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 30 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)
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 Mm\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofBSG1UVw>? MYDJR|UxRTJyLkSg{txO MlywNlU6QTl|NUK=
CLL PBMCs M1HGemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml75SG1UVw>? NEDyco9KSzVyPUKuPUBvVQ>? M33aWlI2QTF5Mk[3
U266 M4nYXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2joN|QxKM7:TR?= MlHnOFghcA>? Ml\ZO|kvPSViaX7obYJqfGmxbjDyZZRm MlrCNlU{Ozl|M{K=
K562 M1fnb2Z2dmO2aX;uJGF{e2G7 MUixJO69VQ>? NG\sfZQ{KGh? NX3iUFVXUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u Mlr2NlUxOTR5N{W=
K562 NWjrXnBpTnWwY4Tpc44hSXO|YYm= NHvmXFgyKM7:TR?= M3GyUlMhcA>? MUjJcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:|cHjvdplt[XSrb36= NYHCcXhQOjVyMUS3O|U>
K562 NWn4SWJDTnWwY4Tpc44hSXO|YYm= MVyxJO69VQ>? M4HkW|MhcA>? NVGwOng1UW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=> MmHGNlUxOTR5N{W=
K562 NGHi[FJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHBNUDPxE1? MnnVO|IhcA>? NITMVXRKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44> MonhNlUxOTR5N{W=
Primary AML cell MnOySpVv[3Srb36gRZN{[Xl? NI\2eXcyKM7:TR?= NWjYcpNROyCq MU\Jcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? M3HN[FI2ODF2N{e1
Primary AML cell Mnr4SpVv[3Srb36gRZN{[Xl? NH3n[HIyKM7:TR?= MkPkN{Bp MkfqTY5pcWKrdHnvckBw\iCSN{DTOmsheGixc4Doc5J6dGG2aX;u NHvrSVQzPTBzNEe3OS=>
Primary AML cell NV;rWHMxTnWwY4Tpc44hSXO|YYm= NG\HV40yKM7:TR?= NXHQRW5{OyCq NV35TY43UW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=> M4r6V|I2ODF2N{e1
Primary AML cell NIDsUplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHrTZgyKM7:TR?= MWOzJIg> NFvae2VUfXCycnXzd4lwdiCxZjDyVm5CKHO7boTo[ZNqew>? M2qwTVI2ODF2N{e1
Microglia NH3X[3pHfW6ldHnvckBCe3OjeR?= MYG1JO69VQ>? MYWxNEBp MkDwSG1UVw>? MXjE[YNz\WG|ZTDv[kBVVk[jIIPlZ5JmfGmxbjDmdo9uKEySUz3zeIlufWyjdHXkJEBxOTFyzsTEPVExSS:GOUGwRUBucWO{b3fsbYE> MofpNlQ3OjV4OES=
Primary CLL cell NYjKNJF3TnWwY4Tpc44hSXO|YYm= NUfVO5pOOSEQvF2= MkPyNVUhdWmw M{fqb2ROW09? MUDCcI9kc3NiQlPSMYlv\HWlZXSgUGNROSC|ZYLpcoUuPSCjY4TpeoF1cW:w M3jVUlI1ODB7MkOz
JEKO-1 NFG1SG1HfW6ldHnvckBCe3OjeR?= NHGyc4IyKM7:TR?= MUS3NkBp NHvp[JpKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gbY4hUWePLYP0bY12dGG2ZXSgTmVMVy1z M{nNbFI{OzRzNUSx
Granta-519 NXn1WIhuTnWwY4Tpc44hSXO|YYm= MX6xJO69VQ>? NVfQUmx5OiCq NXfrSoJNUW6qaXLpeIlwdiCxZjDBb5QpfDNyODmgdIhwe3Cqb4L5cIF1cW:w NWPZPHhLOjN|NEG1OFE>
Granta-519 Mnr6SpVv[3Srb36gRZN{[Xl? NUHCdGdyOSEQvF2= NH24PFAzKGh? M3;TXGlvcGmkaYTpc44hd2ZiQXv0LJM1PzNrIIDoc5NxcG:{eXzheIlwdg>? NWn1[JRjOjN|NEG1OFE>
JEKO-1 MljNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonhNVAh|ryP NH\qTJY4OiCq M{j6T2lvcGmkaYTpc44hd2ZicILvcIln\XKjdHnvckB{dGmpaITsfS=> NFftZlAzOzN2MUW0NS=>
JEKO-1 MoTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3O2RlUh|ryP NWLNUVdDPzJiaB?= M3u0fYRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> M1vNe|I{Pjd4MkKw
MAVER-1 NInqcJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXixe5IzPSEQvF2= NUiwUm1vPzJiaB?= NUjjNpZQ\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? MYqyN|Y4PjJ{MB?=
MINO MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHHW4RnPSEQvF2= NUnvdWV6PzJiaB?= M3HMSYRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> MmjrNlM3PzZ{MkC=
SP53 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTrNE4yKM7:TR?= NUDONmxjPzJiaB?= M4q1TYRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> MojhNlM3PzZ{MkC=
HH MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTyVJZwOTBizszN NXzNUXo5PzJiaB?= NYPreldkTE2VTx?= MkC0TY5lfWO2aX;uJI9nKGGyb4D0c5NqeyC|bHnnbJRtgQ>? NITSN5kzOjhyMUm1PS=>
Myla NGDZdm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PydFExKM7:TR?= Mkn6O|IhcA>? Ml;FSG1UVw>? NHu5Wolld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz Mly1NlI5ODF7NUm=
