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Tivantinib

Tivantinib structure

CAS No:
905854-02-6
Formula:
C23H19N3O2
Chemical Name:
Tivantinib
Synonyms:
2,5-Pyrrolidinedione,3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-,(3R,4R)-;(3R,4R)-3-(5,6-Dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-2,5-pyrrolidinedione;(3R,4R)-3-(5,6-Dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione;Tivantinib;ARQ 197;1000873-98-2;1228508-24-4
Categories:
Biochemical Engineering > Inhibitors

Description

Tivantinib is a novel and highly selective c-Met tyrosine kinase inhibitor with Ki of 355 nM.

LSM-1131 is a member of indoles.|Tivantinib has been investigated in Solid Tumors.|Tivantinib is an orally bioavailable small molecule inhibitor of c-Met with potential antineoplastic activity. c-Met inhibitor ARQ 197 binds to the c-Met protein and disrupts c-Met signal transduction pathways, which may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. c-Met protein, the product of the proto-oncogene c-Met, is a receptor tyrosine kinase also known as hepatocyte growth factor receptor (HGFR); this protein is overexpressed or mutated in many tumor cell types and plays key roles in tumor cell proliferation, survival, invasion, and metastasis, and tumor angiogenesis.

Tivantinib Basic Attributes

Molecular Weight：

369.422

Exact Mass：

369.42

UNII：

PJ4H73IL17

NCI Thesaurus Code：

C62437

Characteristics

PSA：

66.9

XLogP3：

2.9

Density：

1.5±0.1 g/cm3

Boiling Point：

715.95°C at 760 mmHg

Flash Point：

386.8±32.9 °C

Refractive Index：

1.797

Safety Information

Precautionary statement(s)：

P201, P202, P260, P281, P308+P313, P314, P405, P501

Hazard Statements：

H360

Drug Information

Drug Indication：

Treatment of hepatoblastoma

Mechanism of Action：

Tivantinib mediates its effects by inhibiting the activity of c-Met, a receptor tyrosine kinase that plays multiple key roles in human cancer, including cancer cell growth, survival, angiogenesis, invasion and metastasis. C-Met is abnormally activated in most cancers and is believed to control multiple signal transduction pathways involved in tumor growth and metastasis.

MeSH Entry Terms：

(-)-trans-3-(5,6-dihydro-4H-pyrrolo(3,2,1-ij)quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidin-2,5-dione

Tivantinib Use and Manufacturing

Uses

Tivantinib is ahepatocyte growth factor receptor (proto-oncogene c-Met; MET) inhibitor. Tivantinib inhibits human c-Metreceptor tyrosine kinase selectively and is a promising therapeutic option for thetreatment of c-Met-associated cancers.

Use Classification：

Human drugs -> Rare disease (orphan)|Human Drugs -> EU pediatric investigation plans

Computed Properties

Molecular Weight:369.4
XLogP3:2.9
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:2
Rotatable Bond Count:2
Exact Mass:369.147726857
Monoisotopic Mass:369.147726857
Topological Polar Surface Area:66.9
Heavy Atom Count:28
Complexity:666
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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