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About This Item
Empirical Formula (Hill Notation):
C22H18FN7O
CAS Number:
Molecular Weight:
415.42
MDL number:
NACRES:
NA.21
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Application
Idelalisib may be used to study:
- its inhibitory effects on transforming growth factor (TGF) -β2 -stimulated Akt activation, fibronectin expression and collagen gel contraction in human RPE cells
- its effects on the anti-tumor action of CDK4/6 inhibitor palbociclib via Polo-like kinase 1 (PLK1) in B-cell lymphoma
Biochem/physiol Actions
Idelalisib (CAL-101; GS-1101) is an orally active, potent and subtype-selective, in vitro and in vivo, phosphatidylinositol-3-kinase p110delta (PI3Kδ) inhibitor (PI3Kδ/γ/β/α IC50 = 2.5/89/565/820 nM, IC50 = 978 nM/hVPS34, 6.73 µM/DNA-PK, >1 µM/CIIβ & mTOR) that induces apoptosis in diffuse large B-cell lymphoma, follicular lymphoma, and B-ALL cell cultures (0.5-1 µM for 24h) by blocking constitutive PI3K pathway activation.
Regulatory Information
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