CAL-101 (Idelalisib, GS-1101)

Catalog No.S2226

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

Molecular Weight(MW): 415.42

CAL-101 (Idelalisib, 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.

Size Price Stock Quantity  
In DMSO USD 156 In stock
USD 120 In stock
USD 470 In stock

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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 . CAL-101 (Idelalisib, 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. CAL-101 (Idelalisib, 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. CAL-101 (Idelalisib, 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. CAL-101 (Idelalisib, GS-1101) purchased from Selleck.

Purity & Quality Control

Choose Selective PI3K Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description CAL-101 (Idelalisib, 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 MoXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml[wSG1UVw>? MVjJR|UxRTJyLkSg{txO NFuz[mMzPTl7OUO1Ni=>
CLL PBMCs MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPiSG1UVw>? NVH1bXFHUUN3ME2yMlkhdk1? Ml7iNlU6OTd{Nke=
U266 NWrqOIhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1T2XFQxKM7:TR?= NYjhRYo2PDhiaB?= M3[wRlc6NjVnIHnubIljcXSrb36gdoF1\Q>? MUCyOVM{QTN|Mh?=
K562 M{n4WGZ2dmO2aX;uJGF{e2G7 M1\QZ|Eh|ryP NXXlTVhEOyCq Mn;kTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w MX[yOVAyPDd5NR?=
K562 MX\GeY5kfGmxbjDBd5NigQ>? NIn1dYsyKM7:TR?= MXKzJIg> NX3aXIExUW6qaXLpeIlwdiCxZjDQO|BUPkticHjvd5Bpd3K7bHH0bY9v M2r2WVI2ODF2N{e1
K562 NVLXfpNLTnWwY4Tpc44hSXO|YYm= NWPEWZdJOSEQvF2= Mk\2N{Bp M{DWPGlvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= MlfSNlUxOTR5N{W=
K562 NXXUUVRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqxJO69VQ>? NWfwenM{PzJiaB?= M4HqRWlvcGmkaYTpc44hd2ZicILvcIln\XKjdHnvci=> NWLEeYxiOjVyMUS3O|U>
Primary AML cell MV\GeY5kfGmxbjDBd5NigQ>? M4rZUlEh|ryP M3rPPFMhcA>? MVjJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? MWWyOVAyPDd5NR?=
Primary AML cell MVLGeY5kfGmxbjDBd5NigQ>? MmfaNUDPxE1? NW\pN3VIOyCq MVrJcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:|cHjvdplt[XSrb36= MnL1NlUxOTR5N{W=
Primary AML cell NVHD[495TnWwY4Tpc44hSXO|YYm= M2\xXlEh|ryP NYq0clRGOyCq NYm1cowyUW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=> M1PP[FI2ODF2N{e1
Primary AML cell M{GyPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:xJO69VQ>? MWSzJIg> NUf5eItHW3WycILld5Nqd25ib3[gdnJPSSC|eX70bIV{cXN? NWK1SJBYOjVyMUS3O|U>
Microglia M4HubWZ2dmO2aX;uJGF{e2G7 NHjMOWM2KM7:TR?= M1TVOlExKGh? MmXNSG1UVw>? MnfKSIVkemWjc3Wgc4YhXE6IYTDz[YNz\XSrb36g[pJwdSCOUGOtd5RqdXWuYYTl[EAheDFzMN80SFkyOEFxREmxNGEhdWmlcn;ncIli M1HlbVI1PjJ3Nki0
Primary CLL cell NHHuPYpHfW6ldHnvckBCe3OjeR?= M4LSUlEh|ryP M4fuSFE2KG2rbh?= NVTSfVhvTE2VTx?= M1vPWGJtd2OtczDCR3IucW6mdXPl[EBNS1BzIIPldolv\S13IHHjeIl3[XSrb36= M2jpfFI1ODB7MkOz
JEKO-1 Mnz2SpVv[3Srb36gRZN{[Xl? M1XRWVEh|ryP NGPJTFY4OiCq NF:0O2tKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gbY4hUWePLYP0bY12dGG2ZXSgTmVMVy1z Mn\WNlM{PDF3NEG=
Granta-519 NFT3T|RHfW6ldHnvckBCe3OjeR?= NGHqeJgyKM7:TR?= NFLUWHUzKGh? MWrJcohq[mm2aX;uJI9nKEGtdDj0N|A5MSCyaH;zdIhwenmuYYTpc44> M1OwV|I{OzRzNUSx
