Bulk Inquiry
Momelotinib
- CYT387
- Soluble in DMSO
- MF: C23H22N6O2
- MW: 414.46
Description
Selective and ATP-competitive Janus Kinase JAK1/JAK2 inhibitor, with IC50 to be 11 and 18 nM for JAK1 and JAK2 respectively and far less activity against other kinases, including JAK3 (IC50=155 nM). The hydrochloride salt form, Momelotenib hydrochloride (Axon 4124) is also available.
More Information
| Parent CAS No. | 1056634-68-4 |
|---|---|
| Chemical Name | N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide |
| SMILES | C1=CC(=CC=C1C1=NC(NC2=CC=C(N3CCOCC3)C=C2)=NC=C1)C(NCC#N)=O |
| MFCD | MFCD16038899 |
| InChi | InChI=1S/C23H22N6O2/c24-10-12-25-22(30)18-3-1-17(2-4-18)21-9-11-26-23(28-21)27-19-5-7-20(8-6-19)29-13-15-31-16-14-29/h1-9,11H,12-16H2,(H,25,30)(H,26,27,28) |
| InChiKey | ZVHNDZWQTBEVRY-UHFFFAOYSA-N |
| CID | 25062766 |
| Short Description | JAK1/2 inhibitor |
References
- A Pardanan et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia 2009, 23, 1441–1445.
- JW Tyner et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood 2010, 115(25), 5232-5240.
- S Verstovsek. Therapeutic potential of JAK2 inhibitors. Hematology Am Soc Hematol Educ Program. 2009, 636-642.
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