受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C23H25F3N4O3 |
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分子量 | 462.46 | CAS No. | 2230836-55-0 | |
Solubility (25°C)* | 体外 | DMSO | 92 mg/mL (198.93 mM) | |
Ethanol | 92 mg/mL (198.93 mM) | |||
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 | BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities. |
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製品説明 | BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities. |
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in vitro | BI-3406, a selective SOS1 inhibitor, enhanced the AMG 510-induced growth suppression in MIA PaCa-2 cells. Treatment with 5 µM BI-3406 following the excision of endogenous mutant KRAS abolishes both ERK and AKT activation, consistent with the inhibition of WT RAS signaling.[1] |
in vivo | BI-3406, a potent and selective SOS1-KRAS Interaction Inhibitor, is effective in KRAS-driven cancers through combined MEK inhibition.[2] |
細胞アッセイ | 細胞株 | MIA PaCa-2, mT42 cells |
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濃度 | 5 μM, 20 μM to 2 nM | |
反応時間 | 4 days | |
実験の流れ | MIA PaCa-2 cells were seeded at 2,000 cells per well and treated 24 h after seeding with 5 μM BI-3406 or DMSO control and AMG 510 (from 5 μM to 0.1 nM). Cell viability was measured after 4 d with CellTiter-Glo. mT42 cells were seeded at 1,000 cells per well and treated with 4-OHT or DMSO control and BI-3406 in a dose–response manner (from 20 μM to 2 nM). Cell viability was measured using CellTiter-Glo Luminescence assay at day 4. FPC cell line mT42 cells were treated with 5 μM BI-3406, 20 nM trametinib, or DMSO vehicle control in the presence or absence of mutant KRAS by treatment with DMSO vehicle control or 4-OHT, respectively. Immunoblotting was performed for RAS pathways by phospho-ERK and phospho-AKT and the RSK1 substrate phospho-S6. |
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動物実験 | 動物モデル | NSG female mice of KRAS G12V and KRAS Q61K mutant pancreatic PDX model |
投薬量 | 50 mg/kg | |
投与方法 | p.o. |
RAS-dependent RAF-MAPK hyperactivation by pathogenic RIT1 is a therapeutic target in Noonan syndrome-associated cardiac hypertrophy [ Sci Adv, 2023, 9(28):eadf4766] | PubMed: 37450595 |
RAS-dependent RAF-MAPK hyperactivation by pathogenic RIT1 is a therapeutic target in Noonan syndrome-associated cardiac hypertrophy [ Sci Adv, 2023, 9(28):eadf4766] | PubMed: 37450595 |
Impaired proteolysis of non-canonical RAS proteins drives clonal hematopoietic transformation [ Cancer Discov, 2022, CD-21-1631] | PubMed: 35904492 |
In vivo genome-wide CRISPR screening identifies ZNF24 as a negative NF-κB modulator in lung cancer [ Cell Biosci, 2022, 12(1):193] | PubMed: 36457047 |
Profiling oncogenic KRAS mutant drugs with a cell-based Lumit p-ERK immunoassay [ SLAS Discov, 2022, S2472-5552(22)12517-7] | PubMed: 35288294 |
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。