ieiCEbIXlJIF{e2G7LDDJR|UxRTJizszN NXjpVG5iOjR7MEC2NVI>
OCI-AML2 cells M{TpR2N6fG:2b4jpZ4l1gSCjc4PhfS=> NXG2XINoPzJiaB?= MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDPR2kuSU2OMjDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwQVExKM7:TR?= NFPqN3MzOzl4OEWwNS=>
MDA468 cells NFfMeIdEgXSxdH;4bYNqfHliYYPzZZk> MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGE1PjhiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VWyCjc4PhfUwhTUN3ME2xNE46KM7:TR?= NGj2N24zOTd6OEGzOC=>
JJN-3 cells NWLUOGk1S3m2b4TvfIlkcXS7IHHzd4F6 NYLHPVJwPzJiaB?= M2H5XGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGpLVi1|IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEWFNUC9NVYvPyEQvF2= MmfCNlE4QDhzM{S=
DU145 cells NUL5RYR4S3m2b4TvfIlkcXS7IHHzd4F6 MnnXO|IhcA>? NXixdG5TS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiRVO1NF0zOi55IN88US=> MnHFNlE4QDhzM{S=
147EF cells MWDGeY5kfGmxbjDhd5NigQ>? NHvzUFExNjFvMTFOwG0> NF\BfHc{KGh? NV24e4hTUW6qaXLpeIlwdiCxZjDBT3QheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJFE1P0WIIHPlcIx{KGG2IECuNUB1dyBzIIXNJIFnfGW{IEOgbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdiYX7hcJl{cXN? NV\kc3NnOjR7MEC2NVI>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
c-Myc / Cyclin D1 / Survivin ; 

PubMed: 30720080     


BP-1-102 time-dependently (left) and dose-dependently (right) decreased the expression of c-Myc, cyclin D1 and survivin in AGS cells. The results are representative of three independent experiments. STAT3, signal transducer and activator of transcription 3; p-, phosphorylated.

p-STAT3 / STAT3 ; 

PubMed: 30720080     


Western blot analysis of p-STAT3 and STAT3 in AGS cells following treatment with 6 µM BP-1-102 for various durations (left) or with different concentrations of BP-1-102 for 8 h (right). 

30720080
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. BP-1-102 selectively suppresses growth, survival, malignant transformation, migration, and invasion of malignant cells harboring constitutively active stat3. BP-1-102 is detectable at micromolar concentrations in plasma and in micrograms in tumor tissues[1].

Protocol

Cell Research:[1]
- Collapse
  • Cell lines: Cultured MDA-MB-231, DU145, Panc-1, and NIH 3T3/v-Src cells harboring aberrantly active Stat3 and NIH 3T3, NIH 3T3/v-Ras, mouse thymus stromal epithelial cells, TE-71, Stat3-null mouse embryonic fibroblasts (Stat3−/− MEFs), cisplatin-sensitive ovarian cancer cells, A2780S cells
  • Concentrations: 0-30 μM
  • Incubation Time: 24 h
  • Method: Proliferating cells in 6- or 96-well plates are treated once with 0–30 μM BP-1-102 for 24 h or with 10 μM BP-1-102 for up to 96 h. Viable cells are counted by trypan blue exclusion/phase-contrast microscopy or assessed by a CyQUANT Cell Proliferation Kit.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Athymic nude mice
  • Dosages: 1 or 3 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (159.59 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 626.59
Formula

C29H27F5N2O6S

CAS No. 1334493-07-0
Storage powder
in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

STAT Signaling Pathway Map

Related STAT Products

Tags: buy BP-1-102 | BP-1-102 supplier | purchase BP-1-102 | BP-1-102 cost | BP-1-102 manufacturer | order BP-1-102 | BP-1-102 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID