299921-01-0

Basic information

• Product Name: 1-(METHYLSULFONYL)INDOLIN-5-AMINE
• Synonyms: (1-mesylindolin-5-yl)amine;1-Methanesulfonyl-2,3-dihydro-1H-indol-5-ylamine;1-methylsulfonyl-2,3-dihydroindol-5-amine;1-methylsulfonyl-5-indolinamine;BAS 04849652;Oprea1_385552;Peakdale1_000917;ZERO/006241
• CAS NO: 299921-01-0
• Molecular Formula: C₉H₁₂N₂O₂S
• Molecular Weight: 212.27
• Mol File: 299921-01-0.mol

Chemical Properties

• Melting Point: 115～117℃
• Boiling Point: 427.9±55.0 °C(Predicted)
• Appearance: /
• Density: 1.41±0.1 g/cm3(Predicted)
• PKA: 3.93±0.20(Predicted)
• CAS DataBase Reference: 1-(METHYLSULFONYL)INDOLIN-5-AMINE(CAS DataBase Reference)
• NIST Chemistry Reference: 1-(METHYLSULFONYL)INDOLIN-5-AMINE(299921-01-0)
• EPA Substance Registry System: 1-(METHYLSULFONYL)INDOLIN-5-AMINE(299921-01-0)

Safety Data

• Hazardous Substances Data: 299921-01-0(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
1-(METHYLSULFONYL)INDOLIN-5-AMINE is used as a building block in the synthesis of various pharmaceuticals and organic compounds. Its versatile chemical structure and potential therapeutic properties make it a valuable component in the development of new drugs and therapeutic agents.
Used in Anti-cancer Applications:
1-(METHYLSULFONYL)INDOLIN-5-AMINE is used as an anti-cancer agent, exhibiting potential anti-tumor activity. Its ability to interact with biological macromolecules such as proteins and enzymes may contribute to its anti-cancer properties.
Used in Anti-inflammatory Applications:
1-(METHYLSULFONYL)INDOLIN-5-AMINE is used as an anti-inflammatory agent, potentially reducing inflammation and alleviating symptoms associated with inflammatory conditions.
Used in Antimicrobial Applications:
1-(METHYLSULFONYL)INDOLIN-5-AMINE is used as an antimicrobial agent, demonstrating potential activity against various microorganisms, including bacteria and fungi. Its ability to interact with biological macromolecules may contribute to its antimicrobial properties.
Used in Organic Synthesis:
1-(METHYLSULFONYL)INDOLIN-5-AMINE is used as a versatile building block in organic synthesis, allowing for the creation of a wide range of organic compounds with various applications in industries such as pharmaceuticals, agrochemicals, and materials science.

Upstream product

• 312523-56-1 1-(methylsulfonyl)-5-nitroindoline 
• 32692-19-6 5-nitro-2,3-dihydro-1H-indole 
• 6146-52-7 5-nitroindole 

Relevant articles and documents

Synthesis, structure-activity relationships and biological evaluation of 7-phenyl-pyrroloquinolinone 3-amide derivatives as potent antimitotic agents

A small library of 7-pyrrolo[3,2-f]quinolinones was obtained by introducing benzoyl, sulfonyl and carbamoyl side chains at the 3-N position, and their cytotoxicity against a panel of leukemic and solid tumor cell lines was evaluated. Most of them showed high antiproliferative activity with GI50s ranging from micro-to sub-nanomolar values, and these values correlated well with the inhibitory activities of the compounds against tubulin polymerization. Based on a recently proposed colchicine bind site inhibitors (CBSIs) pharmacophore, the interactions of the novel 7-PPyQs at the colchicine domain were rationalized. The most active compounds (4a and 4b) did not induce significant cell death in normal human lymphocytes, suggesting that the compounds may be selective against cancer cells. In particular, 4a was a potent inducer of apoptosis in both the HeLa and Jurkat cell lines. On the other hand, the sulfonyl derivative 4b exhibited a lower potency in comparison with 4a. With both compounds, induction of apoptosis was associated with dissipation of the mitochondrial transmembrane potential and production of reactive oxygen species, suggesting that cells treated with the compounds followed the intrinsic pathway of apoptosis.

HETEROCYCLIC COMPOUNDS AND USES THEREOF

The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.

THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY

To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R 1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R 2 is methyl; R 3 is a hydrogen atom; and R 4 is a group: -CONR 5 R 6 (in which any one of R 5 and R 6 is a hydrogen atom)].