XL019

SKU: orb1304569

Description

XL019 is a highly selective small molecule inhibitor of JAK2, exhibiting potent activity with an IC50 of 2.2 nM and demonstrating 100-fold selectivity against JAK1. It is a valuable research tool for studying JAK2-dependent signaling in cellular assays and has been utilized in preclinical models of myeloproliferative neoplasms.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 945755-56-6
• MW: 444.53
• Purity: 99.23% (May vary between batches)
• Formula: C₂₅H₂₈N₆O₂
• SMILES: O=C(Nc1ccc(cc1)-c1ccnc(Nc2ccc(cc2)N2CCOCC2)n1)[C@@H]1CCCN1
• Target: JAK,FLT,PDGFR,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.5 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:13 mg/mL (29.24 mM)

Bioactivity

• Target IC50:
  JAK3:214.2 nM|JAK2:2.2 nM
• In Vivo:
  L019 inhibits the activation of both JAK2 and its mutant form, JAK2V617F, leading to suppression of the JAK-STAT signaling pathway and inducing apoptosis. Compared to other cellular systems, upon EPO stimulation of the erythroid lineage, L019 demonstrates more than a tenfold selective inhibition of STAT5 phosphorylation (IC50 = 64 nM).
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• In Vitro:
  XL019 exhibits superior pharmacokinetic properties, demonstrating efficient oral absorption, moderate clearance rates, and half-life across various species. Administration of XL019 at 30, 100, and 300 mg/kg significantly inhibits the downstream markers pSTAT1 and pSTAT3, with the effective dose (ED50) for pSTAT1 being 42 mg/kg and for pSTAT3, 210 mg/kg. Furthermore, XL019 effectively suppresses the growth of HEL.92.1.7 xenograft tumors in mice, with dosages of 200 mg/kg and 300 mg/kg administered twice daily for 14 days, achieving tumor growth inhibition rates of 60% and 70%, respectively.
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Storage & Handling

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

Alternative Names

FLT3, Inhibitor, oral, inhibit, JAK2, JAK1, JAK, Janus kinase, JAK3, Apoptosis, antitumor,HEL.92.1.7, cells, tumor, PDGFRβ, selective, phosphorylation, XL 019, XL019, XL-019

Compound Identifiers

PubChem CID

57990869