Napabucasin (BBI608)

別名：BBI608

製品コード：S7977 純度：99.72%

Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.

CAS No. 83280-65-3

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 59500	国内在庫あり
100mg	JPY 149500	国内在庫あり
1g	JPY 445500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

文献中Selleckの製品使用例（32）

製品安全説明書

現在のバッチを見る：純度： 99.72%

99.72

Napabucasin (BBI608)関連製品

関連ターゲット	STAT1 STAT3 STAT5 STAT6	もっと見る
関連製品	Stattic NSC 74859 (S3I-201) Cryptotanshinone (Tanshinone C) SH-4-54 C188-9 (TTI-101) BP-1-102 HO-3867 Nifuroxazide AS1517499 Homoharringtonine (HHT) STAT5-IN-1 Ochromycinone (STA-21) HJC0152 APTSTAT3-9R STAT3-IN-1 SC-1 Narciclasine SH5-07 (SH-5-07) Scutellarin	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Tyrosine Kinase Inhibitor Library JAK/STAT compound library	もっと見る

シグナル伝達経路

STATシグナル伝達経路

STAT阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
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 DU145 cells	Function assay		72 h	Anticancer activity against human DU145 cells after 72 hrs by XTT assay, IC50=0.02304 μM	18829316
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
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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.

Targets

Stat3

In Vitro
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.
細胞実験	細胞株	Cancer stem cells U87-MG, U118, COLO205, DLD1, SW480, HCT116, FaDu, ACHN, SNU-475, Huh7, HepG2, H1975, A549, H460, CAOV-3, SW-626, PaCa2.
	濃度	~2 μM
	反応時間	72 h
	実験の流れ	For cancer stem cells, spheres are dissociated and plated under cancer stem cell culture conditions on coated 96-well plates. After 72 h of culture, wells are dosed with the indicated compounds. Seventy-two hours or 24 h after dosing, CellTiter-Glo 2.0 is added to each well, and the luminescence is measured as described by the manufacturer. IC50 values are calculated by fitting a four parameter dose–response curve to normalized data using GraphPad Prism software. For bulk cells, cells are plated at 5,000 cells per well on 96-well plates. Twenty-four hours after plating, cells are treated with the indicated compounds. Viability is determined at 72 h as described above.
実験結果図	Methods	Biomarkers	結果図	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

In Vivo
In Vivo	In mice bearing PaCa-2 xenografts, Napabucasin (20 mg/kg, i.p.) significantly inhibits tumor growth, relapse and metastasis.
動物実験	動物モデル	Mice bearing PaCa-2 xenografts
	投与量	20 mg/kg
	投与経路	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考
https://pubmed.ncbi.nlm.nih.gov/25605917/

参考

https://pubmed.ncbi.nlm.nih.gov/25605917/

化学情報

分子量	240.21	化学式	C₁₄H₈O₄
CAS No.	83280-65-3	SDF	Download Napabucasin (BBI608) SDFをダウンロードする
Smiles	CC(=O)C1=CC2=C(O1)C(=O)C3=CC=CC=C3C2=O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 14 mg/mL ( (58.28 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.				投与溶液組成計算機
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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	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.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

* 大学・企業名 大学・企業名を記入してください

* 名前 名前を記入してください

* 電子メール 電子メール・アドレスを記入してください 有効なメールアドレスを入力してください

電話番号

* 内容 お問い合わせ内容をご入力ください

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):