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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
| Molecular Weight: | 560.67 |
| Formula: | C29H32N6O4S |
| Purity: | >98% |
| CAS#: | 950769-58-1 |
| Solubility: | DMSO: ≥ 33 mg/mL |
| Chemical Name: | N-(5-tert-butyl-isoxazol-3-yl)-N"-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride |
| Storage: | Powder -20oC 3 years 4oC 2 yearsIn solvent -80oC 6 months-20oC 1 month |
Biological Activity:
Quizartinib is a uniquely potent and selective Flt3 inhibitor with Kd (FLT3 binding affinity) of 1.6±0.7 nM in Biochemical assay.
How to use:
In Vitro: Quizartinib (AC220) is a novel compound expressly optimized as a FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). Quizartinib inhibits FLT3-WT and FLT3-ITD autophosphorylation with IC50 of 4.2±0.3 nM and 1.1±0.1 nM, respectively. Quizartinib inhibits MV4-11 and A375 cells with IC50 of 0.56±0.3 nM and >10 000 nM, respectively. Quizartinib inhibits FLT3 with low nanomolar potency in cellular assays and is highly selective when screened against the majority of the human protein kinome[1].
In Vivo: Quizartinib (AC220) inhibits FLT3 activity in vivo, significantly extends survival in a mouse model of FLT3-ITD AML at doses as low as 1 mg/kg when dosed orally once a day, eradicates tumors in a FLT3-dependent mouse xenograft model at 10 mg/kg, and potently inhibits FLT3 activity in primary patient cells. The oral bioavailability of Quizartinib, determined in rats by comparing oral and intravenous pharmacokinetics at 3 mg/kg, is approximately 40%. A single 10 mg/kg dose of Quizartinib is administered by oral gavage, and mice are killed at 2 time points after dosing, using groups of 4 animals each. Quantitation of total FLT3 and phospho-FLT3 in tumor samples revealed time-dependent inhibition of FLT3 autophosphorylation. FLT3 activity is inhibited by 90% at 2 hours, and 40% at 24 hours after administration. The extent of inhibition therefore correlated well with the expected free Quizartinib plasma levels, based on pharmacokinetic experiments[1].
Reference:
[1]. Zarrinkar PP, et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood, 2009, 114(14), 2984-2992.
[2]. Puissant A, et al. SYK is a critical regulator of FLT3 in acute myeloid leukemia. Cancer Cell. 2014 Feb 10;25(2):226-42.
