A multi-kinase inhibitor; inhibits BTK

PCI-29732 – 10 mg

Brand:
Cayman
CAS:
330786-25-9
Storage:
-20
UN-No:
Non-Hazardous - /

PCI-29732 is a multi-kinase inhibitor.{45563} 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).{45564} 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.  

 

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Description

A multi-kinase inhibitor; inhibits BTK, 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; inhibits calcium flux in Ramos B cells and phosphorylation of PLCɣ1 (IC50s = 0.53 and 0.33 µM, respectively); 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); in combination with topotecan, reduces tumor growth in an H460/MX20 mouse xenograft model at 20 mg/kg

Formal name: 1-cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

Synonyms: 

Molecular weight: 371.4

CAS: 330786-25-9

Purity: ≥98%

Formulation: A crystalline solid

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