A cell permeable inhibitor of the PI3K catalytic subunit p110δ (IC50 = 2.5 nM) that demonstrates 40- to 300-fold selectivity against other PI3K class I enzymes (IC50s = 820

CAL-101 – 25 mg

Brand:
Cayman
CAS:
870281-82-6
Storage:
-20
UN-No:
Non-Hazardous - /

The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival.{13740,17822} CAL-101 is a cell permeable inhibitor of the PI3K catalytic subunit p110δ (IC50 = 2.5 nM) that demonstrates 40- to 300-fold selectivity against other PI3K class I enzymes (IC50s = 820, 565, and 89 nM for p110α, β, and γ, respectively).{25028} At 1 μM it can block constitutive PI3K signaling in malignant B-cell lines and primary patient tumor cells, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase, and apoptosis.{25028} It has also been shown to inhibit the chemotaxis of chronic lymphocytic leukemia cells and to downregulate the secretion of chemokines triggered by B-cell receptor signaling.{25029}  

 

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Description

A cell permeable inhibitor of the PI3K catalytic subunit p110δ (IC50 = 2.5 nM) that demonstrates 40- to 300-fold selectivity against other PI3K class I enzymes (IC50s = 820, 565, and 89 nM for p110α, β, and γ, respectively); blocks constitutive PI3K signaling in malignant B-cell lines and primary patient tumor cells, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and apoptosis

Formal name: 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4(3H)-quinazolinone

Synonyms:  Idelalisib|GS-1101

Molecular weight: 415.4

CAS: 870281-82-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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