Btk Kinase inhibitor

Btk Kinase inhibitor Basic information
Product Name:Btk Kinase inhibitor
Synonyms:Btk Kinase inhibitor;ONO BTK;ONO-4059(GS-4059,Tirabrutinib) free base;ONO-BKT;6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one;Tirabrutinib (ONO-4059);ONO-4059;ONO 4059;ONO4059;6-amino-9-[(3R)-1-(but-2-ynoyl)pyrrolidin-3-yl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one
CAS:1351636-18-4
MF:C25H22N6O3
MW:454.48
EINECS:
Product Categories:
Mol File:1351636-18-4.mol
Btk Kinase inhibitor Structure
Btk Kinase inhibitor Chemical Properties
Boiling point 672.0±65.0 °C(Predicted)
density 1.412±0.06 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO:65.0(Max Conc. mg/mL);143.02(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.3(Max Conc. mg/mL);0.66(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);66.01(Max Conc. mM)
Ethanol:1.0(Max Conc. mg/mL);2.2(Max Conc. mM)


form A crystalline solid
pka3.16±0.20(Predicted)
Safety Information
MSDS Information
Btk Kinase inhibitor Usage And Synthesis
DescriptionBtk Kinase inhibitor is highly potent and selective orally administered, small molecule, and also named tirabrutinib, Brutons tyrosine kinase (BTK) inhibitor being developed by Ono pharmaceutical and its licensee Gilead Sciences for the treatment of autoimmune disorders and haematological malignancies. 
Mechanism of actionThe selective inhibition of cell growth by Btk Kinase inhibitor was due to blocking of BTK-mediated signaling through AKT and cellular protein kinase D. It can inhibit autophosphorylation of the BTK at the Tyr223 position through the ERK, AKT and PKD signaling pathways.
Side effectsAdverse effects of the Btk Kinase inhibitor that occurred in some patients were rash, vomiting, neutropenia, arthralgia, and malaise, and drug-related Grade 3–4 Adverse effects were neutropenia, leukopenia, anemia, hypophosphatemia, PT-INR increased, pneumonitis, and acute myeloid leukemia. in prior Japanese studies, rash, hematologic adverse effects, erythema multiforme, and constipation were frequent adverse effects in a Phase I/II study of some patients with PCNSL, and rash, hematologic adverse effects, and stomatitis were the most common adverse effects in a Phase II study of some patients with WM.
ONO-4059 (hydrochloride)

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