A multi-kinase inhibitor
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PCI-29732

Item No. 29036

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
CAS Number
330786-25-9
Molecular Formula
C22H21N5O
Formula Weight
371.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:2): 0.3 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/ml
λmax
262, 289 nm
SMILES
NC1=C(C(C2=CC=C(OC3=CC=CC=C3)C=C2)=NN4C5CCCC5)C4=NC=N1
InChi Code
InChI=1S/C22H21N5O/c23-21-19-20(26-27(16-6-4-5-7-16)22(19)25-14-24-21)15-10-12-18(13-11-15)28-17-8-2-1-3-9-17/h1-3,8-14,16H,4-7H2,(H2,23,24,25)
InChi Key
GMJUPMONHWAZCP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $253

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    25 mg

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    Product Description

    PCI-29732 is a multi-kinase inhibitor.1 It inhibits the Tec family kinase BTK and the Src family kinases LCK and LYN (Kis = 8.2, 4.6, and 2.5 nM, respectively), as well as the activity of three receptor tyrosine kinases and seven non-receptor tyrosine kinases by greater than 90% in a panel of over 100 kinases at 10 µM. PCI-29732 inhibits calcium flux in Ramos B cells and phosphorylation of phospholipase Cɣ1 (PLCɣ1) with IC50 values of 0.53 and 0.33 µM, respectively. It is cytotoxic to S1-MI-80, H460/MX20, and KBv200 cancer cells overexpressing the ATP-binding cassette transporter (IC50s = 7.8, 6.3, and 6.02 µM, respectively).2 PCI-29732 (20 mg/kg), in combination with the DNA topoisomerase I inhibitor topotecan (Item No. 14129), reduces tumor growth in an H460/MX20 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pan, Z., Scheerens, H., Li, S.J., et al. Discovery of selective irreversible inhibitors for Bruton’s tyrosine kinase. ChemMedChem 2(1), 58-61 (2007).

    2. Ge, C., Wang, F., Ciu, C., et al. PCI29732, a Bruton’s tyrosine kinase inhibitor, enhanced the efficacy of conventional chemotherapeutic agents in ABCG2-overexpressing cancer cells. Cell. Physiol. Biochem. 48(6), 2302-2317 (2018).