PCI-29732
A selective and irreversible Btk inhibitor with biochemical Ki of 8.2 nM; also inhibits Lck and Lyn with Ki of 4.6 and 2.5 nM. (In Vitro) :PCI29732 shows cytotoxicity in different cells. The IC50 values are 7.94 μM for S1, 7.79 μM for S1-MI-80, 6.55 μM for H460, 6.34 μM for H460/MX20, 6.14 μM for KB, 6.02 μM for KBv200, 12.45 μM for HEK293/pcDNA3, 14.58 μM for HEK293-ABCG2-482-R2, and 13.24 μM for HEK293-ABCG2-482-T7 cells.PCI-29732 blocks the transcriptional up-regulation of a panel of B-cell activation genes in human CD20+ B cells stimulated at the B-cell antigen receptor (BCR) . (In Vivo) :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.PCI 29732 (20 mg/kg; p.o.; every 3 d x 5 times) enhances the anticancer efficacy of Topotecan in the H460/MX20 cell xenograft nude mice model.
Product Specifications
CAS Number
330786-25-9
Product Name Alternative
PCI29732 | PCI 29732
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 53 mg/mL
Smiles
NC1=C2C (N (C3CCCC3) N=C2C4=CC=C (OC5=CC=CC=C5) C=C4) =NC=N1
Molecular Formula
C22H21N5O
Molecular Weight
371.435
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 1-cyclopentyl-3- (4-phenoxyphenyl) -
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