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FRAX 597

Cat. No. 6029 3 篇引用文献 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent group I PAK inhibitor
化学名： 6-[2-Chloro-4-(5-thiazolyl)phenyl]-8-ethyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7-(8H)-one
纯度： ≥98% (HPLC)
说明书
引用文献 (3)
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for FRAX 597

FRAX 597 is a potent group I PAK inhibitor (IC50 values are 8, 13 and 19 nM for PAK1, 2 and 3, respectively). FRAX 597 exhibits significant inhibition of YES1, RET, CSF1R and TEK at 100 nM, but is inactive against group II PAK isoforms (IC50 >10 μM for PAK4). FRAX 597 inhibits proliferation of pancreatic cancer and schwannoma cells in vitro and exhibits antitumor effects in mice.

化合物库 for FRAX 597

FRAX 597 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for FRAX 597

分子量 558.1
公式 C29H28ClN7OS
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1286739-19-2
PubChem ID 70934541
InChI Key DHUJCQOUWQMVCG-UHFFFAOYSA-N
Smiles CN(CC1)CCN1C2=CC=C(NC3=NC(N(CC)C(C(C4=CC=C(C5=CN=CS5)C=C4Cl)=C6)=O)=C6C=N3)C=C2

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for FRAX 597

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 11.16 20

制备储备液 for FRAX 597

以下数据基于产品分子量 558.1。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
0.2 mM 8.96 mL 44.79 mL 89.59 mL
1 mM 1.79 mL 8.96 mL 17.92 mL
2 mM 0.9 mL 4.48 mL 8.96 mL
10 mM 0.18 mL 0.9 mL 1.79 mL

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产品说明书 for FRAX 597

分析证书/产品说明书
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化学品安全技术说明书

参考文献 for FRAX 597

参考文献是支持产品生物活性的出版物。

Licciulli et al (2013) FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. J.Biol.Chem. 288 29105 PMID: 23960073

Yeo et al (2016) FRAX597, a PAK1 inhibitor, synergistically reduces pancreatic cancer growth when combined with gemcit. BMC Cancer 16 24 PMID: 26774265

If you know of a relevant reference for FRAX 597, please let us know.

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关键词: FRAX 597, FRAX 597 supplier, FRAX597, potent, group, I, PAK, inhibits, inhibitors, p21, activated, kinase, P21-activated, Kinases, 6029, Tocris Bioscience

3 篇 FRAX 597 的引用文献

引用文献是使用了 Tocris 产品的出版物。 FRAX 597 的部分引用包括：

Pavla et al (2022) PAK1 and PAK2 in cell metabolism regulation. J Cell Biochem 123 375-389 PMID: 34750857

Zheng et al (2022) Structure-based design of CDC42 effector interaction inhibitors for the treatment of cancer. Cell Rep 39 110641 PMID: 35385746

Naoyuki et al (2021) P21-activated kinase regulates oxygen-dependent migration of vascular endothelial cells in monolayers. Cell Adh Migr 15 272-284 PMID: 34550057

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