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Formula | C29H27F5N2O6S |
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Molecular Weight | 626.59 | CAS No. | 1334493-07-0 | ||||
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (159.59 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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. | ||
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Targets |
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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]. |
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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]. |
Animal Study: |
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Data from [Data independently produced by , , J Immunol, 2018, 200(12):4102-4116]
Tumor cell senescence-induced macrophage CD73 expression is a critical metabolic immune checkpoint in the aging tumor microenvironment [ Theranostics, 2024, 14(3):1224-1240] | PubMed: 38323313 |
Extracellular-vesicle-packaged S100A11 from osteosarcoma cells mediates lung premetastatic niche formation by recruiting gMDSCs [ Cell Rep, 2024, 43(2):113751] | PubMed: 38341855 |
JAK3/STAT5 signaling-triggered upregulation of PIK3CD contributes to gastric carcinoma development [ J Cell Commun Signal, 2024, 18(1):e12017] | PubMed: 38545256 |
Synthesis and evaluation of [18F]FBNAF, a STAT3-targeting probe, for PET imaging of tumor microenvironment [ EJNMMI Radiopharm Chem, 2024, 9(1):46] | PubMed: 38834900 |
Targeting FLT3-TAZ signaling to suppress drug resistance in blast phase chronic myeloid leukemia [ Mol Cancer, 2023, 10.1186/s12943-023-01837-4] | PubMed: 37932786 |
Different niches for stem cells carrying the same oncogenic driver affect pathogenesis and therapy response in myeloproliferative neoplasms [ Nat Cancer, 2023, 4(8):1193-1209] | PubMed: 37550517 |
Different niches for stem cells carrying the same oncogenic driver affect pathogenesis and therapy response in myeloproliferative neoplasms [ Nat Cancer, 2023, 4(8):1193-1209] | PubMed: 37550517 |
Chemotherapy-driven increases in the IL6/STAT3/Mcl-1 axis reduce the chemosensitivity of osteosarcoma cells [ Research Square, 2023, 10.21203/rs.3.rs-2885132/v1] | PubMed: none |
Optimized human intestinal organoid model reveals interleukin-22-dependency of paneth cell formation [ Cell Stem Cell, 2022, 29(9):1333-1345.e6] | PubMed: 36002022 |
UHMK1 aids colorectal cancer cell proliferation and chemoresistance through augmenting IL-6/STAT3 signaling [ Cell Death Dis, 2022, 13(5):424] | PubMed: 35501324 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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