A dual inhibitor of Syk and JAKs
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Cerdulatinib

Item No. 20076

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(cyclopropylamino)-2-[[4-[4-(ethylsulfonyl)-1-piperazinyl]phenyl]amino]-5-pyrimidinecarboxamide
CAS Number
1198300-79-6
Synonyms
  • PRT062070
  • PRT2070
Molecular Formula
C20H27N7O3S
Formula Weight
445.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml
λmax
233, 285, 328 nm
SMILES
CCS(N1CCN(C2=CC=C(NC3=NC(NC4CC4)=C(C(N)=O)C=N3)C=C2)CC1)(=O)=O
InChi Code
InChI=1S/C20H27N7O3S/c1-2-31(29,30)27-11-9-26(10-12-27)16-7-5-15(6-8-16)24-20-22-13-17(18(21)28)19(25-20)23-14-3-4-14/h5-8,13-14H,2-4,9-12H2,1H3,(H2,21,28)(H2,22,23,24,25)
InChi Key
BGLPECHZZQDNCD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    Cerdulatinib is a dual inhibitor of spleen tyrosine kinase (Syk) and Janus kinases (JAK; IC50s = 32, 12, 6, 8, and 0.5 nM for Syk, JAK1, JAK2, JAK3, and TYK2, respectively) and also exhibits nanomolar inhibition of other kinases.1 Syk is involved in the B cell receptor (BCR) pathway, and cerdulatinib inhibits downstream Syk-mediated signaling of ERK Y204 phosphorylation (IC50 = 0.5 μM), upregulates cell surface expression of CD69 (IC50 = 0.11 μM), and inhibits FcεRI-mediated basophil degranulation (IC50 = 0.12 μM).1 JAK is involved in JAK-STAT regulation of cytokine receptors. Cerdulatinib inhibits STAT3, STAT5, and STAT6 phosphorylation by interleukin-activated JAK1/3 with IC50 values ranging from 0.16 to 1 μM.1 Cerdulatinib disrupts JAK1/3-mediated signaling more selectively than JAK2 signaling (IC50 > 4 μM).1 Cerdulatinib displays potent antitumor activity against ABC and GCB types of diffuse large B cell lymphoma (DLBCL) by inducing apoptosis via caspase-2 and poly(ADP-ribose) polymerase (PARP) cleavage.2 Cerdulatinib exhibits IC50 values ranging from 0.05 to 2.1 μM against a panel of DLBCL tumor cell lines.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Coffey, G., Betz, A., DeGuzman, F., et al. The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J. Pharmacol. Exp. Ther. 351(3), 538-548 (2014).

    2. Ma, J., Xing, W., Coffey, G., et al. Cerdulatinib, a novel dual SYK/JAK kinase inhibitor, has broad anti-tumor activity in both ABC and GCB types of diffuse large B cell lymphoma. Oncotarget 6(41), 43881-43896 (2015).