BP-1-102

SKU: orb1303866

Description

BP-1-102 is a potent and selective oral STAT3 inhibitor that disrupts STAT3 activation by binding with high affinity (Kd: 504 nM). It effectively suppresses the growth, survival, and invasion of STAT3-dependent cancer cells in vitro by downregulating key oncogenic targets like c-Myc and VEGF, and has demonstrated antitumor efficacy in vivo models.

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1334493-07-0
• MW: 626.59
• Purity: 99.81% (May vary between batches)
• Formula: C₂₉H₂₇F₅N₂O₆S
• SMILES: CN(CC(=O)N(Cc1ccc(cc1)C1CCCCC1)c1ccc(C(O)=O)c(O)c1)S(=O)(=O)c1c(F)c(F)c(F)c(F)c1F
• Target: STAT
• Solubility: DMSO:93 mg/mL (148.42 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.27 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  STAT3:504 nM(Kd)
• 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.
• In Vitro:
  BP-1-102 binds Stat3 with an affinity (KD) of 504 nM, inhibits Stat3-phospho-tyrosine (pTyr) peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits the growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrant Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8, a Stat3 target gene promoting breast tumor cell migration and invasion. Treatment of breast cancer cells with BP-1-102 also blocks Stat3–NF-κB cross-talk, the release of several cytokines, 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 of 6.8±0.8 μM and preferentially inhibits Stat3-Stat3 over other Stat dimer DNA-binding activities. BP-1-102 exerts minimal or no effect on phospho-Shc, Src, Jak-1/2, Erk1/2, or Akt levels.
• Cell Research:
  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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BP 1 102, BP1102, BP-1-102, Inhibitor, inhibit, STAT, STAT3

Compound Identifiers

PubChem CID

53388144