Ruxolitinib phosphate

SKU: orb1227003

Description

A potent, selective, orally active JAK1/JAK2 inhibitor with IC50 of 3.3/2.8 nM, respectively; displays modest selectivity against Tyk2 (6-fold) and marked selectivity (>130-fold) against JAK3; inhibits IL-6 signaling (IC50=281 nM), and proliferation of JAK2V617F(+) Ba/F3 cells (IC50=127 nM); suppresses erythroid progenitor colony formation from JAK2V617F(+) polycythemia vera patients (IC50=67 nM) in primary cultures; markedly reduces level of inflammatory cytokines, and preferentially eliminates neoplastic cells in a mouse model of JAK2V617F(+) MPN.Bone Cancer Approved(In Vitro):Ruxolitinib (INCB018424) potently and selectively inhibits JAK2V617F-mediated signaling and proliferation. Ruxolitinib inhibits the growth of HEL cells with EC50 of 186 nM. Ruxolitinib markedly increases apoptosis in Ba/F3-EpoR-JAK2V617F cell system, and inhibits hematopoietic progenitor cell proliferation in primary MPN patient samples.(In Vivo):Ruxolitinib (180 mg/kg, p.o.) reduces the tumor burden of mice inoculated with JAK2V617F-expressing cells without causing anemia or lymphopenia.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1092939-17-7
• MW: 404.3602
• Purity: >98% (HPLC)
• Formula: C₁₇H₂₁N₆O₄P
• SMILES: C1CCC(C1)[C@@H](CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3.OP(=O)(O)O
• Target: JAK
• Solubility: DMSO: ≥ 31 mg/mL; H2O: 5.4 mg/mL (Need ultrasonic or warming)

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

INCB-018424 phosphate | Ruxolitinib

Quick Database Links

Gene Symbol

JAK