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Napabucasin

(Synonyms: BBI608)

27 Cited Publications

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Based on 27 publication(s) in Google Scholar

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

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Pureté: 99.94%
CAS No.: 83280-65-3
Formule: C₁₄H₈O₄
Masse moléculaire:240.21

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Napabucasin Chemical Structure

CAS No.: 83280-65-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (27)
Solvant et solubilité
- In Vitro
- In Vivo
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Activité biologique

Description

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

IC₅₀ & Target^[1]

STAT3

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Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.12 μM Compound: 6; BBI608	Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay	[PMID: 32044231]
A549	IC₅₀	0.12 μM Compound: 2	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by WST-8 method Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by WST-8 method	[PMID: 37343498]
A549	IC₅₀	0.74 μM Compound: Nap; BBI608	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 28558333]
A549	IC₅₀	6.69 μM Compound: BBI608	Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 48 hrs MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 48 hrs MTT assay	[PMID: 32631508]
AGS	IC₅₀	437 nM Compound: BBI608	Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36103247]
BC1 cell line	ED₅₀	0.4 μg/mL Compound: 5	Cytotoxicity against human BC1 cells Cytotoxicity against human BC1 cells	[PMID: 10785421]
BXPC-3	IC₅₀	1.3 μM Compound: NP	Antiproliferative activity against human BxPC-3 cells harboring ZFP91siRNA assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human BxPC-3 cells harboring ZFP91siRNA assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33506674]
BXPC-3	IC₅₀	1.4 μM Compound: NP	Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33506674]
BXPC-3	IC₅₀	1.8 μM Compound: NP	Antiproliferative activity against ZFP91 knockdown human BxPC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against ZFP91 knockdown human BxPC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33506674]
BXPC-3	IC₅₀	1962 nM Compound: 1c; BBI608	Inhibition of ATP production in human BXPC-3 cells incubated for 20 to 24 hrs by ATP assay kit method Inhibition of ATP production in human BXPC-3 cells incubated for 20 to 24 hrs by ATP assay kit method	[PMID: 36282975]
BXPC-3	IC₅₀	5306 nM Compound: 1c; BBI608	Anti-proliferative activity against human BXPC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay Anti-proliferative activity against human BXPC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay	[PMID: 36282975]
Capan-2	IC₅₀	1586 nM Compound: 1c; BBI608	Anti-proliferative activity against human Capan-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay Anti-proliferative activity against human Capan-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay	[PMID: 36282975]
Col2	ED₅₀	0.4 μg/mL Compound: 5	Cytotoxicity against human Col2 cells Cytotoxicity against human Col2 cells	[PMID: 10785421]
CT26	IC₅₀	2.5 μM Compound: Napabucasin	Antiproliferative activity against mouse CT26 cells after 72 hrs by MTT assay Antiproliferative activity against mouse CT26 cells after 72 hrs by MTT assay	[PMID: 30472602]
DLD-1	IC₅₀	944 nM Compound: NAP	Antiproliferative activity against human DLD-1 cells harboring STAT3 over activation assessed as inhibition of cell growth measured after 24 hrs by CCK-8 assay Antiproliferative activity against human DLD-1 cells harboring STAT3 over activation assessed as inhibition of cell growth measured after 24 hrs by CCK-8 assay	[PMID: 38704936]
DU-145	IC₅₀	23.04 nM Compound: 3	Anticancer activity against human DU145 cells after 72 hrs by XTT assay Anticancer activity against human DU145 cells after 72 hrs by XTT assay	[PMID: 18829316]
HaCaT	IC₅₀	0.5 μM Compound: 4a	Antihyperproliferative activity against human HaCaT cells after 48 hrs by phase contrast microscopy Antihyperproliferative activity against human HaCaT cells after 48 hrs by phase contrast microscopy	[PMID: 22845014]
HaCaT	IC₅₀	0.5 μM Compound: 6	Antiproliferative activity against human HaCaT cells Antiproliferative activity against human HaCaT cells	[PMID: 10479319]