Granta-519 M1zwcmZ2dmO2aX;uJGF{e2G7 MlzRNUDPxE1? MVKyJIg> NVTFc5JMUW6qaXLpeIlwdiCxZjDBb5QpezR5MzmgdIhwe3Cqb4L5cIF1cW:w MlzINlM{PDF3NEG=
JEKO-1 NV\PZXIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPsc|AxOTBizszN MV:3NkBp NFXpUXNKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44he2yrZ3j0cJk> NYWyO4lxOjN|NEG1OFE>
JEKO-1 M3[wdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDSOIM2KM7:TR?= Ml2zO|IhcA>? MYTkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz M3XFSlI{Pjd4MkKw
MAVER-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlqwOUDPxE1? Mk\FO|IhcA>? M{jjfYRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> M17KTFI{Pjd4MkKw
MINO MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVm1JO69VQ>? MV[3NkBp MXXkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz MY[yN|Y4PjJ{MB?=
SP53 NIHqVo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TCNVAvOSEQvF2= M1f2VFczKGh? NHP0SIhld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ M2H4clI{Pjd4MkKw
HH MmXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVmxNEDPxE1? MnnmO|IhcA>? MknCSG1UVw>? M1T1Smlv\HWldHnvckBw\iCjcH;weI9{cXNic3zp[4h1dHl? M3zBUVIzQDBzOUW5
Myla NWG0TWJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfSR3AyOCEQvF2= NXjlc2tXPzJiaB?= NHPWNItFVVOR NGfMVnhld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MVGyNlgxOTl3OR?=
SR786 MlTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXXWolEOTBizszN NWruRYpCPzJiaB?= MlnBSG1UVw>? NGPmenJld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MX6yNlgxOTl3OR?=
HuT78 M3rKbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPzZWVOOTBizszN MYO3NkBp M165TWROW09? MYjkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| NWHXb|NxOjJ6MEG5OVk>
MJ NVnOcHJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXHbJp[OTBizszN MorBO|IhcA>? NEjEd3NFVVOR MWDkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| NUPNbJZjOjJ6MEG5OVk>
DERL7 NWLaZ5o4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVexNEDPxE1? MljPO|IhcA>? MVrEUXNQ M3HCN4Rw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= NX;sR3RxOjJ6MEG5OVk>
L1236 MVjGeY5kfGmxbjDBd5NigQ>? NXLxN2RGOTBizszN MkD1NkBp M{jYdWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= NH64OFMzOjJzMEi3Oy=>
L428 MkHNSpVv[3Srb36gRZN{[Xl? NG\JfZkyOCEQvF2= MorQNkBp M1rvXWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= MWmyNlIyODh5Nx?=
L591 NF;vT4dHfW6ldHnvckBCe3OjeR?= NEK4[4IyOCEQvF2= Mmf4NkBp MXHJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? MUSyNlIyODh5Nx?=
KMH-2 MWrGeY5kfGmxbjDBd5NigQ>? MkfZNVAh|ryP NWDTZXhQOiCq NYn3UlROUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u M{XhNVIzOjFyOEe3
L1236 MVjGeY5kfGmxbjDBd5NigQ>? NXXxW21YPSEQvF2= MmXVNlQhcA>? M1TtemJtd2OtczDz[YNz\XSrb36gc4YhfGinIFPDUFU> MmixNlIzOTB6N{e=
L591 Mki4SpVv[3Srb36gRZN{[Xl? MV21JO69VQ>? NX;1OHVCOjRiaB?= MnrDRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> M1;RRlIzOjFyOEe3
L1236 NIPSR5JCeG:ydH;zbZMhSXO|YYm= M3z1T|Uh|ryP NELhU4kzPCCq M{TKXWlv\HWldHnvckBw\iCjcH;weI9{cXN? NXG3[JBTOjJ{MUC4O|c>
