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 NWXhO3R6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\ZTWROW09? M4PCOGlEPTB;MkCuOEDPxE1? MWGyOVk6QTN3Mh?=
CLL PBMCs Mke0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXKSG1UVw>? M1PoPWlEPTB;Mj65JI5O M2HmW|I2QTF5Mk[3
U266 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjoTGh5PDBizszN MlS2OFghcA>? NFfyO484QS53JTDpcohq[mm2aX;uJJJifGV? NXTtRXdSOjV|M{mzN|I>
K562 MknRSpVv[3Srb36gRZN{[Xl? NWDFTFQ3OSEQvF2= M1X6flMhcA>? NFLMVXFKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= MX:yOVAyPDd5NR?=
K562 M2j0cWZ2dmO2aX;uJGF{e2G7 NXPZXYY2OSEQvF2= NY\5Soh{OyCq NH3JVWZKdmirYnn0bY9vKG:oIGC3NHM3UyCyaH;zdIhwenmuYYTpc44> MViyOVAyPDd5NR?=
K562 NWTxS|VtTnWwY4Tpc44hSXO|YYm= NXu4PJM{OSEQvF2= NUHBfVdPOyCq M3f0OGlvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= NIfzfXYzPTBzNEe3OS=>
K562 M4LIS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInibY0yKM7:TR?= NHPJPVM4OiCq NU\O[WlyUW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9v MYKyOVAyPDd5NR?=
Primary AML cell NXqzNWZmTnWwY4Tpc44hSXO|YYm= NFn3W2MyKM7:TR?= M3fGcFMhcA>? Mn;OTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w M1jBR|I2ODF2N{e1
Primary AML cell NW\wUGY3TnWwY4Tpc44hSXO|YYm= NIjHWFcyKM7:TR?= NYDOeHhjOyCq M3fwb2lvcGmkaYTpc44hd2ZiUEewV|ZMKHCqb4PwbI9zgWyjdHnvci=> MXeyOVAyPDd5NR?=
Primary AML cell MX\GeY5kfGmxbjDBd5NigQ>? M4DaVlEh|ryP NWnONGtwOyCq M1;a[WlvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= MlnNNlUxOTR5N{W=
Primary AML cell M1fFR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF:5XocyKM7:TR?= NFjGfZU{KGh? M4fRcXN2eHC{ZYPzbY9vKG:oIILSUmEhe3mwdHjld4l{ NWLBSItxOjVyMUS3O|U>
Microglia M1TMZmZ2dmO2aX;uJGF{e2G7 Mn7aOUDPxE1? MVqxNEBp NXG5R5A2TE2VTx?= MkSxSIVkemWjc3Wgc4YhXE6IYTDz[YNz\XSrb36g[pJwdSCOUGOtd5RqdXWuYYTl[EAheDFzMN80SFkyOEFxREmxNGEhdWmlcn;ncIli NGHo[2szPDZ{NU[4OC=>
Primary CLL cell M2fsPWZ2dmO2aX;uJGF{e2G7 NEXk[FEyKM7:TR?= MWWxOUBucW5? NX7sUYZiTE2VTx?= NH\1Oo5DdG:la4OgRmNTNWmwZIXj[YQhVEOSMTDz[ZJqdmVvNTDhZ5RqfmG2aX;u Mnn4NlQxODl{M{O=
JEKO-1 NGDwNXhHfW6ldHnvckBCe3OjeR?= NI\5UmUyKM7:TR?= MojsO|IhcA>? NGrpcoJKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gbY4hUWePLYP0bY12dGG2ZXSgTmVMVy1z MVqyN|M1OTV2MR?=
Granta-519 MknPSpVv[3Srb36gRZN{[Xl? MVexJO69VQ>? M{TkOFIhcA>? NXfnbVBDUW6qaXLpeIlwdiCxZjDBb5QpfDNyODmgdIhwe3Cqb4L5cIF1cW:w MYCyN|M1OTV2MR?=
Granta-519 MVPGeY5kfGmxbjDBd5NigQ>? MVSxJO69VQ>? MWKyJIg> NXu2N3hUUW6qaXLpeIlwdiCxZjDBb5QpezR5MzmgdIhwe3Cqb4L5cIF1cW:w MYiyN|M1OTV2MR?=
JEKO-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1H4OFExKM7:TR?= NHPWdFk4OiCq MWLJcohq[mm2aX;uJI9nKHC{b3zp[oVz[XSrb36gd4xq\2i2bIm= NUPrOWtDOjN|NEG1OFE>
JEKO-1 M3vyWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fSdlUh|ryP NGXFd484OiCq MoPO[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> NHTFR3QzOzZ5NkKyNC=>
MAVER-1 NF;1b2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX21JO69VQ>? MUW3NkBp Ml7j[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> MoD5NlM3PzZ{MkC=
MINO MmjRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXu1JO69VQ>? NXjVUWVlPzJiaB?= M2TNTYRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> NU\HWJl{OjN4N{[yNlA>
SP53 NIDJVlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUSwMlEh|ryP M3K2ZVczKGh? MVPkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz M3TCb|I{Pjd4MkKw
HH MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWWxNEDPxE1? NUDyPW9TPzJiaB?= M2K3ZWROW09? M{L0eWlv\HWldHnvckBw\iCjcH;weI9{cXNic3zp[4h1dHl? NFe1c3AzOjhyMUm1PS=>
Myla MkC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PX[VExKM7:TR?= Mnn1O|IhcA>? M2qzZmROW09? NUTa[odK\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> NXXnV3l1OjJ6MEG5OVk>