HCT-116	IC₅₀	0.3 μM Compound: 87; BBI608	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell proliferation incubated for 72 hrs by CellTiter-Glo assay	[PMID: 33445154]
HCT-116	IC₅₀	620.32 nM Compound: NAP	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 24 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 24 hrs by CCK-8 assay	[PMID: 38704936]
HCT-15	IC₅₀	660.3 nM Compound: NAP	Antiproliferative activity against human HCT-15 cells harboring STAT3 over activation assessed as inhibition of cell growth measured after 24 hrs by CCK-8 assay Antiproliferative activity against human HCT-15 cells harboring STAT3 over activation assessed as inhibition of cell growth measured after 24 hrs by CCK-8 assay	[PMID: 38704936]
HEK293	IC₅₀	10.4 μM Compound: NP	Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33506674]
HepG2	IC₅₀	0.66 μM Compound: Nap; BBI608	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 28558333]
HepG2	IC₅₀	0.84 μM Compound: BBI608	Antiproliferative activity against human HepG2 cells overexpressed STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells overexpressed STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 32603980]
HepG2	IC₅₀	10.2 μM Compound: BBI 608	Antiproliferative activity against human HepG2 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells after 48 hrs by CCK-8 assay	[PMID: 29604543]
HepG2	IC₅₀	6.6 μM Compound: Napabucasin	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 30472602]
HT-29	IC₅₀	0.14 μM Compound: BBI608	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 48 hrs MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 48 hrs MTT assay	[PMID: 32631508]
HT-29	IC₅₀	1.6 μM Compound: Napabucasin	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 30472602]
HT-29	IC₅₀	1253.7 nM Compound: NAP	Antiproliferative activity against human HT-29 cells harboring STAT3 over activation assessed as inhibition of cell growth measured after 24 hrs by CCK-8 assay Antiproliferative activity against human HT-29 cells harboring STAT3 over activation assessed as inhibition of cell growth measured after 24 hrs by CCK-8 assay	[PMID: 38704936]
HUVEC	IC₅₀	41.28 μM Compound: BBI608	Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]
K562	IC₅₀	1 μM Compound: 6	Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay	[PMID: 30003778]
KB	ED₅₀	0.2 μg/mL Compound: 5	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 10785421]
KB	ED₅₀	1 μg/mL Compound: 1	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 7153777]
KB	ED₅₀	1 μg/mL Compound: 19	Evaluated for cytotoxicity in the KB cell culture assay Evaluated for cytotoxicity in the KB cell culture assay	[PMID: 3669007]
KB	ED₅₀	4.2 μM Compound: 2	Effective cytotoxic dose against KB cells was evaluated Effective cytotoxic dose against KB cells was evaluated	[PMID: 9873618]
L02	IC₅₀	18.63 μM Compound: Napa; BBI-608	Antiproliferative activity against human L02 cells assessed as cell viability incubated for 48 hrs measured after additional incubation with MTT Antiproliferative activity against human L02 cells assessed as cell viability incubated for 48 hrs measured after additional incubation with MTT	[PMID: 39226127]
L02	IC₅₀	18.7 μM Compound: BBI 608	Antiproliferative activity against human L02 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human L02 cells after 48 hrs by CCK-8 assay	[PMID: 29604543]
LNCaP	ED₅₀	0.2 μg/mL Compound: 5	Cytotoxicity against human LNCaP cells Cytotoxicity against human LNCaP cells	[PMID: 10785421]
M109	ED₅₀	0.9 μg/mL Compound: 5	Cytotoxicity against human M109 cells Cytotoxicity against human M109 cells	[PMID: 10785421]
MCF-10A	IC₅₀	0.54 μM Compound: BBI608	Cytotoxicity against human MCF10A cells assessed as reduction in cell viability measured after 48 hrs MTT assay Cytotoxicity against human MCF10A cells assessed as reduction in cell viability measured after 48 hrs MTT assay	[PMID: 32631508]
MCF-10A	IC₅₀	7.94 μM Compound: Napa; BBI-608	Antiproliferative activity against human MCF-10A cells assessed as cell viability incubated for 48 hrs measured after additional incubation with MTT Antiproliferative activity against human MCF-10A cells assessed as cell viability incubated for 48 hrs measured after additional incubation with MTT	[PMID: 39226127]
MCF7	EC₅₀	1.49 μM Compound: BBI-608	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CyQuant assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CyQuant assay	[PMID: 33352047]
