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

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

Cat. No.: HY-13026 Purity: 98.38%
Data Sheet SDS Handling Instructions

CAL-101 is a highly selective and potent p110δ inhibitor with IC50 of 2.5 nM, is 40- to 300-fold more selective for p110δ relative to other PI3K class I enzymes (p110α, p110β, and p110γ; IC50 are 820, 565, and 89nM, respectively).

For research use only. We do not sell to patients.
CAL-101 Chemical Structure

CAL-101 Chemical Structure

CAS No. : 870281-82-6

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    CAL-101 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 Ibrutinib or Idelalisib induced caspase-3 and PARP cleavage at 6 h. Caspase-3 and PAPR cleavage following Ibrutinib (IB), Idelalisib (ID), ABT-199 (ABT), in the presence of absence of CXCL12 (SDF) and AMD3100 (AMD).

    CAL-101 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.

    CAL-101 purchased from MCE. Usage Cited in: Patent. US 20160222465 A1.

    Impact of Ibrutinib on p-AKT, ERK and BTK expression following SDF-1a stimulation of plenti-GFP vector, CXCR4WT and CXCR4S338X expressing BCWM.1 cells. plenti-GFP vector, CXCR4WT and CXCR4S338X expressing BCWM.1 cells are pretreated for 2 hours with either Ibrutinib (0.5 uM) or AMD3100 (30 uM) prior to stimulation with SDF-1a (20 nM) for 2 minutes. Results depict differences in phospho-AKT, phospho-ERK, and phospho-BTK obtained by immunoblotting follow

    CAL-101 purchased from MCE. Usage Cited in: Patent. US 20160222465 A1.

    CXCR4S338X expressing BCWM.1 and MWCL-1 cells show variable resistance to PARP and caspase 3 cleavage mediated by WM relevant therapeutics in the presence of SDF-1a, and reversed by AMD3100. plenti-GFP vector, CXCR4WT and CXCR4S338X expressing WM cells are treated for 6 hours with Bendamustine (BENDA), Fludarabine (FLUDARA), Bortezomib (BORT), and Idelalisib (IDELA) at their EC50 doses in the presence or absence of SDF-1a (20 nM) and/or the CXCR4 recep

    CAL-101 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

    • Technical Information

    • Purity & Documentation

    • References

    Description

    CAL-101 is a highly selective and potent p110δ inhibitor with IC50 of 2.5 nM, is 40- to 300-fold more selective for p110δ relative to other PI3K class I enzymes (p110α, p110β, and p110γ; IC50 are 820, 565, and 89nM, respectively).

    IC50 & Target

    IC50: 2.5 nM (p110δ), 89 nM (p110γ), 565 nM (p110β), 820 nM (p110α)[1]

