A potent, orally bioavailable Syk inhibitor
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BIIB-057

Item No. 17652

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[[3-(2H-1,2,3-triazol-2-yl)phenyl]amino]-5-pyrimidinecarboxamide
CAS Number
1370261-96-3
Synonyms
  • P505-15
  • PRT062607
  • PRT2607
Molecular Formula
C19H23N9O
Formula Weight
393.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 25 mg/mlEthanol: 10 mg/ml
λmax
264 nm
SMILES
NC(C(C=NC(N[C@@H]1CCCC[C@@H]1N)=N2)=C2NC3=CC(N4N=CC=N4)=CC=C3)=O
InChi Code
InChI=1S/C19H23N9O/c20-15-6-1-2-7-16(15)26-19-22-11-14(17(21)29)18(27-19)25-12-4-3-5-13(10-12)28-23-8-9-24-28/h3-5,8-11,15-16H,1-2,6-7,20H2,(H2,21,29)(H2,22,25,26,27)/t15-,16+/m0/s1
InChi Key
TXGKRVFSSHPBAJ-JKSUJKDBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    500 µg

    $60

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    1 mg

    $104

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    5 mg

    $228

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    10 mg

    $393

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    Product Description

    BIIB-057 is a potent inhibitor of the non-receptor tyrosine kinase Syk (IC50 = 1 nM).1 It displays at least 80-fold selectivity for Syk over other kinases. BIIB-057 blocks B cell receptor-mediated cell signaling and activation in whole blood (IC50s = 0.27 and 0.28 µM, respectively), as well as Fcɛ receptor 1-mediated basophil degranulation (IC50 = 0.15 µM).1 It antagonizes chemokine production, cell migration, and survival of chronic lymphocytic leukemia (CLL) cells after B cell receptor activation and synergistically enhances the action of fludarabine (Item No. 14128) in killing CLL cells.2,3 BIIB-057 is orally bioavailable, as it produces dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis.1 It also prevents splenomegaly and inhibits non-Hodgkin lymphoma tumor growth in a xenograft model.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Coffey, G., DeGuzman, F., Inagaki, M., et al. Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis. J. Pharmacol. Exp. Ther. 340(2), 350-359 (2012).

    2. Hoellenriegel, J., Coffey, G.P., Sinha, U., et al. Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration. Leukemia 26(7), 1576-1583 (2012).

    3. Spurgeon, S.E., Coffey, G., Fletcher, L.B., et al. The selective Syk inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia. J. Pharmacol. Exp. Ther. 344(2), 378-387 (2015).