TG101348 (SAR302503)

TG101348 (SAR302503)

Catalog Number:
L002369045APE
Mfr. No.:
APE-A4136
Price:
$292
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      • Overview
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          Background

          TG101348, also known as SAR302503, is a potent and selective inhibitor of janus kinase 2 (JAK2), one member of a family of 4 cytoplasmic tyrosine kinases including janus kinase 1(JAK1), JAK2, janus kinase 3 (JAK3) and tyrosine kinase 2 (Tyk2), with the inhibition constant IC50 of 3 nM. Comparing to other close related kinases, the selectivity of TG101348 for JAK2 is 35- and 334-fold stronger than that for JAK3 and JAK1 respectively. TG10348 is capable of inducing apoptosis in HEL cells as well BaF/3 cells harboring JAK2V617 mutation and inhibiting hematopoietic progenitor colony formation and erythroid engraftment in samples from polycythemia vera (PV) patients.

      • Properties
        • Alternative Name
          Tg-101348,SAR-302503; N-tert-butyl-3-[[5-methyl-2-[4-(2-pyrrolidin-1-ylethoxy)anilino]pyrimidin-4-yl]amino]benzenesulfonamide
          CAS Number
          936091-26-8
          Molecular Formula
          C27H36N6O3S
          Molecular Weight
          524.68
          Appearance
          A solid
          Purity
          99.51%
          Solubility
          ≥26.23 mg/mL in DMSO; insoluble in H2O; ≥6.69 mg/mL in EtOH with gentle warming and ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Deng R, Zhang P, et al. "HDAC is indispensable for IFN-γ-induced B7-H1 expression in gastric cancer." Clin Epigenetics. 2018 Dec 11;10(1):153. PMID:30537988
          2. Quan Y, Xu H, et al. "JAK-STAT Signaling Pathways and Inhibitors Affect Reversion of Envelope-Mutated HIV-1." J Virol. 2017 Apr 13;91(9). pii: e00075-17. PMID:28202754

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