Ruxolitinib ( INCB18424 ) is potent, selective JAK1 and JAK2 inhibitors (IC50 at 2.7 and 4.5nM, respectively) with potent antitumor and immunomodulatory activities. Ruxolitinib inhibited IL-6 signaling (IC50=281nM) and proliferation of JAK2V617F+Ba/FChemicalbook3 cells (IC50=127nM). Ruxolitinib also inhibited STAT3 phosphorylation in wild-type JAK2 and JAK2V617F mutants. Clinical application of it can significantly reduce the levels of circulatory inflammatory cytokines. ruxolitinib was effective in rat adjuvant arthritis and multiple rat arthritis models.

 

Brand: BCM

 

Target: Apoptosis; Autophagy; Tyrosine Kinases; JAK; Mitophagy

 

Signaling Pathways: Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors

 

Melting Point: 84-89°C

 

pKa: 11.63±0.50(Predicted)

 

Solubility: Soluble in DMSO (up to 28 mg/ml) or in Ethanol (up to 15 mg/ml with warming).

 

Application status: Ruxolitinib (also known as rucotinib) is a kinase inhibitor used for the treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, myelofibrosis after polycythemia vera, and myelofibrosis after thrombocythemia essential. ruxolitinib (Jakavi), an oral JAK1 and JAK2 tyrosine kinase inhibitor, was approved in the EU in August 2012 for the treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, Myelofibrosis after polycythemia vera and myelofibrosis after primary Chemicalbook thrombocythemia. Currently, Rusolitinib Jakavi has been approved by more than 50 countries worldwide, including the European Union, Canada and a number of countries in Asia, Latin America and South America. Novartis licensed the development and commercialization rights for Ruxolitinib outside the United States from Incyte. Both the European Commission and the FDA have granted orphan drug status to Ruxolitinib for the treatment of myelofibrosis. Incyte is already being marketed in the United States under the trade name Jakafi for the treatment of intermediate or high-risk myelofibrosis.

 

GHS: GHS07,GHS08

 

Isomeric SMILES: C1CCC(C1)[C@@H](CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3  

 

InChIKey: HFNKQEVNSGCOJV-OAHLLOKOSA-N  

 

InChI: InChI=1S/C17H18N6/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16/h6,8-12,15H,1-5H2,(H,19,20,21)/t15-/m1/s1 

 

Attribute
[CAS No.]	941678-49-5
[EINECS]	1312995-182-4
[MDL No.]	MFCD12031592
[Formula]	C17H18N6
[Molecular]	306.37
[Form]	White powder
[Storage]	-20°C
[Chem Name]	(3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile
[Synonym]	Ruxolitinib; (R)-Ruxolitinib; INCB018424
[Risk Codes]	H302-H360FD

Goods Tag