Identification | Back Directory | [Name]
PCI-32765 (RaceMate) | [CAS]
936563-87-0 | [Synonyms]
Ibrutinib Racemate PCI-32765 (RaceMate) IBRUTINIB RACEMATE (PCI-32765 RACEMATE) Bruton's Tyrosine Kinase Inhibitor III - CAS 936563-87-0 - Calbiochem 1-[3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one 1-(3-(4-Amino-3-(4-phenyloxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one 2-Propen-1-one, 1-[3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]- | [Molecular Formula]
C25H24N6O2 | [MDL Number]
MFCD12032093 | [MOL File]
936563-87-0.mol | [Molecular Weight]
440.5 |
Chemical Properties | Back Directory | [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 |
Hazard Information | Back Directory | [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. |
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Company Name: |
SPIRO PHARMA
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Tel: |
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Website: |
www.spiropharma.com.cn |
Company Name: |
Musechem
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Tel: |
+1-800-259-7612 |
Website: |
www.musechem.com |
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