BP-1-102

Catalog No.S7769 Batch:S776901

Technical Data

Formula	C₂₉H₂₇F₅N₂O₆S
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
* <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.)

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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].

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 (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models Athymic nude mice Dosages 1 or 3 mg/kg Administration i.v.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
Athymic nude mice
Dosages
1 or 3 mg/kg
Administration
i.v.

References

[1] Zhang X, et al. Proc Natl Acad Sci U S A. 2012, 109(24):9623-8.

Customer Product Validation

: Data from [Data independently produced by , , J Immunol, 2018, 200(12):4102-4116]

Selleck's BP-1-102 has been cited by 37 publications

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
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
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
TIPE1 inhibits osteosarcoma tumorigenesis and progression by regulating PRMT1 mediated STAT3 arginine methylation [ Cell Death Dis, 2022, 13-9:815]	PubMed: 36151091
STAT3 signaling mediates peritoneal fibrosis by activating hyperglycolysis [ Am J Transl Res, 2022, 14(10):7552-7565]	PubMed: 36398234
Modulation of IL-6 Expression by KLF4-Mediated Transactivation and PCAF-Mediated Acetylation in Sublytic C5b-9-Induced Rat Glomerular Mesangial Cells [ Front Immunol, 2021, 12:779667]	PubMed: 35046941

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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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