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Idelalisib (CAL-101)
別名：GS-1101
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.
CAS No. 870281-82-6
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Idelalisib (CAL-101)関連製品
シグナル伝達経路
PI3K阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| SR786 | Growth Inhibition Assay | 10 μM | 72 h | does not induce apoptosis | 22801959 |
| Myla | Growth Inhibition Assay | 10 μM | 72 h | does not induce apoptosis | 22801959 |
| HH | Growth Inhibition Assay | 10 μM | 72 h | Induction of apoptosis slightly | 22801959 |
| SP53 | Growth Inhibition Assay | 0.1 μM | 72 h | does not induce cell cycle arrest or apoptosis | 23676220 |
| MINO | Growth Inhibition Assay | 5 μM | 72 h | does not induce cell cycle arrest or apoptosis | 23676220 |
| MAVER-1 | Growth Inhibition Assay | 5 μM | 72 h | does not induce cell cycle arrest or apoptosis | 23676220 |
| JEKO-1 | Growth Inhibition Assay | 5 μM | 72 h | does not induce cell cycle arrest or apoptosis | 23676220 |
| JEKO-1 | Growth Inhibition Assay | 10 μM | 72 h | Inhibition of proliferation slightly | 23341541 |
| Granta-519 | Function Assay | 1 μM | 2 h | Inhibition of Akt(s473) phosphorylation | 23341541 |
| Granta-519 | Function Assay | 1 μM | 2 h | Inhibition of Akt(t308) phosphorylation | 23341541 |
| JEKO-1 | Function Assay | 1 μM | 72 h | Inhibition of Akt phosphorylation in IgM-stimulated JEKO-1 | 23341541 |
| Primary CLL cell | Function Assay | 1 μM | 15 min | Blocks BCR-induced LCP1 serine-5 activation | 24009233 |
| Microglia | Function Assay | 5 μM | 10 h | Decrease of TNFa secretion from LPS-stimulated p110δD910A/D910A microglia | 24625684 |
| Primary AML cell | Growth Inhibition Assay | 1 μM | 3 h | Suppression of rRNA synthesis | 25014775 |
| Primary AML cell | Function Assay | 1 μM | 3 h | Inhibition of GSK3 phosphorylation | 25014775 |
| Primary AML cell | Function Assay | 1 μM | 3 h | Inhibition of P70S6K phosphorylation | 25014775 |
| Primary AML cell | Function Assay | 1 μM | 3 h | Inhibition of Akt phosphorylation | 25014775 |
| K562 | Growth Inhibition Assay | 1 μM | 72 h | Inhibition of proliferation | 25014775 |
| K562 | Function Assay | 1 μM | 3 h | Inhibition of GSK3 phosphorylation | 25014775 |
| K562 | Function Assay | 1 μM | 3 h | Inhibition of P70S6K phosphorylation | 25014775 |
| K562 | Function Assay | 1 μM | 3 h | Inhibition of Akt phosphorylation | 25014775 |
| U266 | Growth Inhibition Assay | 40 μM | 48 h | 79.5% inhibition rate | 25339332 |
| HuT78 | Growth Inhibition Assay | 10 μM | 72 h | does not induce apoptosis | 22801959 |
| MJ | Growth Inhibition Assay | 10 μM | 72 h | does not induce apoptosis | 22801959 |
| DERL7 | Growth Inhibition Assay | 10 μM | 72 h | does not induce apoptosis | 22801959 |
| L1236 | Function Assay | 10 μM | 2 h | Inhibition of Akt phosphorylation | 22210877 |
| L428 | Function Assay | 10 μM | 2 h | Inhibition of Akt phosphorylation | 22210877 |
| L591 | Function Assay | 10 μM | 2 h | Inhibition of Akt phosphorylation | 22210877 |
| KMH-2 | Function Assay | 10 μM | 2 h | Inhibition of Akt phosphorylation | 22210877 |
| L1236 | Function Assay | 5 μM | 24 h | Blocks secretion of the CCL5 | 22210877 |
| L591 | Function Assay | 5 μM | 24 h | Blocks secretion of the CCL5 | 22210877 |
| L1236 | Apoptosis Assay | 5 μM | 24 h | Induction of apoptosis | 22210877 |
| L591 | Apoptosis Assay | 5 μM | 24 h | Induction of apoptosis | 22210877 |
| U-87MG | Function Assay | 100 nM | 24 h | Inhibition of cell migration | 22079609 |
| SW1783 | Function Assay | 100 nM | 24 h | Inhibition of cell migration | 22079609 |
| U-87MG | Function Assay | 5 μM | 24 h | Inhibition of Akt phosphorylation substantially | 22079609 |
