PCI-32765 (RaceMate) Chemical Properties

Boiling point:

715.0±60.0 °C(Predicted)

Density 

1.34±0.1 g/cm3(Predicted)

storage temp. 

-20C

solubility 

Soluble in DMSO

form 

White crystalline solid

pka

4.09±0.30(Predicted)

color 

White to off-white

PCI-32765 (RaceMate) Usage And Synthesis

Uses

Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.

Definition

ChEBI: 1-[3-[4-amino-3-(4-phenoxyphenyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinyl]-2-propen-1-one is an aromatic ether.

Biological Activity

pci-32765 is an inhibitor of bruton tyrosine kinase (btk) with ic50 value of 0.5nm [1].pci-32765 is a covalent and irreversible inhibitor of btk through bonding to cys-481 in the atp binding domain. pci-32765 inhibits phosphorylation of btk in a b cells (ic50 of 11nm) as well as the downstream substrates phosphoinositide phospholipase cγ (plc γ) and erk in cell assays. pci-32765 has in vivo efficacy in b cell lymphoma. in cll cells, pci-32765 induces cells apoptosis through inhibiting the expression of bcr-dependent udp-glucose ceramide glucosyltransferase [1].pci-32765 is oral effective in vivo. it induces lymphocytosis during the first weeks of therapy in patients with cll. it is also efficacious in autoimmune disease. in the mrl-fas lupus model, pci-32765 inhibits collagen-induced arthritis as well as autoantibody production and development of kidney disease. it also diminished fcγriii-induced production of pro-inflammatory cytokines [1].

References

[1] burger ja, buggy jj. bruton tyrosine kinase inhibitor ibrutinib (pci-32765). leuk lymphoma. 2013 nov;54(11):2385-91.