1. PI3K/Akt/mTOR
    Autophagy
  2. PI3K
    Autophagy
  3. Idelalisib

Idelalisib (Synonyms: CAL-101; GS-1101)

Cat. No.: HY-13026 Purity: 99.98%
Handling Instructions

Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.

For research use only. We do not sell to patients.

Idelalisib Chemical Structure

Idelalisib Chemical Structure

CAS No. : 870281-82-6

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Customer Review

Based on 21 publication(s) in Google Scholar

Other Forms of Idelalisib:

Top Publications Citing Use of Products

    Idelalisib purchased from MCE. Usage Cited in: Br J Haematol. 2015 Jul;170(1):134-8.

    Treatment of CXCR4WT and CXCR4S338X BCWM.1 and MWCL-1 cells with PCI-32765 or Idelalisib induced caspase-3 and PARP cleavage at 6 h. Caspase-3 and PAPR cleavage following PCI-32765 (IB), Idelalisib (ID), ABT-199 (ABT), in the presence of absence of CXCL12 (SDF) and AMD3100 (AMD).

    Idelalisib purchased from MCE. Usage Cited in: Oncotarget. 2016 May 31;7(22):32641-51.

    The well-established PI3Kδ specific inhibitor, CAL-101, shows similar effects as PI3KD-IN-015 with an EC50 of 2.3 nM against PI3Kδ and over 1000-fold less potent against the other three isoforms. Determination of CAL-101 inhibitory activities against PI3Kα, β, δ and γ in cellular background.

    Idelalisib purchased from MCE. Usage Cited in: Oncotarget. 2016 Aug 16;7(33):53515-53525.

    PI3KD/V-IN-01 affects autophagy HeLa cells are treated with different concentrations of PI3KD/V-IN-01, VPS34-IN-1, GDC-0941 or CAL-101 for 16 hours before they are fixed and stained for the autophagy marker LC3B.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.

    IC50 & Target[1]

    p110δ

    2.5 nM (IC50)

    p110γ

    89 nM (IC50)

    p110β

    565 nM (IC50)

    p110α

    820 nM (IC50)

    hVps34

    978 nM (IC50)

    DNA-PK

    6729 nM (IC50)

    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[1]. 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[2].

    In Vivo

    A significant reduction is observed in the CD11b+Ly6G+ neutrophils from brain homogenates of bothp110δD910A/D910A mice and Idelalisib (CAL-101) (40 mg/kg, i.v.) post-treated mice[3].

    Clinical Trial
    Molecular Weight

    415.42

    Formula

    C₂₂H₁₈FN₇O

    CAS No.

    870281-82-6

    SMILES

    O=C1N(C2=CC=CC=C2)C([[email protected]@H](NC3=C4N=CNC4=NC=N3)CC)=NC5=C1C(F)=CC=C5

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 59.7 mg/mL (143.71 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4072 mL 12.0360 mL 24.0720 mL
    5 mM 0.4814 mL 2.4072 mL 4.8144 mL
    10 mM 0.2407 mL 1.2036 mL 2.4072 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [2]

    MTT assays are performed to determine cytotoxicity. Briefly, 1×105 cells (CLL B cells or healthy volunteer T cells or NK cells) are incubated for 48 hours with different concentrations of Idelalisib (CAL-101) (0.1 μM, 1 μM, 5 μM, 10 μM), 25 μM LY294002, or vehicle control. MTT reagent is then added. DMSO is added, and absorbance is measured by spectrophotometry at 540 nm in a Labsystems plate reader. Cell viability is also measured at various time points with the use of annexin/PI flow cytometry. Data are analyzed with Expo-ADC32 software package. At least 10,000 cells are counted for each sample. Results are expressed as the percentage of total positive cells over untreated control. Experiments examining caspase-dependent apoptosis included the addition of 100 μM Z-VAD. Experiments examining survival signals include the addition of 1 μg/mL CD40L, 800 U/mL IL-4, 50 ng/mL BAFF, 20 ng/mL TNF-α, or coculturing on fibronectin or stromal (HS-5 cell line) coated plates. Stromal coculture is done by plating a 75-cm2 flask (80%-100% confluent) per 6-well plate 24 hours before the addition of CLL cells[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Mice[3]
    For Idelalisib (CAL-101) treatment, wild-type C57BL/6 mice are administered either 40 mg/kg Idelalisib (CAL-101) or vehicle DMSO, by 25 μL infusion into the femoral vein, 15 min before I/R (pre-treatment), or 3 and 6 h after initiation of reperfusion (post-treatment). Controls and animals treated with Idelalisib (CAL-101) underwent cerebral blood flow (CBF) measurements using a laser Doppler perfusion monitor. The CBF measurements obtained immediately before and after MCAO and again at 3 h after reperfusion showed an ~90-95% reduction in the blood flow to the MCAO infarct region, which does not differ between groups.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.98%

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    Keywords:

    IdelalisibCAL-101 GS-1101CAL101CAL 101GS1101GS 1101GS-1101PI3KAutophagyPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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