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 29 Publications

4 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.

    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

Choose Selective PI3K Inhibitors

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)
p110β [1]
(Cell-free assay)
p110α [1]
(Cell-free assay)
hVps34 [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MEC1 M4nRdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmL2SG1UVw>? NYTsbnVkUUN3ME2yNE41KM7:TR?= NH7Z[3czPTl7OUO1Ni=>
CLL PBMCs MmnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPKSG1UVw>? MVLJR|UxRTJwOTDuUS=> NWToSY9HOjV7MUeyOlc>
U266 NU\wdXhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUS0NEDPxE1? MWm0PEBp M3T1UFc6NjVnIHnubIljcXSrb36gdoF1\Q>? M4fwRVI2OzN7M{Oy
K562 MVjGeY5kfGmxbjDBd5NigQ>? MnTjNUDPxE1? NUW3bnJ1OyCq NXzIXWNWUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u MVqyOVAyPDd5NR?=
K562 NH36eHZHfW6ldHnvckBCe3OjeR?= NITlWHgyKM7:TR?= NGHNbY0{KGh? NGLRU3dKdmirYnn0bY9vKG:oIGC3NHM3UyCyaH;zdIhwenmuYYTpc44> MoTjNlUxOTR5N{W=
K562 MVnGeY5kfGmxbjDBd5NigQ>? MXSxJO69VQ>? MlzmN{Bp M1Hn[2lvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= NV74c3I6OjVyMUS3O|U>
K562 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7vRWkyKM7:TR?= NUXmZnVtPzJiaB?= MUDJcohq[mm2aX;uJI9nKHC{b3zp[oVz[XSrb36= NUm5TmpkOjVyMUS3O|U>
Primary AML cell MVTGeY5kfGmxbjDBd5NigQ>? NY[4Zo5LOSEQvF2= NHy2fpA{KGh? MVzJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? M2TxNVI2ODF2N{e1
Primary AML cell M2f0OWZ2dmO2aX;uJGF{e2G7 NHjKbYUyKM7:TR?= M4jRTFMhcA>? NH3HNmVKdmirYnn0bY9vKG:oIGC3NHM3UyCyaH;zdIhwenmuYYTpc44> NHnjNHczPTBzNEe3OS=>
Primary AML cell NFXpN2tHfW6ldHnvckBCe3OjeR?= NHW1NlQyKM7:TR?= NFjURlk{KGh? MUXJcohq[mm2aX;uJI9nKEeVS{OgdIhwe3Cqb4L5cIF1cW:w Ml60NlUxOTR5N{W=
Primary AML cell NGDiWVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDEcWEyKM7:TR?= NV25UnJxOyCq MoiyV5VxeHKnc4Ppc44hd2ZicmLORUB{gW62aHXzbZM> NIOzbmszPTBzNEe3OS=>
Microglia MU\GeY5kfGmxbjDBd5NigQ>? M1\1TFUh|ryP MoPMNVAhcA>? NFXVTWRFVVOR MkfOSIVkemWjc3Wgc4YhXE6IYTDz[YNz\XSrb36g[pJwdSCOUGOtd5RqdXWuYYTl[EAheDFzMN80SFkyOEFxREmxNGEhdWmlcn;ncIli NHjlSI4zPDZ{NU[4OC=>
Primary CLL cell MXrGeY5kfGmxbjDBd5NigQ>? Mk\NNUDPxE1? MWOxOUBucW5? M{XrSWROW09? MUXCcI9kc3NiQlPSMYlv\HWlZXSgUGNROSC|ZYLpcoUuPSCjY4TpeoF1cW:w MlLJNlQxODl{M{O=
JEKO-1 M2fzVGZ2dmO2aX;uJGF{e2G7 NYXGbpBGOSEQvF2= NH;1dGY4OiCq MWTJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25iaX6gTYdONXO2aX31cIF1\WRiSlXLU{0y NXnwR3U2OjN|NEG1OFE>
Granta-519 NEfLN|dHfW6ldHnvckBCe3OjeR?= M4PoTVEh|ryP NX6zZppsOiCq NULmV3RwUW6qaXLpeIlwdiCxZjDBb5QpfDNyODmgdIhwe3Cqb4L5cIF1cW:w NX71eZpGOjN|NEG1OFE>
Granta-519 M{\lSGZ2dmO2aX;uJGF{e2G7 MnP2NUDPxE1? MmnqNkBp M4XteGlvcGmkaYTpc44hd2ZiQXv0LJM1PzNrIIDoc5NxcG:{eXzheIlwdg>? MoG4NlM{PDF3NEG=