MCF7	IC₅₀	<1 μM Compound: 6; BBI608	Inhibition of IL-6 induced STAT3 phosphorylation at Tyr705 residue in human MCF7 cells preincubated for 1 hr followed by IL-6 stimulation and measured after 1 hr by Western blot analysis Inhibition of IL-6 induced STAT3 phosphorylation at Tyr705 residue in human MCF7 cells preincubated for 1 hr followed by IL-6 stimulation and measured after 1 hr by Western blot analysis	[PMID: 32044231]
MCF7	IC₅₀	0.24 μM Compound: 6; BBI608	Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay Cytotoxicity against human MCF7 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay	[PMID: 32044231]
MCF7	IC₅₀	0.63 μM Compound: BBI608	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs MTT assay	[PMID: 32631508]
MCF7	IC₅₀	11.42 μM Compound: BBI608	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	EC₅₀	1.8 μM Compound: BBI-608	Antiproliferative activity against human MDA-MB-231 cells harbouring STAT3 assessed as reduction in cell viability at upto 10 uM incubated for 72 hrs by CyQuant assay Antiproliferative activity against human MDA-MB-231 cells harbouring STAT3 assessed as reduction in cell viability at upto 10 uM incubated for 72 hrs by CyQuant assay	[PMID: 33352047]
MDA-MB-231	IC₅₀	0.25 μM Compound: 6; BBI608	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell proliferation measured after 72 hrs by WST8 assay	[PMID: 32044231]
MDA-MB-231	IC₅₀	0.25 μM Compound: 2	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by WST-8 method Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by WST-8 method	[PMID: 37343498]
MDA-MB-231	IC₅₀	0.34 μM Compound: Nap; BBI608	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 28558333]
MDA-MB-231	IC₅₀	0.7 μM Compound: BBI608	Antiproliferative activity against human MDA-MB-231 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 32603980]
MDA-MB-231	IC₅₀	1.29 μM Compound: BBI608	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs MTT assay	[PMID: 32631508]
MDA-MB-231	IC₅₀	10.97 μM Compound: BBI608	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	2.1 μM Compound: 6	Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay	[PMID: 30003778]
MDA-MB-231	IC₅₀	2.94 μM Compound: Napa; BBI-608	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability incubated for 48 hrs measured after additional incubation with MTT Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability incubated for 48 hrs measured after additional incubation with MTT	[PMID: 39226127]
MDA-MB-231	IC₅₀	9.68 μM Compound: BBI608	Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-468	IC₅₀	1.14 μM Compound: 1; BBI608	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell growth measured after 48 hrs by CCK8 assay	[PMID: 33126089]
MDA-MB-468	IC₅₀	1.14 μM Compound: BBI608	Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as reduction in cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 32603980]
MDA-MB-468	IC₅₀	5.22 μM Compound: Napa; BBI-608	Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability incubated for 48 hrs measured after additional incubation with MTT Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability incubated for 48 hrs measured after additional incubation with MTT	[PMID: 39226127]
MGC-803	IC₅₀	871.8 nM Compound: BBI608	Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36103247]
MIA PaCa-2	IC₅₀	1.2 μM Compound: NP	Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33506674]
MKN-45	IC₅₀	3943 nM Compound: BBI608	Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 36103247]
PC-3	IC₅₀	5.25 μM Compound: Napabucasin	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 30472602]
SK-N-SH	ED₅₀	0.8 μg/mL Compound: 5	Cytotoxicity against human SK-N-SH cells Cytotoxicity against human SK-N-SH cells	[PMID: 10785421]
SW480	IC₅₀	762.7 nM Compound: NAP	Antiproliferative activity against human SW480 cells harboring STAT3 over activation assessed as inhibition of cell growth measured after 24 hrs by CCK-8 assay Antiproliferative activity against human SW480 cells harboring STAT3 over activation assessed as inhibition of cell growth measured after 24 hrs by CCK-8 assay	[PMID: 38704936]
SW626	ED₅₀	0.2 μg/mL Compound: 5	Cytotoxicity against human SW626 cells Cytotoxicity against human SW626 cells	[PMID: 10785421]
U-251	IC₅₀	2.6 μM Compound: Napabucasin	Antiproliferative activity against human U251 cells after 72 hrs by MTT assay Antiproliferative activity against human U251 cells after 72 hrs by MTT assay	[PMID: 30472602]

