A staurosporine derivative that binds to dephosphorylated c-Met kinase and to the colchicine binding site of tubulin; promotes mitotic arrest and apoptosis of various human tumor cell lines (EC50s ranging from 60-600 nM)

Tivantinib – 10 mg

Brand:
Cayman
CAS:
905854-02-6
Storage:
-20
UN-No:
Non-Hazardous - /

MET is a proto-oncogene that encodes the hepatocyte growth factor receptor c-Met. The receptor has normal roles in morphogenesis, migration, apoptosis, and angiogenesis.{23657} Dysregulation of c-Met occurs in many types of cancer.{23657} Tivantinib is a staurosporine (Item No. 81590) derivative that binds to dephosphorylated c-Met kinase, yet its mechanism of action is not known.{27930} Tivantinib has been tested in clinical studies for its ability to selectively inhibit c-Met.{27930} However, it can promote mitotic arrest and apoptosis of various human tumor cell lines (EC50s ranging from 60-600 nM) through mechanisms independent of its ability to bind c-Met.{27930} Tivantinib has been reported to bind directly to the colchicine binding site of tubulin, reducing tubulin polymerization in cells and in mouse xenograft tumors in vivo.{27931}  

 

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Description

A staurosporine derivative that binds to dephosphorylated c-Met kinase and to the colchicine binding site of tubulin; promotes mitotic arrest and apoptosis of various human tumor cell lines (EC50s ranging from 60-600 nM)

Formal name: (3R,4R)-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-2,5-pyrrolidinedione

Synonyms:  ​ARQ 197

Molecular weight: 369.4

CAS: 905854-02-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Cell Death|Apoptosis

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