    In Vitro

    CAL-101 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. CAL-101 inhibits LPA-induced pAkt with an EC50 of 1.9 μM. 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-101-induced apoptosis of chronic lymphocytic leukemia (CLL) cells is significant compare with vehicle treatment alone (P<0.001). 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 CAL-101 (40 mg/kg, i.v.) post-treated mice[3].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT00836914 Gilead Sciences Allergic Rhinitis February 2009 Phase 1
    NCT00710528 Gilead Sciences Chronic Lymphocytic Leukemia (CLL)|Lymphoma, Non-Hodgkin (NHL)|Acute Myeloid Leukemia (AML)|Multiple Myeloma (MM) June 2008 Phase 1
    NCT02445131 German CLL Study Group Chronic Lymphocytic Leucemia May 2015 Phase 2
    NCT00836914 Gilead Sciences Allergic Rhinitis February 2009 Phase 1
    NCT00710528 Gilead Sciences Chronic Lymphocytic Leukemia (CLL)|Lymphoma, Non-Hodgkin (NHL)|Acute Myeloid Leukemia (AML)|Multiple Myeloma (MM) June 2008 Phase 1
    NCT02445131 German CLL Study Group Chronic Lymphocytic Leucemia May 2015 Phase 2
    NCT02439138 Dana-Farber Cancer Institute|Gilead Sciences Waldenstrom's Macroglobulinemia October 2015 Phase 2
    NCT01659047 Gilead Sciences Chronic Lymphocytic Leukemia August 2012 Phase 2
    NCT02739360 Gilead Sciences Lymphoid Malignancies May 2016 Phase 4
    NCT02536300 Gilead Sciences Follicular Lymphoma January 14, 2016 Phase 3
    NCT02242045 Gilead Sciences Chronic Lymphocytic Leukemia|Indolent Non-Hodgkin Lymphoma|Follicular Lymphoma|Small Lymphocytic Lymphoma|Lymphoplasmacytic Lymphoma (With or Without Waldenstrom Macroglobulinemia)|Marginal Zone Lymphoma October 1, 2014 Phase 1
    NCT01090414 Gilead Sciences Chronic Lymphocytic Leukemia|Lymphoma, Non-Hodgkin March 22, 2010 Phase 1
    NCT01282424 Gilead Sciences Follicular Lymphoma|Small Lymphocytic Lymphoma|Lymphoplasmacytic Lymphoma|Marginal Zone Lymphoma March 4, 2011 Phase 2
    NCT01393106 Gilead Sciences Hodgkin Lymphoma September 2011 Phase 2
    NCT02590588 John Mark Sloan|Gilead Sciences|Boston Medical Center Amyloidosis January 2016 Phase 2
    NCT01539291 Gilead Sciences Chronic Lymphocytic Leukemia October 2012 Phase 3
    NCT02135133 Dana-Farber Cancer Institute|Gilead Sciences|GlaxoSmithKline Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma June 2014 Phase 2
    NCT01306643 Gilead Sciences Indolent Non-Hodgkin's Lymphoma|Follicular Lymphoma|Small Lymphocytic Lymphoma|Marginal Zone Lymphoma February 2011 Phase 1|Phase 2
    NCT02436135 Gilead Sciences Myelofibrosis June 5, 2015 Phase 1
    NCT01203930 Gilead Sciences Chronic Lymphocytic Leukemia (CLL)|Small Lymphocytic Lymphoma (SLL) October 2010 Phase 2
    NCT02468557 Gilead Sciences Pancreatic Ductal Adenocarcinoma July 2015 Phase 1
    NCT01659021 Gilead Sciences Chronic Lymphocytic Leukemia December 4, 2012 Phase 3
    NCT02258529 Gilead Sciences Follicular Lymphoma|Small Lymphocytic Lymphoma September 14, 2015 Phase 2
    NCT01796470 Gilead Sciences Chronic Lymphocytic Leukemia|Mantle Cell Lymphoma|Diffuse Large B-cell Lymphoma|Indolent Non-Hodgkin's Lymphoma June 2013 Phase 2
    NCT01539512 Gilead Sciences Chronic Lymphocytic Leukemia April 2012 Phase 3
    NCT03151057 Sidney Kimmel Comprehensive Cancer Center B Cells--Tumors|B Cell Chronic Lymphocytic Leukemia|Follicular Lymphoma|Mantle Cell Lymphoma|Large B-cell Diffuse Lymphoma April 20, 2017 Phase 1
    NCT02044822 Gilead Sciences B-cell Chronic Lymphocytic Leukemia (CLL) With 17p Deletion August 6, 2014 Phase 2
    NCT02662296 Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) Prolymphocytic Leukemia|Recurrent Chronic Lymphocytic Leukemia|Recurrent Non-Hodgkin Lymphoma|Recurrent Small Lymphocytic Lymphoma March 2016 Phase 2
    NCT01980888 Gilead Sciences Chronic Lymphocytic Leukemia February 2014 Phase 3
