Name: Napabucasin (BBI608)
Brand: Selleck Chemicals
SKU: S7977
Rating: 5 (32 reviews)

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Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.72%

99.72

Relaterade mål	EGFR JAK Pim
Övrigt STAT Inhibitorer	Stattic NSC 74859 (S3I-201) Cryptotanshinone (Tanshinone C) C188-9 (TTI-101) SH-4-54 BP-1-102 AS1517499 HO-3867 Nifuroxazide Homoharringtonine (HHT)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Cellinjer	Analystyp	Koncentration	Inkubationstid	Aktivitetsbeskrivning	PMID
human DU145 cells	Function assay		72 h	Anticancer activity against human DU145 cells after 72 hrs by XTT assay, IC50=0.02304 μM	18829316
human HaCaT cells	Function assay		48 h	Antihyperproliferative activity against human HaCaT cells after 48 hrs by phase contrast microscopy, IC50=0.5 μM	22845014
human HaCaT cells	Proliferation assay			Antiproliferative activity against human HaCaT cells, IC50=0.5 μM	10479319
KB cells	Cytotoxicity assay			Effective cytotoxic dose against KB cells was evaluated, ED50=4.2 μM	9873618
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.34 μM.	28558333
HepG2	Cytotoxicity assay		72 hrs	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.66 μM.	28558333
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.74 μM.	28558333
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay, IC50 = 1 μM.	30003778
MDA-MB-231	Function assay		4 hrs	Inhibition of STAT3 phosphorylation at Y705 in human MDA-MB-231 cells assessed as reduction in ratio of phosphorylated STAT3 to total STAT3 level after 4 hrs by HTRF assay, EC50 = 1.9 μM.	30003778
MDA-MB-231	Function assay		4 hrs	Inhibition of STAT3 phosphorylation at Y705 in human MDA-MB-231 cells after 4 hrs by HTRF assay, EC50 = 2 μM.	30003778
MDA-MB-231	Antiproliferative assay		48 hrs	Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay, IC50 = 2.1 μM.	30003778
HepG2	Antiproliferative assay		48 hrs	Antiproliferative activity against human HepG2 cells after 48 hrs by CCK-8 assay, IC50 = 10.2 μM.	29604543
L02	Antiproliferative assay		48 hrs	Antiproliferative activity against human L02 cells after 48 hrs by CCK-8 assay, IC50 = 18.7 μM.	29604543
MDA-MB-231	Function assay	100 uM	1 hr	Binding affinity to STAT3 in human MDA-MB-231 cells at 100 uM treated for 1 hr followed by thermolysin addition measured after 30 mins by DARTS-Western blot analysis	30003778
MDA-MB-231	Function assay	5 umol/L	24 hrs	Induction of superoxide generation in human MDA-MB-231 cells at 5 umol/L measured after 24 hrs by DHE staining based flow cytometry	30003778
MDA-MB-231	Function assay	5 umol/L	24 hrs	Induction of superoxide generation in human MDA-MB-231 cells at 5 umol/L measured after 24 hrs in presence of NQO1 inhibitor dicoumarol by DHE staining based flow cytometry	30003778
Klicka för att visa mer experimentella data för cellinjer

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt	240.21	Formel	C₁₄H₈O₄	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	83280-65-3	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel
Synonymer	BBI608			Smiles	CC(=O)C1=CC2=C(O1)C(=O)C3=CC=CC=C3C2=O

Löslighet (Solubility)

In vitro
Batch:

DMSO : 14 mg/mL (58.28 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritetsräknare

Massa	Koncentration	Volym	Molekylvikt
=	×	×

Utspädningsräknare Molekylviktsräknare

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	0.250mg/ml (1.04mM)	Taking the 1 mL working solution as an example, add 100 μL of 2.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

Dosering: mg/kg Djurens medelvikt: g Doseringsvolym per djur:μL Antal djur:

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH₂O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (Mechanism of Action)

Targets/IC₅₀/Ki	Stat3
In vitro	Napabucasin downregulates stemness gene expression driven by Stat3 and cancer stemness properties, and effectively inhibits self-renewal of stemness-high cancer cells with IC50 ranged from 0.291~1.19 μM, on inhibition on normal stem cells.
In vivo	In mice bearing PaCa-2 xenografts, Napabucasin (20 mg/kg, i.p.) significantly inhibits tumor growth, relapse and metastasis.
Referenser	[1] https://pubmed.ncbi.nlm.nih.gov/25605917/

Applikationer (Applications)

Metoder	Biomarkörer	PMID
Western blot	CDK4 / Cyclin D1 STAT3 / β-catenin / c-Myc c-Myc / Nanog / Bmi-1 / Axl / Sox2 / Klf4 / β-catenin / Survivin	31277685
Immunofluorescence	STAT3 Cleaved caspase-3	31277685
Growth inhibition assay	Cell viability	31277685

Klinisk prövningsinformation (Clinical Trial Information)

(data från https://clinicaltrials.gov, uppdaterad den 2024-05-22)

NCT-nummer	Rekrytering	Tillstånd	Sponsor/Samarbetspartners	Startdatum	Faser
NCT03525405	Completed	ADME\|Healthy	Sumitomo Pharma America Inc.	May 18 2018	Phase 1
NCT03416816	Terminated	Neoplasms	Sumitomo Pharma America Inc.\|Syneos Health	May 15 2018	Phase 1
NCT02279719	Completed	Hepatocellular Carcinoma	Sumitomo Pharma America Inc.	December 2014	Phase 1\|Phase 2

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Napabucasin (BBI608) STAT Hämmare

Molekylvikt: 240.21

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Klinisk prövningsinformation (Clinical Trial Information)

Napabucasin (BBI608) STAT Hämmare

Molekylvikt: 240.21

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration (Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Klinisk prövningsinformation (Clinical Trial Information)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)