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ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  Protein tyrosine kinase /JAK / STAT >  JAK inhibitors >  N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide

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

Basic information Description In vitro In vivo Safety Related Supplier
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide Basic information
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide Chemical Properties
  • Boiling point:713.7±70.0 °C(Predicted)
  • Density 1.247
  • form Beige powder.
  • pka11.95±0.50(Predicted)
  • CAS DataBase Reference936091-26-8
Safety Information
  • HS Code 29350090
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide Usage And Synthesis
  • DescriptionFedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35-and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 2.
  • In vitroTG-101348 also significantly inhibits JAK2 V617F, Flt3, and Ret with IC50 of 3 nM, 15 nM, and 48 nM, respectively. TG101348 has an IC50 ~300-fold higher for the closely related JAK3 and is a less potent inhibitor of the JAK1 and TYK2 family members. TG101348 inhibits proliferation of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation, as well as a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F), with IC50 of 305 nM and 270 nM, respectively. TG-101348 also inhibits proliferation of parental Ba/F3 cells to a comparable level, with IC50 of ~420 nM. TG101348 treatment reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation. TG101348 induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner. TG101348 does not show proapoptotic activity in control normal human dermal fibroblasts at concentrations up to 10 μM, and the antiproliferative IC50 against fibroblasts is >5 μM. TG101348 treatment decreases GATA-1 expression, which is associated with erythroid-skewing of JAK2V617F+ progenitor differentiation, and inhibits STAT5 as well as GATA S310 phosphorylation. TG101348 inhibits the proliferation of HMC-1.1 (KITV560G) cells, with somewhat lower potency than HMC-1.2 (KITD816V, KITV560G) cells, with IC50 of 740 nM and 407 nM, respectively.
  • In vivoTG101348 has potential for efficacious treatment of JAK2V617F-associated myeloproliferative diseases (MPD). In treated animals, there is a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis, and, at least in some instances, evidence for attenuation of myelofibrosis, correlated with surrogate endpoints, including reduction/elimination of JAK2V617F disease burden, suppression of endogenous erythroid colony formation, and in vivo inhibition of JAK-STAT signal transduction. There are no apparent toxicities and no effect on T cell number. Oral administration of TG101348 (120 mg/kg) significantly inhibits PV progenitor erythroid differentiation in vivo.
  • UsesA potent, highly selective and ATP-competitive JAK2 inhibitor with an IC50 of 3 nM for JAK2 and JAK2V617F.
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide(936091-26-8)Related Product Information
N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamideSupplierMore
  • Company Name:Shanghaizehan biopharma technology co., Ltd. Gold
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  • Email:sales@zehanbiopharma.com;
  • Products Intro:Product Name:Fedratinib (SAR302503, TG101348)
    CAS:936091-26-8
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  • Company Name:Shanghai Thunder Biological Technology Co., Ltd. Gold
  • Tel:18621609968
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  • Products Intro:Product Name:N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide
    CAS:936091-26-8
    Purity:98 Package:10 g/;50 g/;100 g/
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  • Company Name:Changzhou Yongfeng Biomedicine Co. Ltd. Gold
  • Tel:15006117673
  • Email:2973592490@qq.com
  • Products Intro:Product Name:Fedratinib
    CAS:936091-26-8
    Package:10g/
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  • Company Name:Shanghai Boyle Chemical Co., Ltd.
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  • Email:sales@boylechem.com
  • Products Intro:Product Name:N-(1,1-Dimethylethyl)-3-5-methyl-2-4-2-(1-pyrrolidinyl)ethoxyphenylamino-4-pyrimidinylaminobenzenesulfonamide
    CAS:936091-26-8
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  • Company Name:Chembest Research Laboratories Limited
  • Tel:021-20908456-
  • Email:sales@BioChemBest.com
  • Products Intro:Product Name:TG 101348
    CAS:936091-26-8
    Remarks:C14248
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