Idelalisib (CAL-101, GS-1101)

Catalog No.S2226

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

Molecular Weight(MW): 415.42

Idelalisib (CAL-101, GS-1101) 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.

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Cited by 31 Publications

5 Customer Reviews

  • Invasive migration of RA FLS was analyzed through growth factor–reduced Matrigel-coated transwell inserts in the presence or absence of 1 µM INK007, 5 µM CAL-101, or 0.3 µM IPI-145, or 0.3 µM GDC-0941 inhibitors or DMSO. Cells were allowed to invade through Matrigel toward PDGF-BB (25 ng/ml) containing media for 24 h and were fixed and stained with Hemacolor staining kit.

    J Immunol, 2014, 192(5): 2063-70 . Idelalisib (CAL-101, GS-1101) purchased from Selleck.

    Ppp2r1afl/fl BCR-ABL1 B-ALL cells transduced with 4-OHT-inducible Cre-ERT2 (Cre) or ERT2-vector (EV) were treated with 4-OHT for 3 days and cell lysates were studied by phospho-protein array analysis. Ppp2r1afl/fl BCR-ABL1 ALL cells were transduced with 4-OHT-inducible Cre or EV control and incubated in the presence of the small molecule signaling inhibitor idelalisib (32 μmol/L; C). Percentages of GFP+ cells were measured by flow cytometry at the times indicated following 4-OHT-treatment. Data are shown as mean ± standard deviation (SD) and representative of at least three independent experiments.

    Cell, 2018, 173(2):470-484. Idelalisib (CAL-101, GS-1101) purchased from Selleck.

  • 293T cells were transfected with HA-tagged Fbxo45. At 48 h after transfection, cells were treated with AKT inhibitor (CAL-101; 10 uM, 4 h), cell extracts from the cytoplasm or nuclei were subjected to IP with anti-HA resin followed by western blot analysis with indicated antibodies.

    Cell Death Differ 2014 21(10), 1535-45. Idelalisib (CAL-101, GS-1101) purchased from Selleck.

    Isoform-selective PI3K inhibitors blocked PI3K signaling in corresponding Rh30-Myr-p110 cells. Rh30-Myr-p110s cells were cultured in serum-free medium for 12 h, and then exposed to CAL-101 at indicated concentrations for additional 1 h. The cells were collected to detect the level of phosphorylated and total Akt. β-Actin was served as loading control.

    Acta Pharmacol Sin 2013 34(9),1201-7. Idelalisib (CAL-101, GS-1101) purchased from Selleck.

  • After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of CAL-101 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.