JEKO-1 M3\NVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWWxNEDPxE1? NWnSW3RXPzJiaB?= M1fVRmlvcGmkaYTpc44hd2ZicILvcIln\XKjdHnvckB{dGmpaITsfS=> MX2yN|M1OTV2MR?=
JEKO-1 NVjxXIh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofEOUDPxE1? NITkZpY4OiCq MoXJ[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> Mn3oNlM3PzZ{MkC=
MAVER-1 MnTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYq1JO69VQ>? NVHjZmsyPzJiaB?= NVHkVHdu\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? MXyyN|Y4PjJ{MB?=
MINO NGDGS3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3H5S|Uh|ryP NYW2bGJIPzJiaB?= MmDo[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> MYCyN|Y4PjJ{MB?=
SP53 M3m3R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PJU|AvOSEQvF2= M4rSO|czKGh? MXTkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz MmnzNlM3PzZ{MkC=
HH M2fMXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInRN2IyOCEQvF2= NE\ZNXE4OiCq MXXEUXNQ NWTadXVTUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDzcIlocHSueR?= NGq0doEzOjhyMUm1PS=>
Myla MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnn4NVAh|ryP MWK3NkBp M{fzeWROW09? NInmOHFld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MnjENlI5ODF7NUm=
SR786 M3PvUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVr0RZp5OTBizszN NX3MdmlMPzJiaB?= NIezZlRFVVOR M{TkWYRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= Mn3YNlI5ODF7NUm=
HuT78 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPXTZZoOTBizszN NH\qWZk4OiCq MXLEUXNQ MnPE[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NVP5NYt[OjJ6MEG5OVk>
MJ NIrST21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\qcFEyOCEQvF2= Mle2O|IhcA>? MlXVSG1UVw>? NInGN|hld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MV2yNlgxOTl3OR?=
DERL7 M{Hqd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTWNVAh|ryP NXHzbZJ1PzJiaB?= MkHFSG1UVw>? NWD1XlQ{\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> M3T5UVIzQDBzOUW5
L1236 NVzFXXo2TnWwY4Tpc44hSXO|YYm= NYjmVVdnOTBizszN M1PSPFIhcA>? M3XKb2lvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= MnHZNlIzOTB6N{e=
L428 NFT6[JZHfW6ldHnvckBCe3OjeR?= NXH6UpNpOTBizszN M1HXS|IhcA>? MnPNTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NGrqTIwzOjJzMEi3Oy=>
L591 NEf3NnNHfW6ldHnvckBCe3OjeR?= NV3nSVZqOTBizszN MX2yJIg> NWrvfnc{UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u NV63VWlHOjJ{MUC4O|c>
KMH-2 NWXYTmk5TnWwY4Tpc44hSXO|YYm= MnfwNVAh|ryP M3z1UlIhcA>? MnjGTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w M{LWZlIzOjFyOEe3
L1236 NHvselVHfW6ldHnvckBCe3OjeR?= NVPCR3E3PSEQvF2= M3XiblI1KGh? NFzGe3RDdG:la4Ogd4VkemW2aX;uJI9nKHSqZTDDR2w2 NHnJbZczOjJzMEi3Oy=>
L591 NYnWcmc4TnWwY4Tpc44hSXO|YYm= NX3vOFlKPSEQvF2= MVKyOEBp Mn\nRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> MViyNlIyODh5Nx?=
L1236 NUfQ[XlNSXCxcITvd4l{KEG|c3H5 M{\FcVUh|ryP M1u2N|I1KGh? MkTQTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? M1zOZ|IzOjFyOEe3
L591 NWiyZ2hGSXCxcITvd4l{KEG|c3H5 NFnsRYE2KM7:TR?= M1L5OlI1KGh? NYHudFVKUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= NYrIfZJ5OjJ{MUC4O|c>
U-87MG Ml3xSpVv[3Srb36gRZN{[Xl? MmLkNVAxKG6P MYCyOEBp Mn7sSG1UVw>? MnGzTY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> MVqyNlA4QTZyOR?=
SW1783 M2\CRmZ2dmO2aX;uJGF{e2G7 M1PiU|ExOCCwTR?= NGP0dJozPCCq NEL3TIpFVVOR MYPJcohq[mm2aX;uJI9nKCClZXzsJI1q\3KjdHnvci=> NFnWTG8zOjB5OU[wPS=>
U-87MG M{fmNmZ2dmO2aX;uJGF{e2G7 MUC1JO69VQ>? MVOyOEBp MVTEUXNQ MmjITY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> MWWyNlA4QTZyOR?=
SW1783 MkizSpVv[3Srb36gRZN{[Xl? NWLuO4V4PSEQvF2= NWDjVZFoOjRiaB?= NWHK[JF3TE2VTx?= MkL1TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> MV[yNlA4QTZyOR?=
U-373MG MX;GeY5kfGmxbjDBd5NigQ>? NWL1Oph1PSEQvF2= M2HUR|I1KGh? Mnj2SG1UVw>? NVHrOoFbUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? MXiyNlA4QTZyOR?=
SK-MG3 M3zpbWZ2dmO2aX;uJGF{e2G7 MmiwOUDPxE1? MYWyOEBp NWW0ZmtSTE2VTx?= MVXJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> NHvyT3EzOjB5OU[wPS=>
SU-DHL-5 NU\4bGVvTnWwY4Tpc44hSXO|YYm= MWCxJO69VQ>? M4DLT|I1KGh? NHnqTo9FVVOR NGHKR5JKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NYXpbFduOjB7NUm2NFY>
WSU-NHL MUnGeY5kfGmxbjDBd5NigQ>? MXGxJO69VQ>? MYmyOEBp MnrlSG1UVw>? NGTFUnFKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| MVSyNFk2QTZyNh?=
CCRF-SB MlvUSpVv[3Srb36gRZN{[Xl? M{n4UlEh|ryP Mli5NlQhcA>? MoHwSG1UVw>? NUfacZR1UW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= MV:yNFk2QTZyNh?=
INA-6 MWnGeY5kfGmxbjDBd5NigQ>? NGjWSGc2KM7:TR?= M4i2[VYhcA>? MlfpTY5pcWKrdHnvckBw\iCSSUPLM2FsfCCjbnSgSXJMKHCjdHj3ZZk> NH\we5kzODVyNUG1PC=>
LB MX;GeY5kfGmxbjDBd5NigQ>? NEG2UHc2KM7:TR?= NGToV5o3KGh? MmDBTY5pcWKrdHnvckBw\iCSSUTLM2FsfCCjbnSgSXJMKHCjdHj3ZZk> M1rCXVIxPTB3MUW4

... 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 <1 mg/mL
In vivo 30% PEG 400 (dissolve first)+0.5% Tween 80+5% Propylene glycol 30mg/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 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
NCT02457598 Recruiting B-cell Malignancies Gilead Sciences June 30, 2015 Phase 1
NCT02962401 Not yet recruiting Waldenstrom Macroglobulinemia French Innovative Leukemia Organisation January 2017 Phase 2
NCT02928510 Not yet recruiting 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 Jonsson Comprehensive Cancer Center|Gilead Sciences|National Cancer Institute (NCI) January 2017 --
NCT02968563 Recruiting Chronic Lymphocytic Leukemia Gilead Sciences|German CLL Study Group December 2016 Phase 2
NCT02639910 Recruiting Leukemia, Lymphocytic, Chronic, B-Cell|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma MorphoSys AG November 2016 Phase 2
NCT02970318 Recruiting Chronic Lymphocytic Leukemia Acerta Pharma BV September 2016 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID