FRAX597
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
FRAX597是第一类PAKs(p21-activated kinases)的小分子抑制剂,对PAK1、PAK2和PAK3的IC50值分别为 8 nM、13 nM和19 nM[1]。
PAKs家族包括两个亚群:1和2。PAKs激酶参与不同类型癌症的生长。FRAX597是从高通量筛选的初始命中中获得的第一类PAKs抑制剂。对于第二类PAKs,FRAX597具有最小的抑制活性。FRAX597通过与ATP竞争结合PAK的ATP结合位点,从而抑制PAK的活性。据报道,在Schwann细胞中,FRAX597通过抑制第一类PAKs使细胞周期停滞在G1期,从而抑制细胞增殖,但对细胞活力没有影响。在NF2原位移植肿瘤模型中,FRAX597也可以抑制肿瘤的生长[1]。
参考文献:
[1] Silvia Licciulli, Jasna Maksimoska, Chun Zhou, Scott Troutman, Smitha Kota, Qin Liu, Sergio Duron, David Campbell, Jonathan Chernoff, Jeffery Field, Ronen Marmorstein and Joseph L. Kissil. FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits schwannomas tumorigenesis of NF2-associated. J. Biol. Chem. 2013, August.
2. Nuche-Berenguer B, Ramos-Álvarez I, Jensen RT. "The p21-activated kinase, PAK2, is important in the activation of numerous pancreatic acinar cell signaling cascades and in the onset of early pancreatitis events." Biochim Biophys Acta.2016 Jun;1862(6):1122-36. PMID:26912410
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 558.1 |
Cas No. | 1286739-19-2 |
Formula | C29H28ClN7OS |
Solubility | ≥27.9 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | 6-[2-chloro-4-(1,3-thiazol-5-yl)phenyl]-8-ethyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrido[2,3-d]pyrimidin-7-one |
SDF | Download SDF |
Canonical SMILES | CCN1C2=NC(=NC=C2C=C(C1=O)C3=C(C=C(C=C3)C4=CN=CS4)Cl)NC5=CC=C(C=C5)N6CCN(CC6)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验: [1] | |
细胞系 |
Nf2-null SC4 Schwann细胞 |
制备方法 |
溶解度有限,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
96 h |
实验结果 |
FRAX597显著抑制细胞增殖。FRAX597使G1期细胞增加74%,对照处理的细胞中为50%;减少S期细胞(12%,对照组为27%)和G2/M期细胞(11%,对照组为22%)。 |
动物实验: [1] | |
动物模型 |
8周龄NOD/SCID小鼠,移植Nf2-/- SC4施万细胞的坐骨神经鞘。 |
给药剂量 |
100 mg/kg,口服,一天一次,持续14天 |
实验结果 |
与对照小鼠相比,FRAX597显著减慢小鼠中的肿瘤生长速率。此外,与对照组相比,FRAX597治疗组的平均肿瘤重量显著降低。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: 1. Licciulli S, Maksimoska J, Zhou C et al. FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J Biol Chem. 2013 Oct 4;288(40):29105-14. |
描述 | FRAX597是一种有效的、ATP竞争性的第一类PAKs抑制剂,对PAK1、PAK2和PAK3的IC50值分别为 8 nM、13 nM和19 nM。 | |||||
靶点 | PAK1 | PAK2 | PAK3 | |||
IC50 | 8 nM | 13 nM | 19 nM |
质量控制和MSDS
- 批次:
化学结构
![FRAX597](http://www.apexbt.com//media/diy/images/struct/B1162.png)
相关生物数据
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相关生物数据
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