A potent and selective JAK1/JAK2 inhibitor
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Alternative(s)
11609Ruxolitinib
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Ruxolitinib (phosphate)

Item No. 23215

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
βR-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile, monophosphate
CAS Number
1092939-17-7
Synonyms
  • INC 424 (phosphate)
  • INCB 018424 (phosphate)
Molecular Formula
C17H18N6 • H3PO4
Formula Weight
404.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMSO: 33 mg/mlEthanol: 1 mg/ml
λmax
217, 224, 254, 311 nm
SMILES
N#CC[C@H](C1CCCC1)N(N=C2)C=C2C3=C4C(NC=C4)=NC=N3.O=P(O)(O)O
InChi Code
InChI=1S/C17H18N6.H3O4P/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16;1-5(2,3)4/h6,8-12,15H,1-5H2,(H,19,20,21);(H3,1,2,3,4)/t15-;/m1./s1
InChi Key
JFMWPOCYMYGEDM-XFULWGLBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

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    10 mg

    $219

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    25 mg

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    Product Description

    Ruxolitinib is a potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively, and is relatively less selective for JAK3 (IC50 = 322 nM).1 It blocks interleukin-6 (IL-6) signaling (IC50 = 281 nM) and proliferation of JAK2V617F+ Ba/F3 cells (IC50 = 127 nM).2 In primary cultures, ruxolitinib preferentially suppresses erythroid progenitor colony formation from JAK2V617F+ polycythemia vera patients (IC50 = 67 nM) versus healthy donors (IC50 > 400 nM). In a mouse model of JAK2V617F+ myeloproliferative neoplasms (MPN), 90 mg/kg ruxolitinib reduces splenomegaly, decreases circulating levels of IL-6 and TNF-α, eliminates neoplastic cells, and prolongs survival.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Verstovsek, S. Therapeutic potential of JAK2 inhibitors. Hematology Am. Soc. Hematol. Educ. Program 636-642 (2009).

    2. Quintás-Cardama, A., Vaddi, K., Liu, P., et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: Therapeutic implications for the treatment of myeloproliferative neoplasms. Blood 115(15), 3109-3117 (2010).