In Vitro

Napabucasin inhibits the expressions of stemness markers and kill stemness-high cancer cells isolated from several kinds of tumors except PCa. Napabucasin not only inhibits cell proliferation, cell motility, cell survival, colony formation ability, and tumorigenic potential of PCa cells, and increases cell apoptosis and sensitivity to docetaxel, but also effectively blocks sphere formation of PrCSCs and kill them as well as inhibits stemness gene expression. Napabucasin inhibits cell proliferation in PC-3 cells and 22RV1 cells at 48, 72, 96, and 120 h (P<0.05). Cell motility and colony formation ability are closely correlated with the process of tumor metastasis. Napabucasin significantly decreases colony formation and cell motility ability of PCa cell lines in vitro (P<0.05). The proliferation of PC-3 and 22RV1 cells treated with 1 μM Napabucasin are significantly decreased from day 2 to 5 compared with the control group (P<0.05)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Napabucasin (40 mg/kg) or Docetaxel significantly reduces xenograft tumor growth and tumor volume (TV) compared with PBS (P<0.05). Notably, while no differences are observed between the Napabucasin and the docetaxel groups in PC-3 mouse xenograft models, the TV in Napabucasin group is even lower than docetaxel group in 22RV1 mouse xenograft models (P<0.05). Additionally, Napabucasin or docetaxel also significantly reduces tumor weight compared with PBS (P<0.05)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 83280-65-3
Appearance Solid
Masse moléculaire 240.21
Formule C₁₄H₈O₄
Color Light yellow to green yellow
SMILES

O=C(C1=C2OC(C(C)=O)=C1)C3=C(C2=O)C=CC=C3
Synonyms

BBI608
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (27)

All WBIFFlow CytometryCell Migration/Invasion Assay2D/3D Cell Culture and DifferentiationIHCCell Proliferation/Viability Assay

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Journal Impact Factor

Cell

Cancer SLC6A6-mediated taurine uptake transactivates immune checkpoint genes and induces exhaustion in CD8+ T cells. [Abstract]

2024 Apr 25;187(9):2288-2304.e27. PMID: 38565142
J Clin Invest

IL20RB mediates tumoral response to osteoclastic niches and promotes bone metastasis of lung cancer. [Abstract]

2022 Oct 17;132(20):e157917. PMID: 36006737
J Exp Clin Cancer Res

Napabucasin, a novel STAT3 inhibitor suppresses proliferation, invasion and stemness of glioblastoma cells. [Abstract]

2019 Jul 5;38(1):289. PMID: 31277685

Napabucasin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Jul 5;38(1):289. [Abstract]

Proliferation of glioma cells treated with Napabucasin (0-10 μM, 24-48 h) and detected by CCK-8 assays. Half maximal inhibitory concentrations (IC₅₀) of Napabucasin in U87MG and LN229 cells were 6.4 and 5.6 μM respectively.

Napabucasin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Jul 5;38(1):289. [Abstract]

After treatment with the indicated doses of Napabucasin (0, 1, 5, and 10 μM) for 48 h, protein levels of STAT3 in U87MG and LN229 cells were evaluated by western blotting.

Napabucasin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Jul 5;38(1):289. [Abstract]

IF was used to estimate the expression of STAT3 in U87MG and LN229 cells after treatment with Napabucasin (5 μM, 48 h) (scale bar: 50 μm).

Napabucasin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Jul 5;38(1):289. [Abstract]

EdU incorporation assays showed that exposure to 5 μM Napabucasin for 48 h impaired DNA synthesis in U87MG and LN229 cells.

Napabucasin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Jul 5;38(1):289. [Abstract]

Napabucasin (5 μM, 48 h) arrests the GBM cell cycle and induces apoptosis. Cell cycle distribution of glioma cells analyzed by flow cytometry.

Napabucasin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Jul 5;38(1):289. [Abstract]

Napabucasin represses the migration and invasion of GBM cells. Representative images of the wound healing assay showing that Napabucasin treatment (1 μM, 24 h) inhibited glioma cell migration.

Napabucasin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Jul 5;38(1):289. [Abstract]

Napabucasin impairs the stemness of GBM cells. GSCs from U87MG and LN229 cells were grown in serum-free DMEM/F12 medium with or without Napabucasin (5 μM) for 10 days. Sphere morphology was photographed under a light microscope and spheroids were counted.

