品牌分类
品牌咨询
联系方式
公司地址
苏州工业园区生物纳米园A4#216
联系电话
4000-520-616 / 18915418616
传真号码
0512-67156496
电子邮箱
info@ebiomall.com
公司网址
https://www.ebiomall.com
蚂蚁淘在线 / 品牌中心 / Xcess / Xcessbio/GDC-0449 (Vismodegib), Hedgehog Antagonist -Xcessbio Biosciences Inc/2 mg solid/M60034-2s
商品描述
Details
Xcess新型高效神经保护分子P7C32014年10月13日03:55 | 新闻印刷版刚刚在上个月的Cell中发表，最近关于神经保护小分子P7C3的 MOA研究具有广泛的体外和体内活性，为研究共享其他常见组织的神经系统疾病，损伤，发育和退行性疾病提供了新的令人兴奋的机会机制。 P7C3 是直接从体内神经发生筛选中鉴定出的无毒，稳定且可口服生物利用的合成小分子。它可以保护齿状回中的新生神经元，并刺激新神经元的生长。它还可以增强老年大鼠的学习和记忆能力。在爆炸介导的创伤性脑损伤（TBI）的啮齿动物模型中，P7C3还可以在损伤后，在神经元细胞死亡发生之前保持轴突的完整性。MOA研究表明P7C3可以结合烟酰胺磷酸核糖基转移酶（NAMPT），这是一种将烟酰胺转化为烟酰胺腺嘌呤二核苷酸（NAD）的限速酶。将活性P7C3化学物质施用至用阿霉素处理的细胞（诱导NAD耗竭），可导致细胞内NAD水平反弹，并免受阿霉素介导的毒性的影响。 如何订购： Xcess Biosciences是一家领先的试剂和服务公司，提供10 mM DMSO溶液和以克计的固体形式的化合物。请访问我们的网站以获取订单信息和其他创新产品。特别是Xcess Biosciences继续向我们的表观遗传调节剂工具箱 （现在我们提供72种独特的化合物）和 泛素调节剂工具箱 （现在我们提供15种独特的化合物）中添加了更多新颖的小分子化学探针 。
Product Information
| Chemical Name: | 2-Chloro-N-(4-chloro-3-pyridin-2-ylphenyl)-4-methylsulfonylbenzamide |
| Molecular Weight: | 421.30 |
| Formula: | C19H14Cl2N2O3S |
| Purity: | ≥98% |
| CAS#: | 879085-55-9 |
| Solubility: | DMSO up to 100 mM |
| Storage: | Powder:4oC 1 year DMSO:4oC3 month-20oC 1 year |
Biological Activity:
Vismodegib (GDC-0449) is a potent and specific hedgehog pathway inhibitor with an IC50 of 3 nM. It has been approved by FDA to treat BCC, and also in multiple clinical trials to treat advanced solid tumors. It blocks the activities of the Hedgehog-ligand cell surface receptors PTCH and/or SMO and suppressing Hedgehog signaling. It prevents multiple ATP-binding cassette (ABC) transporters. GDC-0449 also exhibited efficacy in medulloblastoma animal models and primary pancreatic cancer xenograft models. It was shown to inhibit cell growth in cisplatin-resistant lung cancer cells.
How to Use:
- In vitro: GDC-0449 was used at 5-10 µM concentration in the cellular assays.
- In vivo: GDC-0449 was dosed orally 12.5 mg/kg twice per day (lowest dose), up to 100 mg/kg twice per day (formulated as a suspension in 0.5% methylcellulose, 0.2% Tween-80 (MCT))
Reference:
- 1. Robarge KD, et al. GDC-0449-a potent inhibitor of the hedgehog pathway. (2009) Bioorg Med Chem Lett. 19(19):5576-81.
- 2. Yauch RL, et al. Smoothened mutation confers resistance to a Hedgehog pathway inhibitor in medulloblastoma. (2009) Science 326(5952):572-4.
- 3. LoRusso PM, et al. Phase I trial of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with refractory, locally advanced or metastatic solid tumors. (2011) Clin Cancer Res.17(8):2502-11
- 4. Giannetti AM, et al. Identification, characterization, and implications of species-dependent plasma protein binding for the oral Hedgehog pathway inhibitor vismodegib (GDC-0449). (2011) J Med Chem. 54(8):2592-601
- 5. Lorusso PM, et al. Pharmacokinetic dose-scheduling study of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with locally advanced or metastatic solid tumors. (2011) Clin Cancer Res. 17(17):5774-82
- 6. Philips GM, et al. Hedgehog signaling antagonist promotes regression of both liver fibrosis and hepatocellular carcinoma in a murine model of primary liver cancer.(2011) PLoS One. 6(9):e23943.
- 7. Metcalfe C, et al. Hedgehog fights back: mechanisms of acquired resistance against Smoothened antagonists. (2011) Cancer Res. 71(15):5057-61.
- 8. Singh BN, et al. Hedgehog signaling antagonist GDC-0449 (Vismodegib) inhibits pancreatic cancer stem cell characteristics: molecular mechanisms. (2011) PLoS One. 6(11):e27306
- 9. Tian F, et al. The hedgehog pathway inhibitor GDC-0449 alters intracellular Ca2+ homeostasis and inhibits cell growth in cisplatin-resistant lung cancer cells. (2012) Anticancer Res. 32(1):89-94
- Product Specification:
GDC-0449_spec.pdf- Product MSDS:
- GDC-0449_MSDS.pdf
Products are for research use only. Not for human use.