L591 NHTQV|lCeG:ydH;zbZMhSXO|YYm= NWHOdIpuPSEQvF2= MnvwNlQhcA>? MWTJcoR2[3Srb36gc4Yh[XCxcITvd4l{ NV\VTGU{OjJ{MUC4O|c>
U-87MG NYfLZVBzTnWwY4Tpc44hSXO|YYm= MoPwNVAxKG6P NWnSemNOOjRiaB?= NH7QSoNFVVOR MYrJcohq[mm2aX;uJI9nKCClZXzsJI1q\3KjdHnvci=> M3vOfFIzODd7NkC5
SW1783 MXfGeY5kfGmxbjDBd5NigQ>? M2DBSVExOCCwTR?= NF3ab3UzPCCq NWDofXl[TE2VTx?= MlnwTY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> M37SflIzODd7NkC5
U-87MG MXfGeY5kfGmxbjDBd5NigQ>? NUHWcZlnPSEQvF2= NUnQWW9POjRiaB?= M3rVVGROW09? MlzsTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> MYOyNlA4QTZyOR?=
SW1783 MV7GeY5kfGmxbjDBd5NigQ>? NWLQbId6PSEQvF2= NFG0SoMzPCCq M2XBdWROW09? NX;QXYUzUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? NGHIeoUzOjB5OU[wPS=>
U-373MG MmDhSpVv[3Srb36gRZN{[Xl? NYfrUJNCPSEQvF2= MlX1NlQhcA>? M2fYeGROW09? M{fBXWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6 MknPNlIxPzl4MEm=
SK-MG3 NWXxSYgxTnWwY4Tpc44hSXO|YYm= MWW1JO69VQ>? M3zZOFI1KGh? NEL3[|JFVVOR NXTDUWdjUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? MnuxNlIxPzl4MEm=
SU-DHL-5 M4frZWZ2dmO2aX;uJGF{e2G7 NIrUXI0yKM7:TR?= M4jZNFI1KGh? NHTvW|ZFVVOR NHTlfZZKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| M1LBWFIxQTV7NkC2
WSU-NHL NHf0UY5HfW6ldHnvckBCe3OjeR?= M{nCPVEh|ryP NYrpbWVsOjRiaB?= NHPNV|VFVVOR NIrleY5KdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NVjTWHFNOjB7NUm2NFY>
CCRF-SB M{SxXWZ2dmO2aX;uJGF{e2G7 NYrNSFF7OSEQvF2= MV2yOEBp MkK5SG1UVw>? NX3jXotPUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= NWXDWGJbOjB7NUm2NFY>
INA-6 NYfWWJdbTnWwY4Tpc44hSXO|YYm= NEnhfG02KM7:TR?= M4DQUVYhcA>? NF2zV3BKdmirYnn0bY9vKG:oIGDJN2swSWu2IHHu[EBGWkticHH0bJdigQ>? NXHhXXpsOjB3MEWxOVg>
LB NFPDTo5HfW6ldHnvckBCe3OjeR?= M3HJUlUh|ryP MXO2JIg> NUnUSWs2UW6qaXLpeIlwdiCxZjDQTVRMN0GtdDDhcoQhTVKNIIDheIh4[Xl? M2Gwc|IxPTB3MUW4

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay
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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
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  • 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 (199.79 mM) warming
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
NCT02739360 Active, not recruiting Lymphoid Malignancies Gilead Sciences May 2016 Phase 4
NCT02787369 Not yet recruiting Recurrent Chronic Lymphoid Leukemia Dana-Farber Cancer Institute|Acetylon Pharmaceuticals Incorporated May 2016 Phase 1
NCT02662296 Recruiting Prolymphocytic Leukemia|Recurrent Chronic Lymphocytic Leukemia|Recurrent Non-Hodgkin Lymphoma|Recurrent Small Lymphocytic Lymphoma Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) March 2016 Phase 2
NCT02639910 Not yet recruiting Leukemia, Lymphocytic, Chronic, B-Cell|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma MorphoSys AG January 2016 Phase 2
NCT02590588 Recruiting Amyloidosis John Mark Sloan|Gilead Sciences|Boston Medical Center January 2016 Phase 2
NCT02536300 Recruiting Follicular Lymphoma Gilead Sciences January 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

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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