936091-14-4 Usage
Description
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide, also known as TG101209, is a potent and selective inhibitor of Janus kinases JAK2 and JAK3. It is a small molecule compound with a complex chemical structure that allows it to selectively target and inhibit the activity of these kinases, leading to cell cycle arrest and apoptosis in leukemia cell lines.
Uses
Used in Oncology:
TG101209 is used as a tyrosine kinase inhibitor for the treatment of leukemia. It selectively targets and inhibits the activity of JAK2 and JAK3 kinases, which play a crucial role in the development and progression of leukemia. By inhibiting these kinases, TG101209 induces cell cycle arrest and apoptosis in leukemia cell lines, making it a promising therapeutic agent for the treatment of this disease.
Used in Drug Development:
TG101209 is also used in drug development as a lead compound for the discovery of new and more effective treatments for leukemia and other related cancers. Its unique chemical structure and selective inhibition of JAK2 and JAK3 kinases make it an attractive starting point for the design and synthesis of new drugs with improved efficacy and reduced side effects.
Used in Research:
In addition to its therapeutic applications, TG101209 is also used as a research tool to study the role of JAK2 and JAK3 kinases in the development and progression of leukemia and other cancers. Its ability to selectively inhibit these kinases allows researchers to investigate the molecular mechanisms underlying the growth and survival of cancer cells, leading to a better understanding of the disease and the identification of new therapeutic targets.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 936091-14-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,3,6,0,9 and 1 respectively; the second part has 2 digits, 1 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 936091-14:
(8*9)+(7*3)+(6*6)+(5*0)+(4*9)+(3*1)+(2*1)+(1*4)=174
174 % 10 = 4
So 936091-14-4 is a valid CAS Registry Number.
936091-14-4Relevant articles and documents
A sulfonamide compound intermediates, their salts and method for preparing the same
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Paragraph 0086-0090, (2017/01/26)
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
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Page/Page column 108-109, (2008/06/13)
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.