FRAX597

製品コードS7271 バッチS727101

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C29H28ClN7OS
分子量 558.10 CAS No. 1286739-19-2
Solubility (25°C)* 体外 DMSO 14 mg/mL warmed with 50ºC water bath (25.08 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 FRAX597 is a potent, ATP-competitive inhibitor of group I PAKs with IC50 of 8 nM, 13 nM, and 19 nM for PAK1, PAK2, and PAK3, respectively.
in vitro FRAX597 (100 n M) displays a significant inhibitory capacity toward YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%), while displays minimal inhibitory activity towards the group II PAKs: PAK4 (0%), PAK6 (23%), and PAK7 (8%). FRAX597 treatment dramatically impairs the proliferation of Nf2-null SC4 Schwann cells (SC4 cells). FRAX597 displays an IC50 value of 48 nM against wild type PAK1, while IC 50 values against the V342F and V342Y PAK1 mutants are higher than 3μM and 2 μM, respectively.[1] FRAX597 inhibits the proliferation and motility of both benign (Ben-Men1, 3μM) and malignant (KT21-MG1, 0.4 μM) meningiomas cells after treating of 72 h.[2]
in vivo In NOD/SCID mice which bearing Nf2-/-SC4 Schwann cells, FRAX597 (100 mg/kg/day, p.o.) causes more significant tumor growth inhibition cpmpared with control mice.[1] In SCID mice with orthotopic meningioma, FRAX597 (90 mg/kg/day, p.o.) significantly suppresses tumor growth.[2] In KrasG12D mice, treatment with FRAX597 (90 mg/kg/day, p.o.) causes tumor regression and loss of Erk and Akt activity.[3]

プロトコル(参考用のみ)

キナーゼアッセイ Determination of Enzyme IC50 Values
IC50 values are determined using a 10 concentration point, non-radioactive, functional assay that employs a fluorescence-based, coupled-enzyme format, according to the manufacturer’s protocol (Z’-LYTE@biochemical assay). Kinase selectivity is determined using both the Z’-LYTE@ and Adapta@ kinase assay format.
細胞アッセイ 細胞株 SC4 cells
濃度 1 μM
反応時間 4 day
実験の流れ 30,000 cells/well are plated in 12-well dishes in triplicate. Cell growth media with or without FRAX597 is replaced daily. At indicated time points, cells from individual wells are trypsinized and counted using a Coulter counter.
動物実験 動物モデル SCID mice with orthotopic meningioma model
投薬量 90 mg/kg/day
投与方法 p.o.

カスタマーフィードバック

Data from [Data independently produced by , , Oncotarget, 2016, 7(15):19709-22]

Data from [Data independently produced by , , Am J Cancer Res, 2017, 7(8):1724-1737]

Data from [Data independently produced by , , PLoS One, 2016, 11(9):e0162214]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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