    NCT02928510 Jonsson Comprehensive Cancer Center|Gilead Sciences|National Cancer Institute (NCI) Absence of Signs or Symptoms|B-Cell Non-Hodgkin Lymphoma|Digestive System Signs and Symptoms|Indolent Adult Non-Hodgkin Lymphoma|Recurrent B-Cell Non-Hodgkin Lymphoma|Recurrent Chronic Lymphocytic Leukemia|Recurrent Indolent Adult Non-Hodgkin Lymphoma|Recurrent Small Lymphocytic Lymphoma January 2017
    NCT02538614 Gilead Sciences|Boehringer Ingelheim Chronic Lymphocytic Leukemia (CLL) December 29, 2015 Phase 1
    NCT02962401 French Innovative Leukemia Organisation Waldenstrom Macroglobulinemia March 7, 2017 Phase 2
    NCT01838434 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI)|Celgene Corporation|Gilead Sciences|Biologics, Inc. Relapsed/Refractory Mantle Cell Lymphoma July 2013 Phase 1|Phase 2
    NCT01569295 Gilead Sciences Chronic Lymphocytic Leukemia June 26, 2012 Phase 3
    NCT01732913 Gilead Sciences Indolent Non-Hodgkin's Lymphomas January 16, 2013 Phase 3
    NCT03126019 Incyte Corporation Follicular Lymphoma June 29, 2017 Phase 2
    NCT01644799 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI)|Gilead Sciences|Celgene Corporation Recurrent Follicular Lymphoma July 2013 Phase 1
    NCT01980875 Gilead Sciences Chronic Lymphocytic Leukemia April 21, 2015 Phase 3
    NCT02968563 Gilead Sciences|German CLL Study Group Chronic Lymphocytic Leukemia December 13, 2016 Phase 2
    NCT02136511 Gilead Sciences Chronic Lymphocytic Leukemia (CLL)
    NCT02639910 MorphoSys AG Leukemia, Lymphocytic, Chronic, B-Cell|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma November 2016 Phase 2
    NCT01732926 Gilead Sciences Indolent Non-Hodgkin's Lymphomas January 2, 2013 Phase 3
    NCT01088048 Gilead Sciences Indolent Non-Hodgkin's Lymphoma|Chronic Lymphocytic Leukemia|Mantle Cell Lymphoma April 2010 Phase 1
    NCT02603445 Novartis Pharmaceuticals|Novartis Follicular Lymphoma, Mantle Cell Lymphoma November 17, 2015 Phase 1
    NCT02970318 Acerta Pharma BV Chronic Lymphocytic Leukemia September 2016 Phase 3
    NCT02332980 Mayo Clinic|National Cancer Institute (NCI) Recurrent Chronic Lymphocytic Leukemia|Recurrent Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Lymphoplasmacytic Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Nodal Marginal Zone Lymphoma|Recurrent Small Lymphocytic Lymphoma|Recurrent Splenic Marginal Zone Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Extranodal Marginal Zone Lym February 19, 2015 Phase 2
    NCT01644253 Aptevo Therapeutics Chronic Lymphocytic Leukemia September 2012 Phase 1
    NCT02787369 Dana-Farber Cancer Institute|Acetylon Pharmaceuticals Incorporated Recurrent Chronic Lymphoid Leukemia May 2016 Phase 1
    NCT02457598 Gilead Sciences B-cell Malignancies June 16, 2015 Phase 1
    View MoreCollapse
    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) 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
    Cell Assay
    [2]

    CAL-101 is dissolved in DMSO and stored, and then diluted with appropriate media before use[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 CAL-101 (0.1 μM, 1 μM, 5 μM, 10 μM), 25 μM LY294002, or vehicle control. MTT reagent is then added, and plates are incubated for an additional 20 hours before washing with protamine sulfate in phosphate-buffered saline. 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]

    CAL-101 is prepared in DMSO and then diluted[3].

    Mice[3]
    For CAL-101 treatment, wild-type C57BL/6 mice are administered either 40 mg/kg 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 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
    Molecular Weight

    415.42

    Formula

    C₂₂H₁₈FN₇O

    CAS No.

    870281-82-6

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 59.7 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 98.38%

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    CAL-101
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