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Formula | C22H18FN7O |
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Molecular Weight | 415.42 | CAS No. | 870281-82-6 | |
Solubility (25°C)* | In vitro | DMSO | 83 mg/mL (199.79 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Idelalisib (CAL-101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy. | ||||
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In vitro | CAL-101 is not sensitive to other PI3K class I subunits including p110α, p110β, and p110γ. CAL-101 specifically blocks FcϵR1 p110δ-mediated CD63 expression with an EC50 of 8 nM in primary basophil. CAL-101 exhibits greater activity in B-cell acute lymphoblastic leukemia (B-ALL) and chronic lymphocytic leukemia (CLL) cells compared with acute myeloid leukemia (AML) and myeloproliferative neoplasm (MPN) cells. CAL-101 produces the reduction in pAktS473, pAktT308, and the downstream target S6 in SU-DHL-5, KARPAS-422 and CCRF-SB cells with EC50 of 0.1 to 1.0 μM. [1] CAL-101 induces selective cytotoxicity in CLL cells independent of IgVH mutational status or interphase cytogenetics, primarily through a caspase-dependent mechanism. CAL-101 induces cytotoxicity preferentially to CLL cells compared with normal B cells, without producing cytotoxicity in other hematopoietic cells, compared to LY294002. CAL-101 lacks direct cytotoxic potential to T cells and nature killer (NK) cells. CAL-101 can inhibit production of inflammatory cytokines, such as IL-6, IL-10, TNF-α, and IFN-γ, and activation-induced cytokines, such as CD40L. CAL-101 also antagonizes CD40L-mediated CLL cell survival. [2] CAL-101 induces an accumulation of cells in G1 and a decrease in the S-phase population in L1236 and L591 cells, which indicates CAL-101 as a novel strategy for the treatment of hodgkin lymphoma (HL). [3] |
Kinase Assay: |
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Cell Assay: |
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Data from [Data independently produced by Cell Death Differ, 2014, 21(10), 1535-45]
Data from [Data independently produced by Acta Pharmacol Sin, 2013, 34(9),1201-7]
, , Dr. Zhang of Tianjin Medical University
Data from [Data independently produced by , , J Immunol, 2014, 192(5): 2063-70 ]
Complement factor H is an ICOS ligand modulating Tregs in the glioma microenvironment [ Cancer Immunol Res, 2024, 10.1158/2326-6066.CIR-23-1092] | PubMed: 39378431 |
The highly selective and oral phosphoinositide 3-kinase delta (PI3K-δ) inhibitor roginolisib induces apoptosis in mesothelioma cells and increases immune effector cell composition [ Transl Oncol, 2024, 43:101857] | PubMed: 38412661 |
JAK3/STAT5 signaling-triggered upregulation of PIK3CD contributes to gastric carcinoma development [ J Cell Commun Signal, 2024, 18(1):e12017] | PubMed: 38545256 |
Evolutionary states and trajectories characterized by distinct pathways stratify patients with ovarian high grade serous carcinoma [ Cancer Cell, 2023, 41(6):1103-1117.e12] | PubMed: 37207655 |
PD-1 instructs a tumor-suppressive metabolic program that restricts glycolysis and restrains AP-1 activity in T cell lymphoma [ Nat Cancer, 2023, 4(10):1508-1525] | PubMed: 37723306 |
Alcam-a and Pdgfr-α are essential for the development of sclerotome-derived stromal cells that support hematopoiesis [ Nat Commun, 2023, 14(1):1171] | PubMed: 36859431 |
Dasatinib overcomes glucocorticoid resistance in B-cell acute lymphoblastic leukemia [ Nat Commun, 2023, 14(1):2935] | PubMed: 37217509 |
Integrated single-cell (phospho-)protein and RNA detection uncovers phenotypic characteristics and active signal transduction of human antibody secreting cells [ Mol Cell Proteomics, 2023, S1535-9476(23)00001-4] | PubMed: 36623694 |
Intrinsic cancer cell phosphoinositide 3-kinase δ regulates fibrosis and vascular development in cholangiocarcinoma [ Liver Int, 2023, 10.1111/liv.15751] | PubMed: 37804055 |
Activation of glucagon-like peptide-1 receptor in microglia exerts protective effects against sepsis-induced encephalopathy via attenuating endoplasmic reticulum stress-associated inflammation and apoptosis in a mouse model of sepsis [ Exp Neurol, 2023, 363:114348] | PubMed: 36813224 |
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