Napabucasin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Jul 5;38(1):289. [Abstract]

Napabucasin (40 mg/kg, intraperitoneal injection, every other day ) suppresses tumor growth in an orthotopic glioma model. Immunohistochemistry was used to assess the expression of STAT3, MMP2, Ki-67, cyclin D1, β-catenin, and c-Myc in orthotopic xenografted tumors after vehicle or Napabucasin treatments.
Cell Death Dis

Both direct and indirect suppression of MCL1 synergizes with BCLXL inhibition in preclinical models of gastric cancer. [Abstract]

2025 Mar 12;16(1):170. PMID: 40075071
Phytomedicine

β, β-Dimethylacrylshikonin potentiates paclitaxel activity, suppresses immune evasion and triple negative breast cancer progression via STAT3Y705 phosphorylation inhibition based on network pharmacology and transcriptomics analysis. [Abstract]

2023 Jun:114:154769. PMID: 36940580
Oncogene

RAF1 contributes to cell proliferation and STAT3 activation in colorectal cancer independently of microsatellite and KRAS status. [Abstract]

2023 May;42(20):1649-1660. PMID: 37020037
Cell Rep

AKTIP loss is enriched in ERα-positive breast cancer for tumorigenesis and confers endocrine resistance. [Abstract]

2022 Dec 13;41(11):111821. PMID: 36516775
Clin Transl Med

Inhibition of ROCK ameliorates pulmonary fibrosis by suppressing M2 macrophage polarisation through phosphorylation of STAT3. [Abstract]

2022 Oct;12(10):e1036. PMID: 36178087
J Med Chem

A Novel Redox Modulator Induces a GPX4-Mediated Cell Death That Is Dependent on Iron and Reactive Oxygen Species. [Abstract]

2020 Sep 10;63(17):9838-9855. PMID: 32809827
Sci Signal

The E3 ligase TRIM21 promotes progression of pancreatic ductal adenocarcinoma by down-regulating TAp63α and derepressing IL20RB. [Abstract]

2025 Jun 3;18(889):eadv4579. PMID: 40460193
Cells

STAT3 Inhibitor ODZ10117 Suppresses Glioblastoma Malignancy and Prolongs Survival in a Glioblastoma Xenograft Model. [Abstract]

2020 Mar 15;9(3):722. PMID: 32183406
Int Immunopharmacol

Acetylshikonin alleviates pulmonary fibrosis through inhibition of the STAT3 signaling pathway. [Abstract]

2026 Jan 1;168(Pt 1):115811. PMID: 41232362
Cancer Biol Ther

2026 Dec 31;27(1):2665867. PMID: 42100892
Oncol Rep

In vitro assessment of BBI608 in 2D and 3D culture models for drug repositioning in oral squamous cell carcinoma. [Abstract]

2025 Aug;54(2):97. PMID: 40539433
J Biol Chem

STAT3 activation of SCAP-SREBP-1 signaling upregulates fatty acid synthesis to promote tumor growth. [Abstract]

2024 Jun;300(6):107351. PMID: 38718868
J Nat Prod

Telocinobufagin Has Antitumor Effects in Non-Small-Cell Lung Cancer by Inhibiting STAT3 Signaling. [Abstract]

2022 Apr 22;85(4):765-775. PMID: 35200033
J Cancer

Cinobufagin exerts an antitumor effect in non-small-cell lung cancer by blocking STAT3 signaling. [Abstract]

2023 Oct 2;14(17):3309-3320. PMID: 37928418
Cancer Med

Suppression of prostate cancer progression by cancer cell stemness inhibitor napabucasin. [Abstract]

2016 Jun;5(6):1251-8. PMID: 26899963

Napabucasin purchased from MedChemExpress. Usage Cited in: Cancer Med. 2016 Jun;5(6):1251-8. [Abstract]

Representative images of colony formation assay in PCa cell lines (PC-3 and 22RV1) and histological analysis of the colony number show that the colony formation of PCa cell lines are dramatically decreased after treated with 1 μM Napabucasin for 24 h.
J Clin Med

Development of Oxadiazole-Based ODZ10117 as a Small-Molecule Inhibitor of STAT3 for Targeted Cancer Therapy. [Abstract]

2019 Nov 2;8(11):1847. PMID: 31684051
Oncotargets Ther

Bone Marrow-Derived Myofibroblasts Promote Gastric Cancer Metastasis by Activating TGF-β1 and IL-6/STAT3 Signalling Loop. [Abstract]

2020 Oct 16;13:10567-10580. PMID: 33116635
Arch Oral Biol

BBI608 induces apoptosis in mucoepidermoid carcinoma cells by targeting a post-transcriptional regulatory mechanisms of myeloid cell leukemia-1. [Abstract]

