SML4246

Idelalisib

Name: Idelalisib
Brand: SIGMA

≥98% (HPLC), powder, PI3Kδ inhibitor

别名:

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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关于此项目

经验公式（希尔记法）:

C₂₂H₁₈FN₇O

化学文摘社编号:

870281-82-6

分子量:

415.42

MDL number:

MFCD35086135

NACRES:

NA.21

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Quality Level

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.