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TL-895

CAT: 0804-HY-139481-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-139481-01Size:5 mg
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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].
CAS Number
[1415823-49-2]
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

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