| SW1783 | Function Assay | 5 μM | 24 h | Inhibition of Akt phosphorylation substantially | 22079609 |
| U-373MG | Function Assay | 5 μM | 24 h | Inhibition of Akt phosphorylation substantially | 22079609 |
| SK-MG3 | Function Assay | 5 μM | 24 h | Inhibition of Akt phosphorylation substantially | 22079609 |
| SU-DHL-5 | Function Assay | 1 μM | 24 h | Induction of apoptosis | 20959606 |
| WSU-NHL | Function Assay | 1 μM | 24 h | Induction of apoptosis | 20959606 |
| CCRF-SB | Function Assay | 1 μM | 24 h | Induction of apoptosis | 20959606 |
| INA-6 | Function Assay | 5 μM | 6 h | Inhibition of PI3K/Akt and ERK pathway | 20505158 |
| LB | Function Assay | 5 μM | 6 h | Inhibition of PI4K/Akt and ERK pathway | 20505158 |
| MOLM14 | Antitumor assay | 100 mg/kg | 14 days | Antitumor activity against human MOLM14 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 100 mg/kg, po administered daily via gavage dosed for 14 days and measured daily during compound dosing relative to control | 30053721 |
| MOLM14 | Antitumor assay | 100 mg/kg | 14 days | Antitumor activity against human MOLM14 cells xenografted in nu/nu mouse assessed as induction of apoptosis at 100 mg/kg, po administered daily via gavage dosed for 14 days and measured daily during compound dosing by TUNEL based assay | 30053721 |
| MOLM14 | Antitumor assay | 100 mg/kg | 14 days | Antitumor activity against human MOLM14 cells xenografted in nu/nu mouse assessed as inhibition of tumor proliferation 100 mg/kg, po administered daily via gavage dosed for 14 days and measured daily during compound dosing by Ki-67 labelling based immunoh | 30053721 |
| MOLM14 | Antiproliferative assay | 3 days | Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay, IC50 = 3.6 μM. | 27774127 | |
| MV4-11 | Antiproliferative assay | 3 days | Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay, IC50 = 6.3 μM. | 27774127 | |
| Jurkat | Antiproliferative assay | 3 days | Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay, IC50 = 7.9 μM. | 27774127 | |
| Loucy | Antiproliferative assay | 3 days | Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay, IC50 = 8.4 μM. | 27774127 | |
| MOLT4 | Antiproliferative assay | 3 days | Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay, IC50 = 10.6 μM. | 27774127 | |
| SUDHL6 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by alamar blue assay, IC50 = 0.1176 μM. | 27846451 | |
| SU-DHL4 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SU-DHL4 cells measured after 72 hrs by alamar blue assay, IC50 = 1.6 μM. | 27846451 | |
| Pfeiffer | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Pfeiffer cells measured after 72 hrs by alamar blue assay, IC50 = 6.8 μM. | 27846451 | |
| KARPAS422 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human KARPAS422 cells measured after 72 hrs by alamar blue assay, IC50 = 8.1 μM. | 27846451 | |
| Sf21 | Function assay | 30 mins | Inhibition of N-terminal His6-tagged recombinant full-length human PI3K p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2/ATP as substrate after 30 mins by TR-FRET assay, IC50 = 3.7 μM. | 28106991 | |
| Sf21 | Function assay | 30 mins | Inhibition of N-terminal His6-tagged recombinant full-length human PI3K p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2/ATP as substrate after 30 mins by TR-FRET assay, IC50 = 3.7 μM. | 28106991 | |
| RPMI8266 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RPMI8266 cells after 72 hrs by MTT assay, IC50 = 0.00549 μM. | 28325601 | |
| Raji | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Raji cells after 72 hrs by MTT assay, IC50 = 0.00995 μM. | 28325601 | |
| SUDHL6 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SUDHL6 cells after 72 hrs by CCK8 assay, IC50 = 0.65 μM. | 29534936 | |
