JNJ-38877605

製品コードS1114 バッチS111401

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

C19H13F2N7
分子量 377.35 CAS No. 943540-75-8
Solubility (25°C)* 体外 DMSO 50 mg/mL (132.5 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. Phase 1.
in vitro JNJ-38877605 shows more than 600-fold selectivity for c-Met compared with more than 200 other diverse tyrosine and serine-threonine kinases and also potently inhibits HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. [1] In EBC1, GTL16, NCI-H1993, and MKN45 cells, JNJ-38877605 (500 nM) leads to a significant reduction of phosphorylation of Met and RON, another key player in invasive growth. [2] A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells. [3]
in vivo In mice bearing established GTL16 xenografts, JNJ-38877605, dosed orally with 40 mg/kg/day for 72 hours, results in a statistically significant decrease in the plasma levels of human IL-8 (from 0.150 ng/mL to 0.050 ng/mL) and GROα (from 0.080 ng/mL to 0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose. [3]

プロトコル(参考用のみ)

動物実験 動物モデル GTL16 cells are inoculated subcutaneously into the right posterior flank (or both right and left posterior flanks, for determination of uPAR and IL-6) of 6-week-old immunodeficient nu/nu female mice on Swiss CD1 background.
投薬量 ≤40 mg/kg/day
投与方法 Administered via p.o.

カスタマーフィードバック

Data from [PLoS One, 2012, 7, e44937]

Data from [PLoS One, 2012, 7, e44937]

Data from [PLoS One, 2012, 7, e44937]

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：

The Receptor Tyrosine Kinase c-Met Promotes Lipid Accumulation in 3T3-L1 Adipocytes [ Int J Mol Sci, 2023, 24(9)8086] PubMed: 37175792
The Receptor Tyrosine Kinase c-Met Promotes Lipid Accumulation in 3T3-L1 Adipocytes [ Int J Mol Sci, 2023, 24(9)8086] PubMed: 37175792
Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] PubMed: 35868306
Precision Combination Therapies Based on Recurrent Oncogenic Coalterations [ Cancer Discov, 2022, 12(6):1542-1559] PubMed: 35412613
Efficacy of CAR-T immunotherapy in MET overexpressing tumors not eligible for anti-MET targeted therapy [ J Exp Clin Cancer Res, 2022, 41(1):309] PubMed: 36271379
MACC1 promotes pancreatic cancer metastasis by interacting with the EMT regulator SNAI1 [ Cell Death Dis, 2022, 13(11):923] PubMed: 36333284
STAT3 inhibition suppresses adaptive survival of ALK-rearranged lung cancer cells through transcriptional modulation of apoptosis [ NPJ Precis Oncol, 2022, 6(1):11] PubMed: 35228642
MET Oncogene Controls Invasive Growth by Coupling with NMDA Receptor [ Cancers (Basel), 2022, 14(18)4408] PubMed: 36139568
MET∆14 promotes a ligand-dependent, AKT-driven invasive growth [ Life Sci Alliance, 2022, 5(10)e202201409] PubMed: 35636967
Dysbiotic stress increases the sensitivity of the tumor vasculature to radiotherapy and c-Met inhibitors [ Angiogenesis, 2021, 10.1007/s10456-021-09771-z] PubMed: 33629198

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。