BI-3406

製品コードS8916 バッチS891604

印刷

化学情報

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

C23H25F3N4O3
分子量 462.46 CAS No. 2230836-55-0
Solubility (25°C)* 体外 DMSO 92 mg/mL (198.93 mM)
Ethanol 31 mg/mL (67.03 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 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.

生物活性

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.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MIA PaCa-2, mT42 cells
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.
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.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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