936091-14-4

Basic information

• Product Name: N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide
• Synonyms: N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide;TG101209/TG-101209;TG101209, >=99%;N-tert-Butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesul
• CAS NO: 936091-14-4
• Molecular Formula: C26H35N7O2S
• Molecular Weight: 509.67
• Product Categories: Inhibitor;API;Inhibitors;JAK;STAT
• Mol File: 936091-14-4.mol
• Article Data: 3

Chemical Properties

• Melting Point: 243 °C
• Boiling Point: 703.1 °C at 760 mmHg
• Flash Point: 379 °C
• Appearance: /
• Density: 1.250
• Solubility: ≥25.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
• PKA: 11.95±0.50(Predicted)
• CAS DataBase Reference: N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide(CAS DataBase Reference)
• NIST Chemistry Reference: N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide(936091-14-4)
• EPA Substance Registry System: N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide(936091-14-4)

Safety Data

• Hazardous Substances Data: 936091-14-4(Hazardous Substances Data)

Usage

Uses

TG101209 is an effective tyrosine kinase inhibitor of tyrosine kinases JAK2 and JAK3 (janus kinase 2/3), inducing cell arrest and apoptosis in leukemia cell lines.

Biological Activity

tg101209, a small-molecule identified by structure based design, is a selective inhibitor of janus kinase 2 (jak2) that potently inhibits jak/stat pathway in multiple myeloma (mm) cell lines, such as cell harboring jak2v617f or mplw515l/k mutations which are commonly associated with polycythemia vera (pv) and primary myelofibrosis (pmf) respectively. according to results of multiple studies, it has revealed that tg101209 exhibits a dose and time dependent cyctoxicity, which is associated with inhibited cell cycle progrgression and induced apoptosis, in a wild range of mm cell lines through suppressing the expression of pjak2, pstat3 and bcl-xl and inducing the overexpression of perk and pakt.ramakrishnan v, kimlinger t, haug j, timm m, wellik l, halling t, pardanani a, tefferi a, rajkumar sv, kumar s. tg101209, a novel jak2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for cd45+ myeloma cells. am j hematol. 2010;85(9):675-686.

Upstream product

• 308283-47-8 3-bromo-(N-tert-butyl)benzenesulfonamide 
• 936092-52-3 5-methyl-N₂-(4-(4-methylpiperazin-1-yl)phenyl)pyrimidine-2,4-diamine 
• 936092-53-4 N-(tert-butyl)-3-((2-chloro-5-methylpyrimidin-4-yl)amino)benzenesulfonamide 

Relevant articles and documents

A sulfonamide compound intermediates, their salts and method for preparing the same

The invention discloses compounds as shown in a formula III. The invention also discloses a preparation method of salts of sulfonamide compounds as shown in the formula III, comprising carrying out a coupling reaction for a compound of a formula IV and a compound 2 in a solvent, wherein the temperature is 35-200 DEG C, n2=1-4, and X is a protonic acid which can be removed by distillation under reduced pressure. The invention also discloses a preparation method of sulfonamide compounds as shown in the formula I, inlcuding: (1) preparing a compound of the formula III as the above method; and (2) reacting the compound of the formula III obtained in the step (1) with a base in a solvent with a reflux temperature of 0 DEG C; wherein X is a protonic acid; and n2=1-4. The invention also discloses compounds as shown in the formula IV. The preparation method of the present invention is mild in reaction conditions, high in yield, simple in purification and suitable for industrial production.

BI-ARYL META-PYRIMIDINE INHIBITORS OF KINASES

The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non receptor kinases.