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Chemical Structure| 83280-65-3 Chemical Structure| 83280-65-3

Structure of Napabucasin
CAS No.: 83280-65-3

Chemical Structure| 83280-65-3

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Napabucasin (BBI608) is a STAT3 inhibitor that blocks stem cell activity in cancer cells.

Synonyms: BBI608

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Product Details of Napabucasin

CAS No. :83280-65-3
Formula : C14H8O4
M.W : 240.21
SMILES Code : O=C(C1=C2OC(C(C)=O)=C1)C3=C(C2=O)C=CC=C3
Synonyms :
BBI608
MDL No. :MFCD28155270
InChI Key :DPHUWDIXHNQOSY-UHFFFAOYSA-N
Pubchem ID :10331844

Safety of Napabucasin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Napabucasin

JAK-STAT

Isoform Comparison

Biological Activity

Target
  • STAT3

In Vitro:

Cell Line
Concentration Treated Time Description References
MiaPaCa2, AsPc1, Suit2, Panc1 cells 0.5 μM, 1.0 μM, 2.0 μM 2 hours Measured STAT3 phosphorylation levels, found reduction in STAT3 phosphorylation after Napabucasin treatment PMC6891204
Murine MDSC 1 µM 24 hours Napabucasin significantly enhanced MDSC apoptosis and the expression of CD80 and MHC class II molecules, while slightly downregulating iNOS and Arg-1. PMC8932276
CT26 cells 0.1, 0.5, 1, 2, 10 μM 24 hours To evaluate the anti-tumor effect of NAP and N3-TMPs@NAP, results showed that the survival rate of cells in the N3-TMPs@NAP group decreased with increasing concentration. PMC9893668
DLD1 and HCT116 cells 2 μM 24 hours BBI608 inhibited spherogenesis of DLD1 and HCT116 cell lines PMC4330785
U87MG cells 1, 5, 10 μM 24, 48, 72 hours Napabucasin significantly inhibited the proliferation of U87MG cells PMC6612138
LN229 cells 1, 5, 10 μM 24, 48, 72 hours Napabucasin significantly inhibited the proliferation of LN229 cells PMC6612138
Hepa1–6 cells 5 μM 32 hours Inhibition of IL-11-STAT3 signaling, reducing tumor cell proliferation PMC6711863
Pancreatic cancer cell lines 0.01 – 5 μM 6 hours Assessed cell viability, found differential sensitivity to Napabucasin across cell lines PMC6891204
C57BL/6 mouse primary hepatocytes 0.1 mM 72 hours To evaluate the effect of BBI608 on alcohol- and rmIL-6-induced Lcn2 mRNA expression, results showed that BBI608 pretreatment significantly suppressed Lcn2 mRNA expression. PMC10492032
CD44high FaDu cells 400 nM 72 hours BBI608 inhibited spherogenesis of CD44high FaDu cells PMC4330785
Human M-MDSC 0.5 µM 96 hours Napabucasin completely abrogated the suppressive capacity of human M-MDSC on T-cell proliferation. PMC8932276
CT26 cells 0.5 μM, 1 μM To detect the protein and mRNA expression levels of CD44 and BMI1, results showed that the expression levels decreased with increasing NAP concentration. PMC9893668

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Subcutaneous xenograft model of MiaPaCa2 Rosa26 or MiaPaCa2 NQO1–71 cells Oral gavage 200 mg/kg Once daily for 24 days Evaluated the effect of Napabucasin on tumor growth, found that Napabucasin significantly inhibited the growth of MiaPaCa2 Rosa26 xenografts but had no significant effect on NQO1-knockout MiaPaCa2 xenografts PMC6891204
Nude mice orthotopic glioma model intraperitoneal injection 40 mg/kg every other day, until the end of the experiment Napabucasin significantly inhibited the growth of intracranial U87MG-derived tumors PMC6612138
Mice RET transgenic melanoma mouse model Intraperitoneal injection 20 mg/kg Twice a week for 4 weeks Napabucasin significantly prolonged the survival of melanoma-bearing mice and promoted the accumulation of tumor-infiltrating antigen-presenting cells and activation of CD8+ and CD4+ T cells. PMC8932276
Mice alcohol-induced liver metastasis model intraperitoneal injection 20 mg/kg every other day for 2 weeks To evaluate the preventive effect of BBI608 on alcohol-induced liver metastasis, results showed that BBI608 pretreatment significantly suppressed alcohol-induced liver metastasis. PMC10492032
BALB/C mice CT26 colon cancer model Tail intravenous injection 20 mg/kg 14 days To evaluate the anti-tumor effect of N3-TMPs@NAP, results showed that the tumor volume and weight in the N3-TMPs@NAP group were significantly lower than those in other groups. PMC9893668
C57BL/6 mice Hepatocellular carcinoma model Intraperitoneal injection 40 mg/kg Twice per week, for specified duration Inhibition of STAT3 phosphorylation, reducing postoperative HCC recurrence PMC6711863
Nude mice pancreatic cancer xenograft model intraperitoneal injection 20 mg/kg daily for 14 days BBI608 significantly inhibited tumor growth in the pancreatic cancer xenograft model, and no tumor regrowth was observed during the posttreatment observation period PMC4330785

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01775423 Cancer, Advanced Malignancies PHASE1 COMPLETED 2015-08-06 Institute for Translational On... More >>cology Research, Greenville Hospital System, Greenville, South Carolina, 29605, United States|Ottawa Hospital Cancer Center, Ottawa, Ontario, K1H 8L6, Canada|Jewish General Hospital, Montreal, Quebec, H3T 1E2, Canada Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.16mL

0.83mL

0.42mL

20.82mL

4.16mL

2.08mL

41.63mL

8.33mL

4.16mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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