IPI-549 – 5 mg

Brand:
Cayman
CAS:
1693758-51-8
Storage:
-20
UN-No:
De Minimis - 3077 / 9

IPI-549 is an inhibitor of PI3Kγ (IC50s = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively).{42626} It is greater than 100-fold selective for PI3Kγ over a panel of 468 mutant and nonmutant protein and lipid kinases, including Class II PI3K isoforms, and a panel of 80 G protein-coupled receptors, ion channels, and transporters at 10 µM. It inhibits phosphorylation of AKT S473 in SKOV3, 786-0, RAW 264.7, and RAJI cells and inhibits migration of bone marrow-derived macrophages (BMDMs) (IC50 = 85 nM). IPI-549 sensitizes doxorubicin-resistant SW620/Ad300 cells to P-glycoprotein (P-gp) substrates, such as paclitaxel (IC50s = 710 and 6.7 nM for paclitaxel alone and in combination with IPI-549, respectively), and increases the level of intracellular paclitaxel in SW620/Ad300 cells.{42627} It also enhances the tumor growth reduction of paclitaxel (Item No. 10461) in an SW620/Ad300 mouse xenograft model when administered at a dose of 3 mg/kg in combination with paclitaxel.  

 

Available on backorder

SKU: 26416 - 5 mg Category:

Description

An inhibitor of PI3Kγ (IC50s = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively); selective for PI3Kγ over a panel of 468 mutant and nonmutant protein and lipid kinases and a panel of G protein-coupled receptors, ion channels, and transporters at 10 µM; inhibits migration of BMDMs (IC50 = 85 nM); sensitizes doxorubicin-resistant SW620/Ad300 cells to P-gp substrates, such as paclitaxel (IC50s = 710 and 6.7 nM for paclitaxel alone and in combination with IPI-549, respectively); enhances the tumor growth reduction of paclitaxel in an SW620/Ad300 mouse xenograft model at 3 mg/kg in combination with paclitaxel


Formal name: 2-amino-N-[(1S)-1-[1,2-dihydro-8-[2-(1-methyl-1H-pyrazol-4-yl)ethynyl]-1-oxo-2-phenyl-3-isoquinolinyl]ethyl]-pyrazolo[1,5-a]pyrimidine-3-carboxamide

Synonyms: 

Molecular weight: 528.6

CAS: 1693758-51-8

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cancer|Multidrug Resistance||Research Area|Immunology & Inflammation|Innate Immunity