2025 Dec 4:182:106467. PMID: 41352329
Med Sci Monit

Napabucasin Attenuates Resistance of Breast Cancer Cells to Tamoxifen by Reducing Stem Cell-Like Properties. [Abstract]

2019 Nov 24;25:8905-8912. PMID: 31760402
Acta Cir Bras

Effect of napabucasin and doxorubicin via the Jak2/Stat3 signaling pathway in suppressing the proliferation of neuroblastoma cells. [Abstract]

2024 Sep 30:39:e396624. PMID: 39356934
bioRxiv

2026 Mar 26.
Universidad de Las Palmas de Gran Canaria

2023 May 24.
University of Michigan

2020 Oct.
Methods Mol Biol

Homocysteine, Thioretinaco Ozonide, and Oxidative Phosphorylation in Cancer and Aging: A Proposed Clinical Trial Protocol. [Abstract]

2019:1866:285-310. PMID: 30725425

Solvant et solubilité

In Vitro:

N-Methylpyrrolidone (NMP) : 16.67 mg/mL (69.40 mM; Need ultrasonic)

DMSO : 4.44 mg/mL (18.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Ethanol : < 1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.1630 mL

20.8151 mL

41.6302 mL

5 mM

0.8326 mL

4.1630 mL

8.3260 mL

10 mM

0.4163 mL

2.0815 mL

4.1630 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% NMP 40% PEG300 5% Tween-80 50% Saline

Solubility: 0.83 mg/mL (3.46 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 0.5 mg/mL (2.08 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 0.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 0.5 mg/mL (2.08 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 0.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.5 mg/mL (2.08 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[1]

The antiproliferative activity of Napabucasin against the PCa cell lines PC-3 and 22RV1 is examined. For cell proliferation assay, the PCa cell lines (22RV1 and PC-3) are seeded in 96-well plates at 2×10³ cells/well in a final volume of 100 μL and incubated overnight. The proliferation of PC-3 and 22RV1 cells treated with 1 μM Napabucasin. The viability of cells is determined with CellTiter 96 non-radioactive cell proliferation assay (MTS). For colony formation assay, cells are placed in a six-well plate and maintained in RPMI-1640 supplemented with 10% FBS for 2 weeks. The colonies are fixed with 4% paraformaldehyde, stained with 0.1% crystal violet and counted^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
A total of 1×10⁶ PC-3 cells or 8×10⁶ 22RV1 cells in 100 μL of PBS are injected subcutaneously into dorsal flanks of an immunodeficient nude mouse. The animals are treated i.p. with Napabucasin (40 mg/kg), Docetaxel (10 mg/kg), or PBS q3d once the tumors have reached 50 mm³. The tumor volume (TV) is calculated every 4 days according to the following standard formula: TV (mm³)=length×width²×0.5.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Zhang Y, et al. Suppression of prostate cancer progression by cancer cell stemness inhibitor napabucasin. Cancer Med. 2016 Jun;5(6):1251-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / N-Methylpyrrolidone (NMP)	1 mM	4.1630 mL	20.8151 mL	41.6302 mL	104.0756 mL
	5 mM	0.8326 mL	4.1630 mL	8.3260 mL	20.8151 mL
	10 mM	0.4163 mL	2.0815 mL	4.1630 mL	10.4076 mL
	15 mM	0.2775 mL	1.3877 mL	2.7753 mL	6.9384 mL
N-Methylpyrrolidone (NMP)	20 mM	0.2082 mL	1.0408 mL	2.0815 mL	5.2038 mL
	25 mM	0.1665 mL	0.8326 mL	1.6652 mL	4.1630 mL
	30 mM	0.1388 mL	0.6938 mL	1.3877 mL	3.4692 mL
	40 mM	0.1041 mL	0.5204 mL	1.0408 mL	2.6019 mL
	50 mM	0.0833 mL	0.4163 mL	0.8326 mL	2.0815 mL
	60 mM	0.0694 mL	0.3469 mL	0.6938 mL	1.7346 mL

Keywords

Napabucasin

27 Cited Publications

100 mg Obtenir un devis

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Napabucasin

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Small Molecule Immuno-Oncology Compound Library

Anti-Aging Compound Library

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Differentiation Inducing Compound Library

Anti-COVID-19 Compound Library

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Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

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Bioactive Compound Library Max

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Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Napabucasin

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Activité biologique

Chemical Information

Publications (27)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Napabucasin Related Classifications

HY-13919 Related Classifications