| RPMI8226 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay, IC50 = 5.49 μM. | 29534936 | |
| Raji | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Raji cells after 72 hrs by MTT assay, IC50 = 9.95 μM. | 29534936 | |
| MOLM13 | Growth inhibition assay | 72 hrs | Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay, GI50 = 1.7 μM. | 30053721 | |
| MOLM14 | Growth inhibition assay | 72 hrs | Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay, GI50 = 6.4 μM. | 30053721 | |
| CLL PBMCs | Growth Inhibition Assay | IC50=2.9 nM | 25917267 | ||
| MEC1 | Growth Inhibition Assay | IC50=20.4 μM | 25999352 | ||
| B-cells | Function assay | Inhibition of PI3Kdelta in B-cells by proliferation assay, IC50 = 0.0061 μM. | 22924688 | ||
| insect cells | Function assay | Inhibition of recombinant human full length His-tagged PI3Kgamma expressed in insect cells, IC50 = 0.089 μM. | 27846451 | ||
| insect cells | Function assay | Inhibition of recombinant human full length His-tagged PI3Kbeta expressed in insect cells, IC50 = 0.565 μM. | 27846451 | ||
| KARPAS422 | Growth inhibition assay | Growth inhibition of human KARPAS422 cells by CCK8 assay, GI50 = 0.68 μM. | 28835805 | ||
| Pfeiffer | Growth inhibition assay | Growth inhibition of human Pfeiffer cells by CCK8 assay, GI50 = 0.74 μM. | 28835805 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| SU-DHL6 | Growth inhibition assay | Growth inhibition of human SU-DHL6 cells by CellTiter-Glo assay, GI50 = 0.042 μM. | 29601991 | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | 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. | ||||
|---|---|---|---|---|---|
| Targets |
|
| In Vitro | ||||
| 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] |
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|---|---|---|---|---|
| Kinase Assay | 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. | ||||
| 細胞実験 | 細胞株 | CLL B cells or healthy volunteer T cells or NK cells | ||
| 濃度 | 0.01-100 μM | |||
| 反応時間 | 48 hours | |||
| 実験の流れ | 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 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. |
|||
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | PUMA / p53 Bim / Bcl-xl / Bid / Mcl-1 p-p65 p-AKT / AKT Cleaved caspase 3 / Cleaved caspase 9 Mcl-1 / Bcl-2 / Bid / Bcl-xl / Noxa / Bak / Bax p-FoxO3a / FoxO3a Akt(T308) / PDK1(S241) / GSK-3β(S9) |
|
28008149 | |
| Growth inhibition assay | Cell viability Cell viability |
|
28008149 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03582098 | Completed | Chronic Lymphocytic Leukaemia |
Gilead Sciences |
September 12 2018 | -- |
| NCT03151057 | Terminated | B Cells-Tumors|B Cell Chronic Lymphocytic Leukemia|Follicular Lymphoma|Mantle Cell Lymphoma|Large B-Cell Diffuse Lymphoma of Bone (Diagnosis) |
Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Gilead Sciences |
July 31 2018 | Phase 1 |
| NCT03568929 | Completed | Follicular Non-Hodgkin''s Lymphoma Refractory |
Gilead Sciences |
May 25 2018 | -- |
化学情報
| 分子量 | 415.42 | 化学式 | C22H18FN7O |
| CAS No. | 870281-82-6 | SDF | Download Idelalisib (CAL-101) SDFをダウンロードする |
| Smiles | CCC(C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5 | ||
| 保管 | |||
|
In vitro |
DMSO : 83 mg/mL ( (199.79 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble Ethanol : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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* 必須
よくある質問（FAQ）
質問1:
What is the recommended dose of CAL-101 and the route of administration for mouse studies?
回答
According to the following paper, S2226 can be used by I.V. administration at the concentration of 40 mg/kg. https://www.ncbi.nlm.nih.gov/pubmed/24625684
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