CAL-101 (Idelalisib, GS-1101)

CAL-101 (Idelalisib, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110δ thanp110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.

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CAL-101 (Idelalisib, GS-1101) Chemical Structure

CAL-101 (Idelalisib, GS-1101) Chemical Structure
Molecular Weight: 415.42

Validation & Quality Control

Customer Reviews(1)

Quality Control & MSDS

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CAL-101 (Idelalisib, GS-1101) is available in the following compound libraries:

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Product Information

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Product Description

Biological Activity

Description CAL-101 (Idelalisib, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110δ thanp110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.
Targets p110δ [1] p110γ [1] p110β [1] p110α [1] hVps34 [1]

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IC50 2.5 nM 89 nM 565 nM 820 nM 978 nM
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]
In vivo
Features

Protocol(Only for Reference)

Kinase Assay: [2]

PI3K assay PI3K assay is preformed on whole-cell lysates from CLL or normal B cells. A PI3K ELISA assay is performed. Briefly, whole-cell extracts are added to a mixture of PI(4,5)P2 substrate and reaction buffer containing adenosine triphosphate (ATP) and allowed to incubate at room temperature. The reaction is stopped by adding PI(3,4,5)P3 detector mixed with EDTA (ethylenediaminetetraacetic acid) and allowed to incubate at room temperature for 1 hour. After this time, the mixture is transferred from each well to a PI3K ELISA plate and allowed to incubate 1 hour. Plates are washed and then incubated with secondary detector for 30 minutes. Plates are washed again, and 3,3′,5,5′-tetramethylbenzidine solution is added for 5 minutes at which time H2SO4 is added to stop all reactions. Plates are read at 450 nm on a Labsystems 96-well plate reader.

Cell Assay: [2]

Cell lines CLL B cells or healthy volunteer T cells or NK cells
Concentrations 0.01-100 μM
Incubation Time 48 hours
Method MTT assays are performed to determine cytotoxicity. 1 × 105 cells are incubated with CAL-101. 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. At least 104 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Lannutti BJ, et al. Blood, 2011, 117(2), 591-594.

[2] Herman SE, et al. Blood, 2010, 116(12), 2078-2088.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-09-13)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01980875 Not yet recruiting Chronic Lymphocytic Leukemia Gilead Sciences January 2015 Phase 3
NCT02044822 Recruiting B-cell Chronic Lymphocytic Leukemia (CLL) With 17p Deletion Gilead Sciences July 2014 Phase 2
NCT02135133 Recruiting Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma Dana-Farber Cancer Institute|Gilead Sciences|GlaxoSmithKline June 2014 Phase 2
NCT01980888 Recruiting Chronic Lymphocytic Leukemia Gilead Sciences February 2014 Phase 3
NCT01838434 Recruiting Relapsed/Refractory Mantle Cell Lymphoma Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI)|Celgene Corporation|Gilead Sciences|Biologics, Inc. July 2013 Phase 1|Phase 2

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Chemical Information

Download CAL-101 (Idelalisib, GS-1101) SDF
Molecular Weight (MW) 415.42
Formula

C22H18FN7O

CAS No. 870281-82-6
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 83 mg/mL (199 mM)
Water <1 mg/mL (<1 mM)
Ethanol 35 mg/mL (84 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
* <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.
Chemical Name (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one

Research Area

Customer Reviews (1)


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Rating
Source Dr. Zhang of Tianjin Medical University. CAL-101 (Idelalisib, GS-1101) purchased from Selleck
Method Western blot
Cell Lines A549 cells
Concentrations 0-1 μM
Incubation Time 3 h
Results Reduction of AKT phosphorylation in A549 cells treated with CAL-101 was observed.

Product Citations (17)

Tech Support & FAQs

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