| 名稱 | FRAX597 |
| 描述 | FRAX597 is an effective, ATP-competitive inhibitor of group I PAKs, and for PAK1(IC50=8 nM), PAK2(IC50=13 nM), and PAK3 (IC50=19 nM). |
| 細胞實驗 | 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.(Only for Reference) |
| 激酶實驗 | 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. |
| 體外活性 | 負荷Nf2-/-SC4 Schwann細胞的NOD/SCID小鼠中,每天口服 FRAX597（100 mg/kg）,對腫瘤生長有明顯的抑制作用.患有原位腦膜瘤的SCID小鼠中,每天口服 FRAX597（90 mg/kg）,明顯抑制腫瘤生長.在KrasG12D小鼠中,每天口服 FRAX597（90 mg/kg）,處理引起腫瘤消退以及Erk與Akt活性損失. |
| 體內(nèi)活性 | FRAX597抗野生型PAK1（IC50=48 nM）,而抗V342F PAK1突變型(IC50>3 μM)和V342Y PAK1突變型(IC50>2 μM)。FRAX597(100 nM )對YES1 (87%),RET (82%),CSF1R (91%),TEK (87%),PAK1 (82%),和PAK2 (93%)表現(xiàn)出明顯的抑制作用。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Saline : < 1.31 mg/mL (2.35 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1.33 mg/mL (2.38 mM), Solution.
DMSO : 13.06 mg/mL (23.4 mM), Sonication is recommended.
|
| 關(guān)鍵字 | PAK3 | PAK2 | PAK1 | PAK | p21 activated kinases | Inhibitor | inhibit | FRAX-597 | FRAX597 | FRAX 597 |
| 相關(guān)產(chǎn)品 | ZINC194100678 | FRAX1036 | 5-Aminosalicylic Acid | GNE 2861 | P505-15 Acetate | G-5555 | PF-3758309 hydrochloride | PIR 3.5 | AZ13705339 | Fingolimod hydrochloride | PRT062607 hydrochloride | AZA197 |
| 相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 激酶抑制劑庫 | 細胞骨架化合物庫 | 多靶點化合物庫 | 表型篩選靶點鑒定庫 | 蛋白翻譯后修飾化合物庫 |