TL-895

• Description :

  TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor. TL-895 is active against recombinant BTK (average IC50: 1.5 nM) and inhibits only three additional kinases BLK, BMX (IC50 = 1.6 nM) and TXK with IC50 within tenfold of BTK activity. TL-895 inhibits BTK auto-phosphorylation at the Y223 phosphorylation site (IC50: 1-10 nM) . The TL-895 effectively inhibits the production of inflammatory factors such as IL-8, IL-1β, MCP-1 and TNF-α by monocytes or macrophages, and reduces the chemotactic migration of MF cells towards SDF-1. TL-895 is used be for studies of chronic lymphocytic leukemia (CLL), myelofibrosis (MF), and B-cell malignancies[1][2][3].

• UNSPSC :

  12352005

• Target :

  BMX Kinase; Btk; Interleukin Related; TNF Receptor

• Type :

  Reference compound

• Related Pathways :

  Apoptosis; Immunology/Inflammation; Protein Tyrosine Kinase/RTK

• Applications :

  COVID-19-anti-virus

• Field of Research :

  Cancer; Inflammation/Immunology

• Assay Protocol :

  https://www.medchemexpress.com/tl-895.html

• Concentration :

  10mM

• Purity :

  99.86

• Solubility :

  DMSO : 250 mg/mL (ultrasonic)

• Smiles :

  O=C(N1CCC(CNC2=NC=NC(N)=C2C3=CC=C(C=C3)OC4=CC=CC=C4)(CC1)F)C=C

• Molecular Formula :

  C25H26FN5O2

• Molecular Weight :

  447.50

• References & Citations :

  [1]Valeria Di Battista, et al. Genetics and Pathogenetic Role of Inflammasomes in Philadelphia Negative Chronic Myeloproliferative Neoplasms: A Narrative Review. Int J Mol Sci|[2]A Study of TL-895 With Standard Available Treatment Versus Standard Available Treatment for the Treatment of COVID-19 in Patients With Cancer|[3]Study of TL-895 in Subjects With Myelofibrosis|[4]Richard D Caldwell, et al. Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases. J Med Chem. 2019 Sep 12;62(17):7643-7655.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  IL-1; IL-6; IL-8

• CAS Number :

  [1415823-49-2]