PCI-32765 Racemate
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.
| Storage | Store at RT |
| M.Wt | 440.5 |
| Cas No. | 936563-87-0 |
| Formula | C25H24N6O2 |
| Solubility | Soluble in DMSO |
| Chemical Name | 1-[3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one |
| SDF | Download SDF |
| Canonical SMILES | C=CC(=O)N1CCCC(C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C5)C(=NC=N3)N |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