    Dr. Zhang of Tianjin Medical University. Idelalisib (CAL-101, GS-1101) purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Idelalisib (CAL-101, GS-1101) 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.
Targets
p110δ [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
2.5 nM 89 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MEC1 NF;vO2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\EUXNQ M3\je2lEPTB;MkCuOEDPxE1? M2r0WlI2QTl7M{Wy
CLL PBMCs MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjEUXNQ MULJR|UxRTJwOTDuUS=> M1zsVVI2QTF5Mk[3
U266 NXroPHF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWm0NEDPxE1? NGHuW5o1QCCq NH;Bd2c4QS53JTDpcohq[mm2aX;uJJJifGV? M2TCdFI2OzN7M{Oy
K562 MV3GeY5kfGmxbjDBd5NigQ>? MX[xJO69VQ>? NYXoOXJwOyCq MVXJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NUPyeIhEOjVyMUS3O|U>
K562 NWTZSYRRTnWwY4Tpc44hSXO|YYm= MnvXNUDPxE1? MXuzJIg> NXjCVVVOUW6qaXLpeIlwdiCxZjDQO|BUPkticHjvd5Bpd3K7bHH0bY9v MXSyOVAyPDd5NR?=
K562 M4f0Z2Z2dmO2aX;uJGF{e2G7 NYr0fVVsOSEQvF2= M2nyRVMhcA>? NXjsbYIzUW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=> NG\yXVIzPTBzNEe3OS=>
K562 NHXKTIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonaNUDPxE1? M3fPbVczKGh? Mny0TY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;u NF;iU4gzPTBzNEe3OS=>
Primary AML cell MkWxSpVv[3Srb36gRZN{[Xl? MUWxJO69VQ>? MXqzJIg> MofyTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w MUmyOVAyPDd5NR?=
Primary AML cell NGjHdmdHfW6ldHnvckBCe3OjeR?= MkiwNUDPxE1? NXrh[HQyOyCq MonsTY5pcWKrdHnvckBw\iCSN{DTOmsheGixc4Doc5J6dGG2aX;u NHrxPJIzPTBzNEe3OS=>
Primary AML cell M1;BVWZ2dmO2aX;uJGF{e2G7 NGf2Rm4yKM7:TR?= MXezJIg> NYrqRYJHUW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=> M1rDe|I2ODF2N{e1
Primary AML cell MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\VTVEh|ryP Ml7uN{Bp NIfzN2ZUfXCycnXzd4lwdiCxZjDyVm5CKHO7boTo[ZNqew>? MV2yOVAyPDd5NR?=
Microglia NIqyU|hHfW6ldHnvckBCe3OjeR?= MYW1JO69VQ>? MWexNEBp NWXVT4UyTE2VTx?= NXrI[otSTGWlcnXhd4Uhd2ZiVF7GZUB{\WO{ZYTpc44h\nKxbTDMVHMue3SrbYXsZZRm\CBicEGxNO61TDlzMFGvSFkyOEFibXnjdo9odGmj M3TQSlI1PjJ3Nki0
Primary CLL cell M{HlSmZ2dmO2aX;uJGF{e2G7 M{ns[|Eh|ryP MW[xOUBucW5? MV3EUXNQ NUnkco85SmyxY3vzJGJEWi2rbnT1Z4VlKEyFUEGgd4VzcW6nLUWgZYN1cX[jdHnvci=> M{XKRlI1ODB7MkOz
JEKO-1 M2fjcWZ2dmO2aX;uJGF{e2G7 NEfKOWsyKM7:TR?= MUC3NkBp NYnzcm42UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJIlvKEmpTT3zeIlufWyjdHXkJGpGU09vMR?= MnKzNlM{PDF3NEG=
Granta-519 NXG2b2tNTnWwY4Tpc44hSXO|YYm= NFvGZocyKM7:TR?= MYmyJIg> NVvtcYhbUW6qaXLpeIlwdiCxZjDBb5QpfDNyODmgdIhwe3Cqb4L5cIF1cW:w NXftZpNCOjN|NEG1OFE>
Granta-519 MoWySpVv[3Srb36gRZN{[Xl? NYDKS2VbOSEQvF2= MVGyJIg> MYjJcohq[mm2aX;uJI9nKEGtdDjzOFc{MSCyaH;zdIhwenmuYYTpc44> MnnLNlM{PDF3NEG=
JEKO-1 M4HQSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYSxNEDPxE1? MWC3NkBp Mnv1TY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJJNtcWeqdHz5 NYXWXopMOjN|NEG1OFE>
JEKO-1 NGfSVZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrxXlVXPSEQvF2= MXO3NkBp M37DZYRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> MlfaNlM3PzZ{MkC=
MAVER-1 MlvnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFL5d202KM7:TR?= MnvBO|IhcA>? NYWySGQ4\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? MWmyN|Y4PjJ{MB?=
MINO MmPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3[4d|Uh|ryP M1Xw[VczKGh? MV\kc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz NGGy[|gzOzZ5NkKyNC=>
SP53 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYe1NmI6OC5zIN88US=> NXG3ZpdvPzJiaB?= M1TpSoRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> MWKyN|Y4PjJ{MB?=
HH NYSzZ25MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljINVAh|ryP M{iwdFczKGh? Mo\nSG1UVw>? NIS0[2lKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IIPsbYdpfGy7 MnjjNlI5ODF7NUm=
Myla MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXexNEDPxE1? Mlf0O|IhcA>? MlzHSG1UVw>? M2TQboRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= NHr4V4szOjhyMUm1PS=>
SR786 MlntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXsNVAh|ryP NIjKbmw4OiCq MlnmSG1UVw>? MWDkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MojhNlI5ODF7NUm=
HuT78 M170TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HvR|ExKM7:TR?= NYTmUGloPzJiaB?= NGDHPJpFVVOR Mora[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= MkHpNlI5ODF7NUm=
