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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C28H32ClN7O |
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分子量 | 518.05 | CAS No. | 1432908-05-8 | |
Solubility (25°C)* | 体外 | 4-Methylpyridine | 21 mg/mL warmed with 50ºC water bath (40.53 mM) | |
DMSO | Insoluble | |||
Water | 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. |
製品説明 | FRAX-1036 is a potent and selective PAK1 inhibitor. |
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in vitro | Potent cellular inhibition of group I PAK substrate phosphorylation (MEK1-S298 and CRAF-S338) was observed at 2.5 to 5 μM concentrations of FRAX1036 in PAK1-amplified MDA-MB-175 cells. Treatment of PAK1-amplified breast cancer cells with FRAX1036 results in apoptosis[1]. And treatment of OVCAR-3 cells with FRAX-1036 results in upregulation of p53 and p21, while down-regulating cyclin B1[3]. |
in vivo | Treatment with Frax1036 results in slower KT21 tumor growth and is unlikely to have significant blood brain barrier permeability in mice[4]. |
細胞アッセイ | 細胞株 | MDA-MB175 cells |
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濃度 | 0, 0.5, 1, 2.5, 5 μM | |
反応時間 | 24 h | |
実験の流れ | MDA-MB175 cells are treated with increasing concentrations of FRAX1036 for 24 hours. Cell lysates are immunoblotted with antibodies against biomarkers involved in PAK1 effector and survival signaling. |
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動物実験 | 動物モデル | Pak2-deficient mice |
投薬量 | 30 mg/kg | |
投与方法 | by oral gavage |
Targetable leukemia dependency on noncanonical PI3Kγ signaling [ bioRxiv, 2023, 10.1101/2023.12.15.571909] | PubMed: none |
MICAL1 activation by PAK1 mediates actin filament disassembly [ Cell Rep, 2022, 41(1):111442] | PubMed: 36198272 |
EGFR activation limits the response of liver cancer to lenvatinib [ Nature, 2021, 595(7869):730-734] | PubMed: 34290403 |
Functional proteomics interrogation of the kinome identifies MRCKA as a therapeutic target in high-grade serous ovarian carcinoma. [ Sci Signal, 2020, 13(619)] | PubMed: 32071169 |
ROCK1 but not LIMK1 or PAK2 is a key regulator of apoptotic membrane blebbing and cell disassembly. [ Cell Death Differ, 2019, 10.1038/s41418-019-0342-5] | PubMed: 31043701 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。