テポチニブ
テポチニブ 物理性質
- 沸点 :
- 626.5±65.0 °C(Predicted)
- 比重(密度) :
- 1.25
- 貯蔵温度 :
- Store at -20°C
- 酸解離定数(Pka):
- 8.93±0.10(Predicted)
- 水溶解度 :
- ≥ 4.93 mg/mL in DMSO, <2.52 mg/mL in EtOH, <2.56 mg/mL in Water
- InChIKey:
- AHYMHWXQRWRBKT-UHFFFAOYSA-N
- SMILES:
- C(#N)C1=CC=CC(C2=NN(CC3=CC=CC(C4=NC=C(OCC5CCN(C)CC5)C=N4)=C3)C(=O)C=C2)=C1
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
| 絵表示（GHS） |
|
| 注意喚起語 |
警告 |
| 危険有害性情報 |
| コード |
危険有害性情報 |
危険有害性クラス |
区分 |
注意喚起語 |
シンボル |
P コード |
| H302 |
飲み込むと有害 |
急性毒性、経口 |
4 |
警告 |
|
P264, P270, P301+P312, P330, P501 |
|
| 注意書き |
| P280 |
保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。 |
| P305+P351+P338 |
眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。 |
|
テポチニブ 価格
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
テポチニブ 化学特性,用途語,生産方法
説明
Tepotinib is a highly selective inhibitor against MET. In xenograft models, acquired resistance to EGFR TKIs via secondary EGFR T790 M mutations can be overcome with tepotinib treatment.
使用
EMD 1214063 is a novel ATP-comptetitive inhibitor of the MET hepatocyte growth factor receptor and a novel kinase inhibitor and a therapeutic agent for neuroblastoma. Potent c-MET inhibitor.
作用機序
Tepotinib is a Kinase Inhibitor. The mechanism of action of tepotinib is as a Mesenchymal Epithelial Transition Inhibitor, and P-Glycoprotein Inhibitor.
臨床応用
Tepotinib is currently being evaluated in combination with EGFR TKI gefitinib and also a separate trial in NSCLC patients with MET exon 14 skipping mutation and MET amplification.
薬物相互作用
Tepotinib is indicated for the treatment of adult patients with
metastatic non-small cell lung cancer (NSCLC) who have
mesenchymal-epithelial transition (_MET_) exon 14 skipping alterations.
代謝
Tepotinib is metabolized primarily by CYP3A4 and CYP2C8, with some
apparent contribution by unspecified UGT enzymes. The metabolite M506 is
the major circulating metabolite, comprising approximately 40.4% of
observed drug material in plasma, while the M668 glucuronide metabolite
has been observed in plasma at much lower quantities (~4% of an orally
administered dose). A total of 10 phase I and phase II metabolites have
been detected following tepotinib administration, most of which are
excreted in the feces.
テポチニブ 上流と下流の製品情報
原材料
準備製品
テポチニブ 生産企業
Global( 157)Suppliers
1100598-32-0(テポチニブ)キーワード:
- 1100598-32-0
- Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl]
- 3-(1-(3-(5-((1-Methylpiperidin-4-yl)Methoxy)pyriMidin-2-yl)benzyl)-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile
- 3-(1-(3-(5-((1-METHYLPIPERIDIN-4-YL)METHOXY)PYRIMIDIN-2-YL)BENZYL)-1,6-DIHYDRO-6-OXOPYRIDAZIN-3-YL)B
- 3-[1,6-Dihydro-1-[[3-[5-[(1-methyl-4-piperidinyl)methoxy]-2-pyrimidinyl]phenyl]methyl]-6-oxo-3-pyridazinyl]benzonitrile
- Tepotinib (EMD 1214063)
- MSC2156119
- 3-[1,6-Dihydro-1-[[3-[5-[(1-methyl-4-piperidinyl)methoxy]-2-pyrimidinyl]phenyl]methyl]-6-oxo-3-pyridazinyl]benzonitrile EMD-1214063
- EMD-1214063
3-[1,6-Dihydro-1-[[3-[5-[(1-methyl-4-piperidinyl)methoxy]-2-pyrimidinyl]phenyl]methyl]-6-oxo-3-pyridazinyl]benzonitrile
- 3-(1-(3-(5-((1-Methylpiperidin-4-yl)methoxy)pyrimidin-2-yl)benzyl)-6-oxo-1,6-dihydropyridazin-
- Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)
- CS-977
- EMD 1214063; EMD1214063
- 3-[1-[[3-[5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin-2-yl]phenyl]methyl]-6-oxopyridazin-3-yl]benzonitrile
- epotinib(EMD 1214063)
- EMD1214063,Tepotinib
- Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl] USP/EP/BP
- EMD-1214063
- Tepotinib
- Veledimex
- 3-{1-[(3-{5-[(1-メチルピペリジン-4-イル)メトキシ]ピリミジン-2-イル}フェニル)メチル]-6-オキソ-1,6-ジヒドロピリダジン-3-イル}ベンゾニトリル
- テポチニブ
- 3-[1-[3-[5-[(1-メチルピペリジン-4-イル)メトキシ]ピリミジン-2-イル]ベンジル]-1,6-ジヒドロ-6-オキソピリダジン-3-イル]ベンゾニトリル
- 3-[1-[3-[5-(1-メチル-4-ピペリジニルメトキシ)-2-ピリミジニル]ベンジル]-6-オキソ-1,6-ジヒドロピリダジン-3-イル]ベンゾニトリル