Napabucasin
(Synonyms: 2-乙酰基呋喃并-1,4-萘醌,BBI608) 目录号 : GC11474
An inhibitor of cancer cell stemness
Cas No.:83280-65-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
PCa cell lines (22RV1and PC-3) |
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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. |
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Reacting condition |
1 μmol/L, 48, 72, 96, and 120 h |
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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]: | |
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Animal models |
Immunodeficient nude mouse bearing PC-3 cells or 22RV1 cells |
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Dosage form |
Intraperitoneal injection, 40 mg/kg, every 3 days |
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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. |
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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. |
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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. | |
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.
| 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。 |
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| 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。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。