A JAK2 inhibitor
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TG101348

Item No. 16289

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(1,1-dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]-benzenesulfonamide
CAS Number
936091-26-8
Synonyms
  • Fedratinib
  • SAR302503
Molecular Formula
C27H36N6O3S
Formula Weight
524.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mg/mlEthanol: 0.5 mg/ml
λmax
275 nm
SMILES
CC(C)(C)NS(C1=CC=CC(NC2=NC(NC3=CC=C(OCCN4CCCC4)C=C3)=NC=C2C)=C1)(=O)=O
InChi Code
InChI=1S/C27H36N6O3S/c1-20-19-28-26(30-21-10-12-23(13-11-21)36-17-16-33-14-5-6-15-33)31-25(20)29-22-8-7-9-24(18-22)37(34,35)32-27(2,3)4/h7-13,18-19,32H,5-6,14-17H2,1-4H3,(H2,28,29,30,31)
InChi Key
JOOXLOJCABQBSG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $63

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    5 mg

    $129

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    10 mg

    $206

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    25 mg

    $468

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    Product Description

    TG101348 is a JAK2 inhibitor (IC50 = 3 nM for wild-type and JAK2V617F enzymes).1 It is 35-, 334-, and 135-fold selective for JAK2 over JAK1, JAK3, and tyrosine kinase 2 (TYK2), respectively. It is also selective for JAK2 over a panel of 34 kinases at 500 nM but does inhibit FMS-related tyrosine kinase 3 (FLT3) and RET (IC50s = 15 and 48 nM, respectively). TG101348 reduces the proliferation of HEL human erythroleukemic cells as well as Ba/F3 murine hematopoioetic cells expressing JAK2V617F (IC50s = 305 and 270 nM, respectively). It inhibits the differentiation of hematopoietic stem cells and myeloid progenitor cells isolated from patients with the myeloproliferative neoplasm (MPN) polycythemia vera when used at a concentration of 300 nM.2 TG101348 (60 and 120 mg/kg) improves survival and reduces spleen weight in a syngeneic mouse model of polycythemia vera induced by transplantation of Jak2V617F-expressing whole bone marrow.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wernig, G., Kharas, M.G., Okabe, R.O., et al. Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell 13(4), 311-320 (2008).

    2. Geron, I., Abrahamsson, A.E., Barroga, C.F., et al. Selective inhibition of JAK2-driven erythroid differentiation of polycythemia vera progenitors. Cancer Cell 13(4), 321-330 (2008).