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Idelalisib

CAS No. : 870281-82-6

MCE 国际站：Idelalisib

产品活性：Idelalisib (CAL-101; GS-1101) 是一种口服有效的高选择性 p110δ 抑制剂，IC₅₀ 为 2.5 nM，比 p110δ 和其他 PI3K class I 酶的选择性高 40 到 300 倍。

研究领域：PI3K/Akt/mTOR | Autophagy

作用靶点：PI3K | Autophagy

In Vitro: Idelalisib (CAL-101; GS-1101) is a highly selective and potent p110δ inhibitor (EC₅₀=8 nM). Greater selectivity (400- to 4000-fold) is seen against related kinases C2β, hVPS34, DNA-PK, and mTOR, whereas no activity is observed against a panel of 402 diverse kinases at 10 µM. CAL-101 reduces PDGF-induced pAkt by only 25% at 10 µM. Idelalisib (CAL-101) inhibits LPA-induced pAkt with an EC₅₀ of 1.9 µM. Idelalisib (CAL-101) blocks FcϵRI p110δ-mediated CD63 expression with an EC₅₀ of 8 nM, whereas formyl-methionyl-leucyl-phenylalanine activation of p110γ is inhibited with an EC₅₀ of 3 µM. Thus, in cell-based assays, CAL-101 has 240- to 2500-fold selectivity for p110δ over the other class I PI3K isoforms. CAL-101Idelalisib (CAL-101)-induced apoptosis of chronic lymphocytic leukemia (CLL) cells is significant compare with vehicle treatment alone (P<0.001). Idelalisib (CAL-101) induces selective cytotoxicity in CLL cells independent of IgVH mutational status or interphase cytogenetics.

In Vivo: A significant reduction is observed in the CD11b⁺Ly6G⁺ neutrophils from brain homogenates of bothp110δ^D910A/D910A mice and Idelalisib (CAL-101) (40 mg/kg, i.v.) post-treated mice.

相关产品：Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | FDA-Approved Drug Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Oxygen Sensing Compound Library | Anti-COVID-19 Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Drug-Induced Liver Injury (DILI) Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Targeted Therapy Drug Library | 3-Methyladenine | LY294002 | Wortmannin | Quercetin | 740 Y-P | PI-103 | Isorhamnetin | Recilisib | Autophinib | AZD 6482 | PI3K-IN-1 | TG100-115 | α-Linolenic acid | TGX-221 | 1-Deoxynojirimycin | YS-49 | AS-605240 | PKI-402 | Disitertide | Erucic acid | CNX-1351 | GSK1059615 | Sonolisib | 1,3-Dicaffeoylquinic acid | GNE-317 | Esculetin | HS-173 | Oroxin B

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