BP-1-102
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406523

CAS#: 1334493-07-0

Description: BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor. BP-1-102 binds Stat3 with an affinity (K(D)) 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.


Chemical Structure

img
BP-1-102
CAS# 1334493-07-0

Theoretical Analysis

MedKoo Cat#: 406523
Name: BP-1-102
CAS#: 1334493-07-0
Chemical Formula: C29H27F5N2O6S
Exact Mass: 626.151
Molecular Weight: 626.59
Elemental Analysis: C, 55.59; H, 4.34; F, 15.16; N, 4.47; O, 15.32; S, 5.12

Price and Availability

Size Price Availability Quantity
5.0mg USD 85.0 Ready to ship
10.0mg USD 150.0 Ready to ship
25.0mg USD 250.0 Ready to ship
50.0mg USD 450.0 Ready to ship
100.0mg USD 750.0 Ready to ship
200.0mg USD 1350.0 Ready to ship
500.0mg USD 2650.0 Ready to ship
1.0g USD 3650.0 2 Weeks
Click to view more sizes and prices
Bulk inquiry

Synonym: BP-1-102; BP1-102; BP 1-102; BP1102; BP-1102; BP 1102.

IUPAC/Chemical Name: 4-(N-(4-cyclohexylbenzyl)-2-(2,3,4,5,6-pentafluoro-N-methylphenylsulfonamido)acetamido)-2-hydroxybenzoic acid

InChi Key: WNVSFFVDMUSXSX-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H27F5N2O6S/c1-35(43(41,42)28-26(33)24(31)23(30)25(32)27(28)34)15-22(38)36(19-11-12-20(29(39)40)21(37)13-19)14-16-7-9-18(10-8-16)17-5-3-2-4-6-17/h7-13,17,37H,2-6,14-15H2,1H3,(H,39,40)

SMILES Code: O=C(O)C1=CC=C(N(CC2=CC=C(C3CCCCC3)C=C2)C(CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O)=O)C=C1O

Appearance: white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Biological target: BP-1-102 is an inhibitor of transcription factor Stat3 with an IC50 of 6.8 μM.
In vitro activity: AGS and HGC-27 cells were exposed to various concentrations of BP-1-102 to evaluate its effect on the proliferation of GC (gastric cancer) cells using a CCK8 assay. Compared with the control group, BP-1-102 treatment dose-dependently suppressed the proliferation of AGS cells (Fig. 2A) but had no such inhibitory effect on HGC-27 cells (Fig. 2B). Furthermore, the results of the colony formation assays showed that the BP-1-102-treated AGS cells formed smaller and fewer colonies compared with those in the control group. BP-1-102 was less effective towards HGC-27 cells than AGS cells (Fig. 2C and D). These results indicated that BP-1-102 exerted a tumor suppressive role in GC cells lines and that this effect was enhanced by high expression levels of p-STAT3 (Y705). Reference: Mol Med Rep. 2019 Apr;19(4):2698-2706. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6423579/
In vivo activity: The role of BP-1-102, an oral bioavailable STAT3 inhibitor, in IA (intracranial aneurysms) was investigated. An IA mouse model was constructed by injecting elastase into the cerebrospinal fluid with simultaneous induction of hypertension by deoxycorticosterone acetate (DOCA) implantation. The results showed that the proportion of IA rupture in mice after BP-1-102 administration was significantly reduced, and the survival time was significantly extended. Further research showed that compared with the Vehicle group, the proportion of macrophages infiltrated at the aneurysm and the expression of pro-inflammatory cytokines in the BP-1-102 administration group were significantly reduced. Reference: J Drug Target. 2021 Mar 8:1-25. https://www.tandfonline.com/doi/abs/10.1080/1061186X.2021.1895817?journalCode=idrt20

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 15.0 23.9

Preparing Stock Solutions

The following data is based on the product molecular weight 626.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Jiang X, Tang J, Wu M, Chen S, Xu Z, Wang H, Wang H, Yu X, Li Z, Teng L. BP‑1‑102 exerts an antitumor effect on the AGS human gastric cancer cell line through modulating the STAT3 and MAPK signaling pathways. Mol Med Rep. 2019 Apr;19(4):2698-2706. doi: 10.3892/mmr.2019.9892. Epub 2019 Jan 24. PMID: 30720080; PMCID: PMC6423579. 2. Wu QY, Cheng Z, Zhou YZ, Zhao Y, Li JM, Zhou XM, Peng HL, Zhang GS, Liao XB, Fu XM. A novel STAT3 inhibitor attenuates angiotensin II-induced abdominal aortic aneurysm progression in mice through modulating vascular inflammation and autophagy. Cell Death Dis. 2020 Feb 18;11(2):131. doi: 10.1038/s41419-020-2326-2. PMID: 32071300; PMCID: PMC7028955. 3. Jiang Z, Huang J, You L, Zhang J. BP-1-102, a STAT3 inhibitor, reduces intracranial aneurysm rupture and suppresses inflammatory responses in a mouse model. J Drug Target. 2021 Mar 8:1-25. doi: 10.1080/1061186X.2021.1895817. Epub ahead of print. PMID: 33682559.
In vitro protocol: 1. Jiang X, Tang J, Wu M, Chen S, Xu Z, Wang H, Wang H, Yu X, Li Z, Teng L. BP‑1‑102 exerts an antitumor effect on the AGS human gastric cancer cell line through modulating the STAT3 and MAPK signaling pathways. Mol Med Rep. 2019 Apr;19(4):2698-2706. doi: 10.3892/mmr.2019.9892. Epub 2019 Jan 24. PMID: 30720080; PMCID: PMC6423579. 2. Wu QY, Cheng Z, Zhou YZ, Zhao Y, Li JM, Zhou XM, Peng HL, Zhang GS, Liao XB, Fu XM. A novel STAT3 inhibitor attenuates angiotensin II-induced abdominal aortic aneurysm progression in mice through modulating vascular inflammation and autophagy. Cell Death Dis. 2020 Feb 18;11(2):131. doi: 10.1038/s41419-020-2326-2. PMID: 32071300; PMCID: PMC7028955.
In vivo protocol: 1. Jiang Z, Huang J, You L, Zhang J. BP-1-102, a STAT3 inhibitor, reduces intracranial aneurysm rupture and suppresses inflammatory responses in a mouse model. J Drug Target. 2021 Mar 8:1-25. doi: 10.1080/1061186X.2021.1895817. Epub ahead of print. PMID: 33682559. 2. Wu QY, Cheng Z, Zhou YZ, Zhao Y, Li JM, Zhou XM, Peng HL, Zhang GS, Liao XB, Fu XM. A novel STAT3 inhibitor attenuates angiotensin II-induced abdominal aortic aneurysm progression in mice through modulating vascular inflammation and autophagy. Cell Death Dis. 2020 Feb 18;11(2):131. doi: 10.1038/s41419-020-2326-2. PMID: 32071300; PMCID: PMC7028955.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

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

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Zhang X, Yue P, Page BD, Li T, Zhao W, Namanja AT, Paladino D, Zhao J, Chen Y, Gunning PT, Turkson J. Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts. Proc Natl Acad Sci U S A. 2012 Jun 12;109(24):9623-8. doi: 10.1073/pnas.1121606109. Epub 2012 May 23. PubMed PMID: 22623533; PubMed Central  PMCID: PMC3386073.



Additional Information