A potent and selective Syk inhibitor
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PRT060318

Item No. 22476

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[(3-methylphenyl)amino]-5-pyrimidinecarboxamide
CAS Number
1194961-19-7
Synonyms
  • P142-76
  • PRT318
Molecular Formula
C18H24N6O
Formula Weight
340.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMF:PBS (pH7.2) (1:30): 0.03 mg/mlDMSO: InsoubleEthanol: InsoublePBS (pH 7.2): Insouble
λmax
250, 288 nm
SMILES
N[C@@H]1[C@H](NC2=NC=C(C(N)=O)C(NC3=CC(C)=CC=C3)=N2)CCCC1
InChi Code
InChI=1S/C18H24N6O/c1-11-5-4-6-12(9-11)22-17-13(16(20)25)10-21-18(24-17)23-15-8-3-2-7-14(15)19/h4-6,9-10,14-15H,2-3,7-8,19H2,1H3,(H2,20,25)(H2,21,22,23,24)/t14-,15+/m0/s1
InChi Key
NZNTWOVDIXCHHS-LSDHHAIUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $159

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    10 mg

    $302

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    25 mg

    $553

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    Product Description

    PRT060318 is a potent and selective inhibitor of spleen tyrosine kinase (Syk; IC50 = 4 nM).1,2 It is selective, inhibiting 92% of Syk activity, while other kinases retain >70% activity, at a concentration of 50 nM in a panel of 270 kinases.2 PRT060318 inhibits convulxin-induced aggregation of human platelet-rich plasma (IC50 = 2.5 μM) in vitro and prevents thrombosis in a transgenic mouse model of heparin-induced thrombocytopenia. It induces chronic lymphocytic leukemia (CLL) B cell apoptosis and inhibits the secretion of chemokines CCL3, CCL4, and CXCL13.3 PRT060318 also inhibits CLL B cell chemotaxis and pseudoemperipolesis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Woodford, M.R., Dunn, D.M., Blanden, A.R., et al. The FNIP co-chaperones decelerate the Hsp90 chaperone cycle and enhance drug binding. Nat. Commun. 7, 12037 (2016).

    2. Archari, G.A., and Ramesh, R. Characterization of bacteria degrading 3-hydroxy palmitic acid methyl ester (3OH-PAME), a quorum sensing molecule of Ralstonia solanacearum. Lett. Appl. Microbiol. 60(5), 447-455 (2015).

    3. 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).