ChemicalBook > CAS DataBase List > N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide

N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide

N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide Structure
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide
  • CAS No.936091-14-4
  • Chemical Name:N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide
  • CBNumber:CB82485001
  • Molecular Formula:C26H35N7O2S
  • Formula Weight:509.67
  • MOL File:936091-14-4.mol
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide Property
  • Melting point 243 °C
  • Boiling point 703.1±70.0 °C(Predicted)
  • Density 1.250
  • storage temp. Store at -20°C
  • solubility ≥25.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
  • form solid
  • pka 11.95±0.50(Predicted)
  • color White to gray
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordDanger
  • Hazard statements H302-H314
  • Precautionary statements P260-P264-P270-P280-P301+P330+P331+P310-P303+P361+P353+P310+P363-P304+P340+P310-P305+P351+P338+P310-P405-P501

N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide Chemical Properties,Usage,Production

  • 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.
  • Definition ChEBI: TG101209 is a member of the class of pyrimidines that is 5-methylpyrimidine-2,4-diamine in which the amino group at position 2 is substituted by a p-(4-methylpiperazin-1-yl)phenyl group, while that at position 4 is substituted by a m-(tert-butylsulfamoyl)phenyl group. A Janus kinase 2 (JAK2) inhibitor. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, an apoptosis inducer and an antineoplastic agent. It is a sulfonamide, a member of pyrimidines, a N-alkylpiperazine, a N-arylpiperazine and a secondary amino compound.
  • 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.
  • in vivo

    TG101209 (100 mg/kg) effectively prolongs the survival in JAK2V617F-induced disease (10 days). Compared with placebo-treated animals, TG101209-treated animals exhibit statistically significant, dose-dependent reduction in the circulating tumor cell burden at day +11 to 20%[1].

  • target 6 nM
  • IC 50 JAK2: 6 nM (IC50); JAK3: 169 nM (IC50); RET: 17 nM (IC50); FLT3: 25 nM (IC50)
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide Preparation Products And Raw materials
Raw materials
Preparation Products
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide Suppliers
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N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide Spectrum
936091-14-4, N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamideRelated Search:
  • API
  • Inhibitor
  • Inhibitors
  • STAT
  • JAK
  • 抑制剂
  • 药靶配体
  • 标准品
  • 小分子抑制剂，天然产物
  • 小分子抑制剂
  • C26H35N7O2S
  • 化合物TG101209,10 MM DMSO 溶液
  • N-(1,1-二甲基乙基)-3-[[5-甲基-2-[[4-(4-甲基-1-哌嗪)苯基]氨基]-4-嘧啶]氨基]苯磺酰胺
  • 化合物TG101209
  • N-(1,1-二甲基乙基)-3-[[5-甲基-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-4-嘧啶基]氨基]苯磺酰胺
  • 936091-14-4
  • TG101209, 10 mM in DMSO
  • Cluster of differentiation antigen 135,RET,TG101209,Inhibitor,Janus kinase,CD135,Fms like tyrosine kinase 3,TG 101209,FLT3,TG-101209,Apoptosis,JAK,inhibit,Autophagy
  • Benzenesulfonamide, N-(1,1-dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]-
  • CS-94
  • TG101209;TG 101209;TG-101209
  • N-tert-Butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesul
  • TG101209/TG-101209
  • N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide
  • TG101209, >=99%

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