PCI 29732

Catalog No.S6725 Batch:S672501

Print

Technical Data

Formula

C22H21N5O
Molecular Weight 371.43 CAS No. 330786-25-9
Solubility (25°C)* In vitro DMSO 74 mg/mL (199.23 mM)
Ethanol 4 mg/mL (10.76 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description PCI 29732 is a selective and irreversible Btk inhibitor with an IC50 of 0.5 nM.
Targets
BTK [1]
(Cell-free assay)		 BLK [1]
(Cell-free assay)		 Bmx [1]
(Cell-free assay)		 EGFR [1]
(Cell-free assay)		 YES [1]
(Cell-free assay)		 View More
0.5 nM 0.5 nM 0.8 nM 5.6 nM 6.5 nM
In vitro

PCI-32765 blocks BCR signaling in human peripheral B cells at concentrations that does not affect T cell receptor signaling. In DOHH2 cells, PCI-32765 inhibits autophosphorylation of Btk (IC50, 11 nM), phosphorylation of Btk’s physiological substrate PLCγ(IC50, 29 nM), and phosphorylation of a further downstream kinase, ERK (IC50, 13 nM). PCI-32765 is more than 1,000-fold selective for inhibition of antigen receptor signaling in B cells over T cells, and that only B-cell inhibition is sustained following short duration treatment[1].
In vivo

In mice with collagen-induced arthritis, orally administered PCI-32765 reduces the level of circulating autoantibodies and completely suppresses disease. PCI-32765 also inhibits autoantibody production and the development of kidney disease in the MRL-Fas(lpr) lupus model. The mean terminal plasma half-life of PCI-32765 following oral dosing in mice is 1.7 to 3.1 h[1].

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Arthritic DBA/1 mice

  • Dosages

    3.125, 12.5, or 50 mg/kg per day

  • Administration

    oral

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.