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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 | C28H24F3N7O2 |
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分子量 | 547.53 | CAS No. | 839706-07-9 | |
Solubility (25°C)* | 体外 | DMSO | 20 mg/mL (36.52 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. |
製品説明 | GNF-7 is a potent type-II kinase Bcr-Abl inhibitor with IC50 of <5 nM, 61 nM, 122 nM, 136 nM, and 133 nM for M351T, T315I, E255 V, G250E, and c-Abl, respectively. |
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in vitro | GNF-7 shows potent antiproliferative activity against wild-type and mutant Bcr-Abl Ba/F3 cells with IC50 less than 11 nM. In human colon cancer cells (Colo205 and SW620), GNF-7 also displays excellent growth inhibitory activity with IC50 of 5 nM and 1 nM, respectively. [1] GNF-7, potently and selectively inhibits NRAS-dependent acute myelogenous leukemia and acute lymphoblastic leukemia cells through combined inhibition of ACK1/AKT and GCK. [2] |
in vivo | GNF-7 exhibits excellent pharmacokinetic parameters in mice. In a bioluminescent xenograft mouse model using a transformed T315I-Bcr-Abl-Ba/F3 cell line, GNF-7 (10 mg/kg, p.o.) effectively inhibits tumor growth. [1] In NSG mice bearing human mutant NRAS-expressing MOLT-3-luc+ tumors, GNF-7 (15 mg/kg, p.o.) significantly decreases disease burden, prolongs overall survival, and causes strong suppression of phospho-AKT and phospho-RPS6. [2] |
動物実験 | 動物モデル | SCID beige female mice bearing T315I-Bcr-Abl-Ba/F3 orthotopic xenografts |
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投薬量 | 20 mg/kg | |
投与方法 | p.o. |
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Identification of PARN nuclease activity inhibitors by computational-based docking and high-throughput screening [ Sci Rep, 2023, 13(1):5244] | PubMed: 37002320 |
Identification of PARN nuclease activity inhibitors by computational-based docking and high-throughput screening [ Sci Rep, 2023, 13(1):5244] | PubMed: 37002320 |
SH2 domain protein E (SHE) and ABL signaling regulate blood vessel size [ bioRxiv, 2023, 2023.07.03.547455] | PubMed: 37461480 |
SH2 domain protein E -SHE) and ABL signaling regulate blood vessel size [ bioRxiv, 2023, 2023.07.03.547455] | PubMed: 37461480 |
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。