174634-08-3

Basic information

• Product Name: TAS 103
• Synonyms: TAS 103;BMS-247615;TAS-103(salt);6-[[2-(Dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one;TAS-103 HC1;TA103(bms-247615)
• CAS NO: 174634-08-3
• Molecular Formula: C20H19N3O2
• Molecular Weight: 333.38376
• Mol File: 174634-08-3.mol

Chemical Properties

• Melting Point: 216-217 °C(Solv: ethanol (64-17-5))
• Boiling Point: 589.5±50.0 °C(Predicted)
• Appearance: /
• Density: 1.350±0.06 g/cm3(Predicted)
• PKA: 7.88±0.20(Predicted)
• CAS DataBase Reference: TAS 103(CAS DataBase Reference)
• NIST Chemistry Reference: TAS 103(174634-08-3)
• EPA Substance Registry System: TAS 103(174634-08-3)

Safety Data

• Hazardous Substances Data: 174634-08-3(Hazardous Substances Data)

Usage

Uses

Used in Oncology:
TAS 103 is used as an anticancer agent for its effectiveness against a wide range of solid tumors and hematological malignancies. It is particularly effective against cancers such as lung, breast, and colon cancers, as well as leukemia and lymphoma due to its ability to inhibit DNA synthesis in cancer cells.
Used in Cancer Treatment Research:
TAS 103 is used as a subject of clinical trials to further evaluate its safety and efficacy in treating various types of cancer. The ongoing research aims to establish TAS 103 as a viable option for cancer therapy, leveraging its dual topoisomerase inhibitory properties.

Upstream product

• 174634-05-0 3-methoxy-6-(3-dimethylaminoethylamino)indeno[2,1-c]quinolin-7-one 

Relevant articles and documents

Synthesis, cytotoxicity, DNA interaction, and topoisomerase II inhibition properties of novel indeno[2,1-c]quinolin-7-one and indeno[1,2-c]isoquinolin-5, 11-dione derivatives

Indeno[2,1-c]quinolin-7-ones and 6H-indeno[1,2-c]isoquinolin-5,11-diones, bearing two cationic aminoalkyl side chains, were synthesized and evaluated for DNA interaction, topoisomerases inhibition, and cytotoxicity against human cancer cell lines. They displayed strong interaction with DNA and one indeno[1,2-c]isoquinolin-5,11-dione bearing side chains at N-6 and C-8 positions (6a) was a potent human topoisomerase II inhibitor with high cytotoxicity toward HL60 cells. An increased topoisomerase II inhibition is found with (a) a cationic aminoalkyl side chain at the C-8 rather than at the C-9 position, (b) a dimethylaminoethoxy side chain at the C-8 position introduced on the N-6 monosubstituted derivative, going with suppression of topoisomerase I poisoning, and (c) a dimethylaminoethyl rather than a dimethylaminopropyl side chain at the N-6 position. The cytotoxicity was only partially reduced when using the topoisomerase II-mutated mitoxantrone-resistant HL60/MX2 cell line, suggesting that additional targets are involved in their mechanism of action. These indeno[1,2-c]isoquinolin-5,11-dione derivatives represent new DNA-topoisomerase II interfering anticancer molecules.