Tepotinib

한글명:Tepotinib

카스 번호1100598-32-0

상품명:Tepotinib

CBNumberCB72550731

분자식C29H28N6O2

포뮬러 무게492.57

MOL 파일1100598-32-0.mol

화학적 성질

끓는 점	626.5±65.0 °C(Predicted)
밀도	1.25
저장 조건	Store at -20°C
물리적 상태	Solid
산도 계수 (pKa)	8.93±0.10(Predicted)
수용성	≥ 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

그림문자(GHS)

Tepotinib 화학적 특성, 용도, 생산

개요
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.
용도
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.
상표명
Tepmetko
Mechanism of action
Tepotinib is a Kinase Inhibitor. The mechanism of action of tepotinib is as a Mesenchymal Epithelial Transition Inhibitor, and P-Glycoprotein Inhibitor.
Clinical Use
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.
Drug interactions
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.
신진 대사
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.

Tepotinib 준비 용품 및 원자재

Tepotinib 공급 업체

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