UNC2250

製品コードS7342 バッチS734201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H36N6O2
分子量 440.58 CAS No. 1493694-70-4
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 2 mg/mL (4.53 mM)
Water Insoluble
Ethanol 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
0.13mg/ml Taking the 1 mL working solution as an example, add 50 μL 2.5 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to make it clear. Volume up 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 UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.
in vitro UNC2250 efficiently inhibits Mer phosphorylation in 697 B-ALL cells and Colo699 NSCLC cells. Moreover, UNC2250 also displays functional antitumor activity by reducing colony-forming potential in both rhabdoid tumor cells and NSCLC cells. [1]
in vivo According to in vivo PK experiment, UNC2250 has a moderate half-life, clearance, and volume of distribution as well as reasonable oral bioavailability and good solubility. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Microfluidic Capillary Electrophoresis (MCE) Assay
Activity assays are performed in a 384-well, polypropylene microplate in a final volume of 50 μL of 50 mM Hepes, pH 7.4, containing 10 mM MgCl2, 1.0 mM DTT, 0.01% Triton X-100, 0.1% bovine serum albumin (BSA), containing 1.0 μM fluorescent substrate and ATP at the Km for each enzyme. All reactions are terminated by addition of 20 μL of 70 mM EDTA. After an 180 min incubation, phosphorylated and unphosphorylated substrate peptides are separated in buffer supplemented with 1× CR-8 on a LabChip EZ Reader equipped with a 12-sipper chip. Data are analyzed using EZ Reader software.
細胞アッセイ 細胞株 BT-12 rhabdoid tumor cells, and Colo699 NSCLC cells
濃度 ~3 μM for BT-12, ~300 nM for Colo699
反応時間 3 weeks for BT-12, 2 weeks for Colo699
実験の流れ BT-12 rhabdoid tumor cells (10 000 cells) are cultured in 2.0 mL of 0.35% soft agar containing 0.5× RPMI medium, 7.5% FBS, and the indicated concentrations of 10 or DMSO vehicle only and overlaid with 0.5 mL of 1× RPMI medium containing 15% FBS and 10 or DMSO vehicle only. Medium and 10 or vehicle are refreshed 2 times per week. Colonies were stained with thiazolyl blue tetrazolium bromide and counted after 3 weeks. Colo699 NSCLC cells (15 000 cells) are cultured in 1.5 mL of 0.35% soft agar containing 1× RPMI medium and 10% FBS and overlaid with 2.0 mL of 1× RPMI medium containing 10% FBS and the indicated concentrations of 10 or DMSO vehicle only. Medium and 10 or vehicle are refreshed 3 times per week. Colonies are stained with nitrotetrazolium blue chloride and counted after 2 weeks.
動物実験 動物モデル Mice
投薬量 ~3 mg/kg
投与方法 i.v. or p.o.

カスタマーフィードバック

Data from [Data independently produced by , , J Hematol Oncol, 2018, 11(1):43]

Data from [Data independently produced by , , Arthritis Res Ther, 2016, 18(1):268]

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：

Targeted transplantation of engineered mitochondrial compound promotes functional recovery after spinal cord injury by enhancing macrophage phagocytosis [ Bioact Mater, 2024, 32:427-444] PubMed: 37954465
N-glycosylation stabilizes MerTK and promotes hepatocellular carcinoma tumor growth [ Redox Biol, 2022, 54:102366] PubMed: 35728303
GAS6/TAM signaling pathway controls MICA expression in multiple myeloma cells [ Front Immunol, 2022, 13:942640] PubMed: 35967396
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] PubMed: 35207746
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] PubMed: 35118583
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z] PubMed: 34304386
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4] PubMed: 34731453
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918] PubMed: 34383271
CoQ10 promotes resolution of necrosis and liver regeneration after acetaminophen-induced liver injury [ Toxicol Sci, 2021, kfab123] PubMed: 34668565
MerTK inhibits the activation of the NLRP3 inflammasome after subarachnoid hemorrhage by inducing autophagy [ Brain Res, 2021, 1766:147525] PubMed: 34010608

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。