SR786 MlrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLRNVAh|ryP NWW5VYFrPzJiaB?= MnjmSG1UVw>? MXnkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MX[yNlgxOTl3OR?=
HuT78 Mn;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfpUIIyOCEQvF2= NUfae4VjPzJiaB?= M1j0emROW09? MXzkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| NYDNcIo3OjJ6MEG5OVk>
MJ M3XhSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\RNVAh|ryP MYK3NkBp Ml7ySG1UVw>? MXHkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MoTkNlI5ODF7NUm=
DERL7 M1HEeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn4WGhPOTBizszN Mm\BO|IhcA>? NWjHe|BDTE2VTx?= NHzpSHlld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MnrINlI5ODF7NUm=
L1236 NHKyfFNHfW6ldHnvckBCe3OjeR?= NFXud4kyOCEQvF2= NYiwd45mOiCq NITle2JKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= NXTVTGFDOjJ{MUC4O|c>
L428 NV3XOog5TnWwY4Tpc44hSXO|YYm= M{Lm[lExKM7:TR?= NVTscpZpOiCq NFfqRZJKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= M{T4VVIzOjFyOEe3
L591 MorsSpVv[3Srb36gRZN{[Xl? NGSwW|MyOCEQvF2= M3SxXVIhcA>? NWjISWRvUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u MnroNlIzOTB6N{e=
KMH-2 NELPRVlHfW6ldHnvckBCe3OjeR?= NFH4NFkyOCEQvF2= NVnzNFZtOiCq MXLJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NWCyOIVGOjJ{MUC4O|c>
L1236 M1rZXGZ2dmO2aX;uJGF{e2G7 NIP3eHo2KM7:TR?= MlW1NlQhcA>? Ml3pRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> NEXGeJUzOjJzMEi3Oy=>
L591 MUjGeY5kfGmxbjDBd5NigQ>? MlfwOUDPxE1? NGXVcIUzPCCq NGTGdFlDdG:la4Ogd4VkemW2aX;uJI9nKHSqZTDDR2w2 NIi0SGszOjJzMEi3Oy=>
L1236 MnTqRZBweHSxc3nzJGF{e2G7 Ml;mOUDPxE1? MmTKNlQhcA>? M3zs[Glv\HWldHnvckBw\iCjcH;weI9{cXN? NYHpZ2prOjJ{MUC4O|c>
L591 Mn\zRZBweHSxc3nzJGF{e2G7 M4LmTFUh|ryP MWiyOEBp MnjMTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? M1jJOFIzOjFyOEe3
U-87MG NVLBdFFLTnWwY4Tpc44hSXO|YYm= M2HITlExOCCwTR?= MVWyOEBp NXSwfoJETE2VTx?= MlG2TY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> M1PIcFIzODd7NkC5
SW1783 MWDGeY5kfGmxbjDBd5NigQ>? M1vNSFExOCCwTR?= M{PjblI1KGh? M2fP[WROW09? NFvUVplKdmirYnn0bY9vKG:oIDDj[YxtKG2rZ4LheIlwdg>? MVSyNlA4QTZyOR?=
U-87MG M4nldWZ2dmO2aX;uJGF{e2G7 M{TKU|Uh|ryP NHe0O2EzPCCq NYHkeZQ{TE2VTx?= MULJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> M1jt[|IzODd7NkC5
SW1783 MmPvSpVv[3Srb36gRZN{[Xl? MYm1JO69VQ>? Mm\JNlQhcA>? NVPDUFFyTE2VTx?= M1PqRmlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6 M{SyfFIzODd7NkC5
U-373MG MkOxSpVv[3Srb36gRZN{[Xl? MlzMOUDPxE1? NUjIOFVUOjRiaB?= NEjF[GxFVVOR MmHZTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NGnO[ZIzOjB5OU[wPS=>
SK-MG3 MnHjSpVv[3Srb36gRZN{[Xl? NGjLeoU2KM7:TR?= NXjhSm1ZOjRiaB?= M1;yVGROW09? MkjvTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NUOxdGxEOjJyN{m2NFk>
SU-DHL-5 M{n0PGZ2dmO2aX;uJGF{e2G7 MnzFNUDPxE1? M2LZcVI1KGh? M{X2dWROW09? NXi3Wmx{UW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= MUCyNFk2QTZyNh?=
WSU-NHL NIe1WFRHfW6ldHnvckBCe3OjeR?= M4HI[|Eh|ryP NXrmWWhDOjRiaB?= MUjEUXNQ MX;JcoR2[3Srb36gc4Yh[XCxcITvd4l{ M3rUOVIxQTV7NkC2
CCRF-SB NEG1fHdHfW6ldHnvckBCe3OjeR?= NYXsXXdvOSEQvF2= NH7BZXgzPCCq NX\Hc3VMTE2VTx?= M1uzc2lv\HWldHnvckBw\iCjcH;weI9{cXN? NGHONHUzODl3OU[wOi=>
INA-6 MUTGeY5kfGmxbjDBd5NigQ>? Mk\HOUDPxE1? NGfWU3c3KGh? MVPJcohq[mm2aX;uJI9nKFCLM1uvRYt1KGGwZDDFVmsheGG2aIfhfS=> NYnyOHBlOjB3MEWxOVg>
LB MVnGeY5kfGmxbjDBd5NigQ>? MWm1JO69VQ>? NXLKSVJIPiCq NVrudXN2UW6qaXLpeIlwdiCxZjDQTVRMN0GtdDDhcoQhTVKNIIDheIh4[Xl? MW[yNFUxPTF3OB?=

... 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
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. https://www.ncbi.nlm.nih.gov/pubmed/24625684

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID