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PCI-29732

Cat. No. M9889
PCI-29732 Structure
Synonym:

PCI29732

Size Price Availability Quantity
5mg USD 130.5  USD145 In stock
10mg USD 189  USD210 In stock
25mg USD 391.5  USD435 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PCI-29732 is a potent, reversible BTK inhibitor. PCI-29732 blocks B cell antigen receptor (BCR)-mediated gene expression in CD20+ B cells. PCI-29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 and enhances the anti-tumor efficacy of substrate chemotherapeutic agents. In vivo, PCI-29732 (20 mg/kg; p.o.; 5 times/3 days) enhances the anticancer efficacy of Topotecan in the H460/MX20 cell xenograft nude mice model.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 371.44
Formula C22H21N5O
CAS Number 330786-25-9
Purity >99%
Solubility DMSO ≥ 45 mg/mL
Storage at -20°C
References

PCI29732, a Bruton's Tyrosine Kinase Inhibitor, Enhanced the Efficacy of Conventional Chemotherapeutic Agents in ABCG2-Overexpressing Cancer Cells
Chunlei Ge, et al. Cell Physiol Biochem. 2018;48(6):2302-2317. PMID: 30114704.

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy
Lee A Honigberg, et al. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80. PMID: 20615965.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PCI-29732, PCI29732 supplier, BTK, inhibitors

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