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Napabucasin Sale

(Synonyms: 2-乙酰基呋喃并-1,4-萘醌,BBI608) 目录号 : GC11474

An inhibitor of cancer cell stemness

Napabucasin Chemical Structure

Cas No.:83280-65-3

规格 价格 库存 购买数量
5mg
¥662.00
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25mg
¥1,953.00
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100mg
¥4,253.00
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500mg
¥11,813.00
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1g
¥15,593.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

PCa cell lines (22RV1and PC-3)

Preparation method

Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1 μmol/L, 48, 72, 96, and 120 h

Applications

In PCa cell lines PC-3 and 22RV1, Napabucasin (1 μM) inhibited cell proliferation, cell motility, cell survival, colony formation ability and induced cell apoptosis. Napabucasin increased the sensitivity of PCa cells to Docetaxel. Napabucasin treatment decreased the stemness-high cancer cells in PC-3 and 22RV1 cells. Napabucasin obviously inhibited both the SP cells from 22RV1 cells and CD133+/CD44+ cells from PC-3 cells as well as spheres from PC-3 and 22RV1 cells. In PC-3 stemness-high cancer cells, Napabucasin significantly decreased mRNA expression of Nanog, Klf4, survivin, and β-catenin.

Animal experiment [1]:

Animal models

Immunodeficient nude mouse bearing PC-3 cells or 22RV1 cells

Dosage form

Intraperitoneal injection, 40 mg/kg, every 3 days

Application

Napabucasin significantly suppressed the tumor growth on prostate cancer (PCa) mouse xenograft models. Treatment with napabucasin resulted in inhibition of spherogenesis with numbers of spheres significantly decreased.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Zhang Y, Jin Z, Zhou H, et al. Suppression of prostate cancer progression by cancer cell stemness inhibitor napabucasin[J]. Cancer medicine, 2016, 5(6): 1251-1258.

产品描述

Target: Signal transducer and activator of transcription 3 (Stat3)

IC50: 0.395 μM (Bulk cells), 0.142 μM (Cancer stem cells)

Napabucasin, also named (BBI608), is an orally available small molecule by the ability to inhibit gene transcription of STAT3 and cancer stemness properties and suppresses spherogenesis or kills stemnesshigh cancer cells isolated from several kinds of cancer types [1]. Stat3 is critically important for maintaining cancer stemness.

In vitro: Napabucasin (1 μmol/L) not only decreased cell viability, migration, colony formation, and survival with cell cycle arrest, and increased cell apoptosis and sensitivity to docetaxel, but also obviously blocked PrCSCs sphere formation and killed them in vitro [1]. Napabucasin (1, and 2 μmol/L) decreased the expressions of stemness markers such as Nanog, Klf4, survivin, C-myc, and β-catenin [1].

In vivo: Napabucasin (40 mg/kg, i.p. injection) inhibited tumor growth on prostate cancer (PCa) mouse xenograft models, the PC-3 cells or 22RV1 cells were inoculated into nude mice. In addition, Napabucasin suppressed the self-renewal of stemness-high prostate cancer (PCa) cells in vivo [1]. Moreover, Napabucasin (20 mg/kg, i.p. injection) effectively blocked cancer relapse and metastasis in xenografted human cancers including PaCa-2 human pancreatic cancer and HT29 human colon cancer [2].

References:
1.  Zhang Y, Jin Z, Zhou H, Ou X, Xu Y, Li H, et al. Suppression of prostate cancer progression by cancer cell stemness inhibitor napabucasin. Cancer Med. 2016;5(6):1251-8.
2.  Li Y, Rogoff HA, Keates S, Gao Y, Murikipudi S, Mikule K, et al. Suppression of cancer relapse and metastasis by inhibiting cancer stemness. Proc Natl Acad Sci U S A. 2015;112(6):1839-44.

Chemical Properties

Cas No. 83280-65-3 SDF
别名 2-乙酰基呋喃并-1,4-萘醌,BBI608
化学名 2-acetylnaphtho[2,3-b]furan-4,9-dione
Canonical SMILES CC(C(O1)=CC2=C1C(C3=CC=CC=C3C2=O)=O)=O
分子式 C14H8O4 分子量 240.21
溶解度 ≥ 8.7mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 4.163 mL 20.8151 mL 41.6302 mL
5 mM 0.8326 mL 4.163 mL 8.326 mL
10 mM 0.4163 mL 2.0815 mL 4.163 mL
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