SR786 Mo\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWWxNEDPxE1? NWq5coZKPzJiaB?= NFP0do1FVVOR MYfkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| M3;vPVIzQDBzOUW5
HuT78 M4r2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTpNVAh|ryP MkLEO|IhcA>? NGP5eHBFVVOR MUHkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| Mn7YNlI5ODF7NUm=
MJ NWLOTFhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nnU|ExKM7:TR?= NV\ZVHN2PzJiaB?= MorrSG1UVw>? MoLL[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= MoTVNlI5ODF7NUm=
DERL7 NUHPU29VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHaNVAh|ryP MUC3NkBp NH7KNnFFVVOR Moiy[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= MYOyNlgxOTl3OR?=
L1236 NYjNXFBoTnWwY4Tpc44hSXO|YYm= M4fSUlExKM7:TR?= MU[yJIg> NWK4Z3FOUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u M3XPOlIzOjFyOEe3
L428 NGXEXW9HfW6ldHnvckBCe3OjeR?= M2DSb|ExKM7:TR?= M3\pe|IhcA>? M1e3NWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= MXOyNlIyODh5Nx?=
L591 M3mwSmZ2dmO2aX;uJGF{e2G7 NV;j[FN[OTBizszN M3L5VlIhcA>? MVHJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? MYCyNlIyODh5Nx?=
KMH-2 MV;GeY5kfGmxbjDBd5NigQ>? MoDNNVAh|ryP MkLWNkBp NHXR[4tKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= MY[yNlIyODh5Nx?=
L1236 MnLOSpVv[3Srb36gRZN{[Xl? M1[xb|Uh|ryP NHnKXoMzPCCq M2jCTGJtd2OtczDz[YNz\XSrb36gc4YhfGinIFPDUFU> Mm\jNlIzOTB6N{e=
L591 M2jBNmZ2dmO2aX;uJGF{e2G7 M2OwbFUh|ryP MXSyOEBp MoDiRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> M{LDU|IzOjFyOEe3
L1236 M1S4T2Fxd3C2b4Ppd{BCe3OjeR?= NIrWO5g2KM7:TR?= NVH0fVVjOjRiaB?= NVPhWG5ZUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= MXWyNlIyODh5Nx?=
L591 NGmxeGFCeG:ydH;zbZMhSXO|YYm= MXm1JO69VQ>? NXfGboZ[OjRiaB?= M1jSZWlv\HWldHnvckBw\iCjcH;weI9{cXN? MVWyNlIyODh5Nx?=
U-87MG MYnGeY5kfGmxbjDBd5NigQ>? MkTBNVAxKG6P M{DVelI1KGh? M2HsZmROW09? NEHrWI5KdmirYnn0bY9vKG:oIDDj[YxtKG2rZ4LheIlwdg>? NEnhUWgzOjB5OU[wPS=>
SW1783 NFH6[IpHfW6ldHnvckBCe3OjeR?= MkDlNVAxKG6P M2PQUVI1KGh? MU\EUXNQ M4PY[mlvcGmkaYTpc44hd2ZiIHPlcIwhdWmpcnH0bY9v M2Pw[lIzODd7NkC5
U-87MG NGPZbXNHfW6ldHnvckBCe3OjeR?= MmW0OUDPxE1? Mm\sNlQhcA>? NEHtfGdFVVOR MUnJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> NULOeY55OjJyN{m2NFk>
SW1783 NXvpU45mTnWwY4Tpc44hSXO|YYm= MX61JO69VQ>? MkPoNlQhcA>? MkXXSG1UVw>? NIT3OFZKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? NWjQ[mRtOjJyN{m2NFk>
U-373MG MV3GeY5kfGmxbjDBd5NigQ>? MYS1JO69VQ>? NHTEc4YzPCCq MnTWSG1UVw>? MUXJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> NWHqZ21sOjJyN{m2NFk>
SK-MG3 M3zD[GZ2dmO2aX;uJGF{e2G7 NFTUWHk2KM7:TR?= M{XkSVI1KGh? NFPIfFZFVVOR M1m3WWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6 M{e1bFIzODd7NkC5
SU-DHL-5 MYjGeY5kfGmxbjDBd5NigQ>? MU[xJO69VQ>? M1O3eFI1KGh? NFq3O45FVVOR NH;zWIRKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| Mn;qNlA6PTl4ME[=
WSU-NHL MoXaSpVv[3Srb36gRZN{[Xl? MWmxJO69VQ>? NHfIeVIzPCCq NIq0OW1FVVOR NH3Tc|ZKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NWD3d2w4OjB7NUm2NFY>
CCRF-SB M3rTNGZ2dmO2aX;uJGF{e2G7 NFjpNXUyKM7:TR?= MV6yOEBp NXvKS4FLTE2VTx?= MYnJcoR2[3Srb36gc4Yh[XCxcITvd4l{ NUeyc3lOOjB7NUm2NFY>
INA-6 M3fJZWZ2dmO2aX;uJGF{e2G7 MWO1JO69VQ>? NUW0VYlNPiCq MULJcohq[mm2aX;uJI9nKFCLM1uvRYt1KGGwZDDFVmsheGG2aIfhfS=> M1nuVVIxPTB3MUW4
LB M3\vbmZ2dmO2aX;uJGF{e2G7 NWjEb4J1PSEQvF2= NIXMW4k3KGh? MUnJcohq[mm2aX;uJI9nKFCLNFuvRYt1KGGwZDDFVmsheGG2aIfhfS=> NFfwfFIzODVyNUG1PC=>

... 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:
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
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

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

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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. http://www.ncbi.nlm.nih.gov.ezproxy.liv.ac.uk/pubmed/?term=PI3K%CE%B4+inhibition+reduces+TNF+secretion+and+neuroinflammation+in+a+mouse+cerebral+stroke+model

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID