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 NHjkfFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkKxSG1UVw>? M1LIRWlEPTB;MkCuOEDPxE1? NIXkc3EzPTl7OUO1Ni=>
CLL PBMCs NIn1VW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUD6WG1jTE2VTx?= NXjxS5M3UUN3ME2yMlkhdk1? M3vXT|I2QTF5Mk[3
U266 NIL2bY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIGwO2Q1OCEQvF2= NGHHTmo1QCCq MlT3O|kvPSViaX7obYJqfGmxbjDyZZRm M{PVdFI2OzN7M{Oy
K562 M3vk[WZ2dmO2aX;uJGF{e2G7 NELXeYYyKM7:TR?= MoHJN{Bp MlqxTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NEHSd5UzPTBzNEe3OS=>
K562 NH3VemtHfW6ldHnvckBCe3OjeR?= MoLONUDPxE1? MnT3N{Bp MonKTY5pcWKrdHnvckBw\iCSN{DTOmsheGixc4Doc5J6dGG2aX;u MU[yOVAyPDd5NR?=
K562 NGHsWXFHfW6ldHnvckBCe3OjeR?= MV6xJO69VQ>? NULRVHo5OyCq NV72[WFtUW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=> MnvCNlUxOTR5N{W=
K562 NIfLeoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXm[|cyKM7:TR?= M2T1NFczKGh? NYn0O49YUW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9v NGS2cW0zPTBzNEe3OS=>
Primary AML cell NEK2Z|FHfW6ldHnvckBCe3OjeR?= MYexJO69VQ>? MWCzJIg> NGnOOplKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= M1TPWVI2ODF2N{e1
Primary AML cell NEHzOWNHfW6ldHnvckBCe3OjeR?= M1rYOlEh|ryP NEXYV3o{KGh? MmW4TY5pcWKrdHnvckBw\iCSN{DTOmsheGixc4Doc5J6dGG2aX;u MUSyOVAyPDd5NR?=
Primary AML cell MXzGeY5kfGmxbjDBd5NigQ>? NYr2PYxyOSEQvF2= Mo\rN{Bp MmX3TY5pcWKrdHnvckBw\iCJU1uzJJBpd3OyaH;yfYxifGmxbh?= MXSyOVAyPDd5NR?=
Primary AML cell MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLONUDPxE1? MX2zJIg> NIm5cmZUfXCycnXzd4lwdiCxZjDyVm5CKHO7boTo[ZNqew>? NI\JVlczPTBzNEe3OS=>
Microglia NGTkdHZHfW6ldHnvckBCe3OjeR?= MUe1JO69VQ>? NVizO3liOTBiaB?= NEXIR|ZFVVOR MoXzSIVkemWjc3Wgc4YhXE6IYTDz[YNz\XSrb36g[pJwdSCOUGOtd5RqdXWuYYTl[EAheDFzMN80SFkyOEFxREmxNGEhdWmlcn;ncIli MWiyOFYzPTZ6NB?=
Primary CLL cell M2DpNWZ2dmO2aX;uJGF{e2G7 NE\rfocyKM7:TR?= NUfWeFN[OTVibXnu NVTEWXVZTE2VTx?= MXrCcI9kc3NiQlPSMYlv\HWlZXSgUGNROSC|ZYLpcoUuPSCjY4TpeoF1cW:w Mn2xNlQxODl{M{O=
JEKO-1 NE\BT2JHfW6ldHnvckBCe3OjeR?= M3P1UVEh|ryP NFPie2I4OiCq M4THWWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDpckBK\01vc4TpcZVt[XSnZDDKSWtQNTF? NXfGTldzOjN|NEG1OFE>
Granta-519 NWXYVYVUTnWwY4Tpc44hSXO|YYm= MUWxJO69VQ>? M3mxdVIhcA>? NV3xWGUxUW6qaXLpeIlwdiCxZjDBb5QpfDNyODmgdIhwe3Cqb4L5cIF1cW:w M1S0d|I{OzRzNUSx
Granta-519 MWLGeY5kfGmxbjDBd5NigQ>? M1PVZVEh|ryP NEfYUIkzKGh? M3rI[GlvcGmkaYTpc44hd2ZiQXv0LJM1PzNrIIDoc5NxcG:{eXzheIlwdg>? MmTVNlM{PDF3NEG=
JEKO-1 NF2ydVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7GbY4yOCEQvF2= M{jnNVczKGh? MnzNTY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJJNtcWeqdHz5 NX:4SINUOjN|NEG1OFE>
JEKO-1 NWD3VpV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\4RnFVPSEQvF2= NITlO5k4OiCq Mnz0[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> NH[xVmMzOzZ5NkKyNC=>
MAVER-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\pOUDPxE1? MUe3NkBp MYXkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz M4m1eFI{Pjd4MkKw
MINO MorPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTKOUDPxE1? NF\ZSmg4OiCq NVzrOWxt\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? M1TZeFI{Pjd4MkKw
SP53 MnezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUWwMlEh|ryP NYPSe5dkPzJiaB?= M3\SVIRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> MX[yN|Y4PjJ{MB?=
HH M3vBWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXycI4yOCEQvF2= Mm\vO|IhcA>? NWfhOFROTE2VTx?= M1PY[Wlv\HWldHnvckBw\iCjcH;weI9{cXNic3zp[4h1dHl? Mo\mNlI5ODF7NUm=
Myla MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELiR5cyOCEQvF2= NHPrWXU4OiCq M37aWWROW09? MoTm[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NYDaeohWOjJ6MEG5OVk>
SR786 NGezZnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLjPJEyOCEQvF2= M1vEOlczKGh? M4rkeWROW09? M{Xid4Rw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= MVeyNlgxOTl3OR?=
HuT78 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVexNEDPxE1? MYS3NkBp M37VemROW09? M3u4V4Rw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= M1XWW|IzQDBzOUW5
MJ NWTsR4c5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGL6V5UyOCEQvF2= MlHZO|IhcA>? MYLEUXNQ M2TTWoRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= NXnsOnlFOjJ6MEG5OVk>
DERL7 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHFNVAh|ryP MljSO|IhcA>? NHTwWndFVVOR MVnkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MnnXNlI5ODF7NUm=
L1236 MYHGeY5kfGmxbjDBd5NigQ>? MXWxNEDPxE1? NWrTTIlmOiCq MlfRTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NV[2[YhZOjJ{MUC4O|c>
L428 M{HY[2Z2dmO2aX;uJGF{e2G7 NHfiV4UyOCEQvF2= M{GyTFIhcA>? MWLJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? MnTPNlIzOTB6N{e=
L591 M1nUfGZ2dmO2aX;uJGF{e2G7 MWOxNEDPxE1? NVvnW|BROiCq MUPJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? MX2yNlIyODh5Nx?=
KMH-2 NXfofXhYTnWwY4Tpc44hSXO|YYm= NX3PdmxGOTBizszN NYW2Z483OiCq NYnIWllWUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u MUSyNlIyODh5Nx?=
L1236 NFnjVYlHfW6ldHnvckBCe3OjeR?= MWS1JO69VQ>? M1rOelI1KGh? MoTZRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> MWGyNlIyODh5Nx?=
L591 M2TaXGZ2dmO2aX;uJGF{e2G7 M{P4[VUh|ryP MkLuNlQhcA>? MnzkRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> Mny0NlIzOTB6N{e=
L1236 NYj5RXVTSXCxcITvd4l{KEG|c3H5 MUK1JO69VQ>? M37BVVI1KGh? MX3JcoR2[3Srb36gc4Yh[XCxcITvd4l{ MmHFNlIzOTB6N{e=
L591 NX7ycW13SXCxcITvd4l{KEG|c3H5 M4rzXVUh|ryP MV:yOEBp NETYXpdKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NFHUSWwzOjJzMEi3Oy=>
U-87MG MnTqSpVv[3Srb36gRZN{[Xl? NUHRSWpNOTByIH7N NYq5TWdOOjRiaB?= NGjYTlFFVVOR M3[1ZWlvcGmkaYTpc44hd2ZiIHPlcIwhdWmpcnH0bY9v MnPnNlIxPzl4MEm=
SW1783 MmGySpVv[3Srb36gRZN{[Xl? NGK4OnIyODBibl2= NWLCXGpzOjRiaB?= NUTYZlhWTE2VTx?= NF\IVHdKdmirYnn0bY9vKG:oIDDj[YxtKG2rZ4LheIlwdg>? Mnq2NlIxPzl4MEm=
U-87MG MYDGeY5kfGmxbjDBd5NigQ>? MlTlOUDPxE1? NETvS2czPCCq M4THemROW09? MWfJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> M3LF[FIzODd7NkC5
SW1783 NY\VbFB6TnWwY4Tpc44hSXO|YYm= MYK1JO69VQ>? M2\vW|I1KGh? M2nFT2ROW09? M3XkfWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6 MlPZNlIxPzl4MEm=
U-373MG M2fvVGZ2dmO2aX;uJGF{e2G7 Ml;uOUDPxE1? MmrVNlQhcA>? MnnPSG1UVw>? MXPJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> M3jkcVIzODd7NkC5
SK-MG3 NXXnfmp2TnWwY4Tpc44hSXO|YYm= Mn25OUDPxE1? NUXvdG5{OjRiaB?= MlXnSG1UVw>? NIDGfopKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? NHTwUHAzOjB5OU[wPS=>
SU-DHL-5 NGHVSodHfW6ldHnvckBCe3OjeR?= M{fJNlEh|ryP NYfm[3E2OjRiaB?= M{HEfGROW09? M1jaSGlv\HWldHnvckBw\iCjcH;weI9{cXN? Ml62NlA6PTl4ME[=
WSU-NHL M1nEcWZ2dmO2aX;uJGF{e2G7 M1HXUFEh|ryP MXOyOEBp M3XwTWROW09? M1njUWlv\HWldHnvckBw\iCjcH;weI9{cXN? M3PnXFIxQTV7NkC2
CCRF-SB Mn73SpVv[3Srb36gRZN{[Xl? MYGxJO69VQ>? NHfnbZozPCCq MUXEUXNQ MVvJcoR2[3Srb36gc4Yh[XCxcITvd4l{ MYKyNFk2QTZyNh?=
INA-6 MWPGeY5kfGmxbjDBd5NigQ>? M3HkdFUh|ryP Mnv4OkBp NILjeHlKdmirYnn0bY9vKG:oIGDJN2swSWu2IHHu[EBGWkticHH0bJdigQ>? NH;Hd2EzODVyNUG1PC=>
LB NWLWUWh6TnWwY4Tpc44hSXO|YYm= NW\6eVNGPSEQvF2= NEKxV2w3KGh? NWrNOYNNUW6qaXLpeIlwdiCxZjDQTVRMN0GtdDDhcoQhTVKNIIDheIh4[Xl? M2\RVFIxPTB3MUW4

... 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 individually and in order:
30% PEG 400 (dissolve first)+0.5% Tween 80+5% Propylene glycol
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
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