JNJ-38877605

製品コードS1114 バッチS111404

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 37 mg/mL (98.05 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）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
30%propylene glycol 5%Tween80 65%D5W

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 30.000mg/ml (79.50mM) Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W 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 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, this compound (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 this chemical 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.

参考

  • http://www.mindcull.com/data/american-association-for-cancer-research/aacr-2008-american-association
  • https://pubmed.ncbi.nlm.nih.gov/21464397/
  • https://pubmed.ncbi.nlm.nih.gov/21500189/

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：

Combined Therapy Targeting MET and Pro-HGF Activation Shows Significant Therapeutic Effect Against Liver Metastasis of CRPC [ Int J Mol Sci, 2025, 26(5)2308] PubMed: 40076928
Functional genomics reveals an off-target dependency of drug synergy in gastric cancer therapy [ Gastric Cancer, 2024, 10.1007/s10120-024-01537-y] PubMed: 39033209
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
Temporal mapping and pharmacological manipulation of signaling architecture of Tyrosine kinases in Traumatic Brain Injury (TBI) [ oparu, 2023, 10.18725/OPARU-47820] PubMed: None
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

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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