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Cerdulatinib
- PRT 062070
- Soluble in DMSO
- MF: C20H27N7O3S
- MW: 445.54
Description
Cerdulatinib is an orally active kinase inhibitor that demonstrates activity against Syk and JAK with IC50 values of 32 nM, 12 nM, 6 nM and 8 nM for Syk, JAK1, JAK2 and JAK3, respectively. Cellular assays demonstrated specific inhibitory activity against signaling pathways that use Syk and JAK1/3. Limited inhibition of JAK2 was observed. Potent antitumor activity was observed in a subset of B-cell lymphoma cell lines.
More Information
| Parent CAS No. | 1198300-79-6 |
|---|---|
| Chemical Name | 4-(Cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide |
| SMILES | C1(N2CCN(S(=O)(=O)CC)CC2)C=CC(NC2N=C(NC3CC3)C(C(=O)N)=CN=2)=CC=1 |
| MFCD | N.A. |
| InChi | 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) |
| InChiKey | BGLPECHZZQDNCD-UHFFFAOYSA-N |
| CID | 44595079 |
| Short Description | Syk/JAK inhibitor |
References
- G Coffey et al. The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer. J Pharmacol Exp Ther. 2014 Dec;351(3):538-48.
- MD Blunt et al. The SykJak Inhibitor Cerdulatinib (PRT062070) Shows Promising Preclinical Activity in Chronic Lymphocytic Leukemia By Antagonising B Cell Receptor and Microenvironmental Signalling. Blood 2015 126:1716
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