MJ NHLVXGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFmzSnAyOCEQvF2= Mny4O|IhcA>? MnLiSG1UVw>? NWrBfXo4\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> NHLBc4kzOjhyMUm1PS=>
DERL7 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXq0[Wp[OTBizszN NFrLO4s4OiCq M3fCbWROW09? NFHOb5pld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz NHzrfI8zOjhyMUm1PS=>
L1236 MlnVSpVv[3Srb36gRZN{[Xl? NYXVdVlpOTBizszN M4ju[FIhcA>? M3r4OmlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= M2DEOFIzOjFyOEe3
L428 NU\VeIJuTnWwY4Tpc44hSXO|YYm= NH3PRXIyOCEQvF2= MYqyJIg> MkPKTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w MmHqNlIzOTB6N{e=
L591 M1fLPWZ2dmO2aX;uJGF{e2G7 MX6xNEDPxE1? NHPtVJMzKGh? Mn3ITY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w MlLENlIzOTB6N{e=
KMH-2 MVfGeY5kfGmxbjDBd5NigQ>? NULFSG5NOTBizszN MYGyJIg> NXe1bJJ2UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u MmjSNlIzOTB6N{e=
L1236 MkXUSpVv[3Srb36gRZN{[Xl? M2W3UFUh|ryP MWiyOEBp MonZRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> MYWyNlIyODh5Nx?=
L591 NVHRXI44TnWwY4Tpc44hSXO|YYm= M17hTFUh|ryP MWCyOEBp MnLFRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> M{fMbVIzOjFyOEe3
L1236 MWnBdI9xfG:|aYOgRZN{[Xl? NYewPXpjPSEQvF2= MUOyOEBp M1XLVmlv\HWldHnvckBw\iCjcH;weI9{cXN? MoPGNlIzOTB6N{e=
L591 NXvCXYN2SXCxcITvd4l{KEG|c3H5 M4fFeVUh|ryP NFXvSFYzPCCq MX;JcoR2[3Srb36gc4Yh[XCxcITvd4l{ M2\Pc|IzOjFyOEe3
U-87MG NWCy[HprTnWwY4Tpc44hSXO|YYm= M4fiTlExOCCwTR?= MUGyOEBp MYnEUXNQ NG\5WpBKdmirYnn0bY9vKG:oIDDj[YxtKG2rZ4LheIlwdg>? NX;MZXpFOjJyN{m2NFk>
SW1783 M3zZcmZ2dmO2aX;uJGF{e2G7 M4\ab|ExOCCwTR?= Mn:4NlQhcA>? NH\XdJRFVVOR MVnJcohq[mm2aX;uJI9nKCClZXzsJI1q\3KjdHnvci=> MYeyNlA4QTZyOR?=
U-87MG MWDGeY5kfGmxbjDBd5NigQ>? NH;3bnI2KM7:TR?= M{K2RVI1KGh? MlraSG1UVw>? MUHJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> NGPBd4wzOjB5OU[wPS=>
SW1783 NYOwR4t[TnWwY4Tpc44hSXO|YYm= NXjC[nZQPSEQvF2= NUG3SnFrOjRiaB?= MmXRSG1UVw>? MojRTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> MYqyNlA4QTZyOR?=
U-373MG M3fOR2Z2dmO2aX;uJGF{e2G7 NIDme|Y2KM7:TR?= NWXEXWU3OjRiaB?= M3nzUGROW09? MV;Jcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> M{ewSlIzODd7NkC5
SK-MG3 M4TN[mZ2dmO2aX;uJGF{e2G7 M33yS|Uh|ryP MVqyOEBp NE\HRVlFVVOR MmrOTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NWSxPWd[OjJyN{m2NFk>
SU-DHL-5 M2HPUmZ2dmO2aX;uJGF{e2G7 M1;QSFEh|ryP MYiyOEBp MmXKSG1UVw>? NXzufXVbUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= NH7uTJIzODl3OU[wOi=>
WSU-NHL Mk[1SpVv[3Srb36gRZN{[Xl? NUS0eHRGOSEQvF2= MVqyOEBp NITE[pFFVVOR MW\JcoR2[3Srb36gc4Yh[XCxcITvd4l{ MU[yNFk2QTZyNh?=
CCRF-SB MnXySpVv[3Srb36gRZN{[Xl? MoPCNUDPxE1? MoLjNlQhcA>? MnvJSG1UVw>? MV7JcoR2[3Srb36gc4Yh[XCxcITvd4l{ MmHoNlA6PTl4ME[=
INA-6 NIPjT3NHfW6ldHnvckBCe3OjeR?= NF3ld5k2KM7:TR?= NVi3d|c5PiCq MlnITY5pcWKrdHnvckBw\iCSSUPLM2FsfCCjbnSgSXJMKHCjdHj3ZZk> MoTFNlA2ODVzNUi=
LB NHTpNFVHfW6ldHnvckBCe3OjeR?= M{j2PFUh|ryP MVW2JIg> MoLLTY5pcWKrdHnvckBw\iCSSUTLM2FsfCCjbnSgSXJMKHCjdHj3ZZk> M1jERVIxPTB3MUW4

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:[2]
+ Expand

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 Research:[2]
+ Expand
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL warmed (199.79 mM)
Ethanol 23 mg/mL (55.36 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG 400 (dissolve first)+0.5% Tween 80+5% Propylene glycol
For best results, use promptly after mixing.
30mg/mL

* 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 Information

Molecular Weight 415.42
Formula

C22H18FN7O

CAS No. 870281-82-6
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03576443 Recruiting Diffuse Large B Cell Lymphoma Nordic Lymphoma Group July 7 2017 Phase 2
NCT02962401 Active not recruiting Waldenstrom Macroglobulinemia French Innovative Leukemia Organisation March 7 2017 Phase 2
NCT02044822 Terminated B-cell Chronic Lymphocytic Leukemia (CLL) With 17p Deletion Gilead Sciences August 6 2014 Phase 2
NCT02436135 Completed Myelofibrosis Gilead Sciences June 5 2015 Phase 1
NCT01980888 Terminated Chronic Lymphocytic Leukemia Gilead Sciences February 5 2014 Phase 3
NCT02739360 Completed Lymphoid Malignancies Gilead Sciences May 4 2016 Phase 4

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    What is the recommended dose of CAL-101 and the route of administration for mouse studies?

  • Answer:

    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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID