A potent ATP mimetic that inhibits JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM

Ruxolitinib (phosphate) – 25 mg

Brand:
Cayman
CAS:
1092939-17-7
Storage:
-20
UN-No:
Non-Hazardous - /

Ruxolitinib is a potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively, and is relatively less selective for JAK3 (IC50 = 322 nM).{21781} It blocks interleukin-6 (IL-6) signaling (IC50 = 281 nM) and proliferation of JAK2V617F+ Ba/F3 cells (IC50 = 127 nM).{21782} In primary cultures, ruxolitinib preferentially suppresses erythroid progenitor colony formation from JAK2V617F+ polycythemia vera patients (IC50 = 67 nM) versus healthy donors (IC50 > 400 nM). In a mouse model of JAK2V617F+ myeloproliferative neoplasms (MPN), 90 mg/kg ruxolitinib reduces splenomegaly, decreases circulating levels of IL-6 and TNF-α, eliminates neoplastic cells, and prolongs survival.  

 

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SKU: 23215 - 25 mg Category:

Description

A potent ATP mimetic that inhibits JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively; less selective for JAK3 (IC50 = 322 nM); blocks IL-6 signaling (IC50 = 281 nM) and proliferation of JAK2V617F+ Ba/F3 cells (IC50 = 127 nM); reduces splenomegaly, decreases circulating levels of IL-6 and TNF-α, eliminates neoplastic cells, and prolongs survival in a mouse model of JAK2V617F+ MPN,

Formal name: βR-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile, monophosphate

Synonyms:  INC 424 (phosphate)|INCB 018424 (phosphate)

Molecular weight: 404.4

CAS: 1092939-17-7

Purity: ≥98%

Formulation: A crystalline solid

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

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