An ATP-competitive inhibitor of JAK1 and JAK2 (IC50s = 11 and 18 nM

CYT387 – 10 mg

Brand:
Cayman
CAS:
1056634-68-4
Storage:
-20
UN-No:
Non-Hazardous - /

CYT387 is an ATP-competitive inhibitor of the Janus kinases JAK1 and JAK2 (IC50s = 11 and 18 nM, respectively).{28486,27397} It displays significantly less activity against other kinases, including JAK3 (IC50 = 0.16 µM).{28486} At 0.5 to 1.5 µM, CYT387 causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines.{28486} It is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms, although kinase domain mutations can confer resistance.{28486,28485} CYT387 also blocks paclitaxel-induced JAK2 activation in ovarian cancer cells, preventing the development of a cancer stem cell-like population following chemotherapy.{28484}  

 

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Description

An ATP-competitive inhibitor of JAK1 and JAK2 (IC50s = 11 and 18 nM, respectively); causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines; is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms

Formal name: N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide

Synonyms:  Momelotinib

Molecular weight: 414.5

CAS: 1056634-68-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cell Biology|Cell Signaling|JAK Signaling

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