SML4246
Idelalisib
≥98% (HPLC)
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
生化/生理作用
Orally active, potent and subtype-selective phosphatidylinositol-3-kinase p110delta (PI3Kδ) inhibitor in vitro and in vivo.
Idelalisib (CAL-101; GS-1101) is an orally active, potent and subtype-selective 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.
Idelalisib (CAL-101; GS-1101) is an orally active, potent and subtype-selective 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.
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