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SML4246

Idelalisib

≥98% (HPLC), powder, PI3Kδ inhibitor

Synonym(s):

CAL 101, CAL-101, CAL101, GS 1101, GS-1101, GS1101, 5-Fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one, N6-[(S)-1-(5-Fluoro-4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)propyl]adenine

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About This Item

Empirical Formula (Hill Notation):
C22H18FN7O
CAS Number:
870281-82-6
Molecular Weight:
415.42
MDL number:
MFCD35086135
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

100

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.

Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

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