A selective JAK2 inhibitor that blocks signaling (IC50 = 58 nM at 5 mM ATP) and proliferation of JAK2-expressing cell lines (GI50 = 60 nM); displays good pharmacokinetics in vivo

AZD1480 – 10 mg

Brand:
Cayman
CAS:
935666-88-9
Storage:
-20
UN-No:
Non-Hazardous - /

Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2 where a switch from valine to phenylalanine occurs at the 617 position (V617F).{27171} AZD1480 is a potent JAK2 inhibitor that blocks signaling (IC50 = 58 nM at 5 mM ATP) and proliferation of JAK2-expressing cell lines (GI50 = 60 nM).{29735,18888} It is selective for JAK2 over other JAK family members as well as a panel of related kinases.{18888} AZD1480 also inhibits the growth of cells expressing the V617F mutant of JAK2 (GI50 = 60 nM).{18888} It reversibly blocks JAK2-mediated phosphorylation of STAT3 and STAT5.{18888} AZD1480 displays good pharmacokinetics in vivo, inhibits STAT3 and STAT5 activation in vivo, and suppresses tumorigenesis in mouse xenografts harboring constitutive STAT3 activity.{29735,18888} In addition to suppressing myeloma cell growth and survival, AZD1480 reduces angiogenesis and metastasis in vitro and in human xenograft tumor models.{29736,29737}  

 

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SKU: 10702 - 10 mg Category:

Description

A selective JAK2 inhibitor that blocks signaling (IC50 = 58 nM at 5 mM ATP) and proliferation of JAK2-expressing cell lines (GI50 = 60 nM); displays good pharmacokinetics in vivo, inhibits STAT3 and STAT5 activation in vivo, and suppresses tumorigenesis in mouse xenografts harboring constitutive STAT3 activity

Formal name: 5-chloro-N2-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine

Synonyms: 

Molecular weight: 348.8

CAS: 935666-88-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|JAK Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cancer|Transcription Factors|STATs||Research Area|Cell Biology|Cell Signaling|JAK Signaling

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