Idelalisib (CAL-101, GS-1101)

For research use only.

Catalog No.S2226

187 publications

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

CAS No. 870281-82-6

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. Idelalisib also stimulates autophagy.

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Selleck's Idelalisib (CAL-101, GS-1101) has been cited by 187 publications

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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. Idelalisib also stimulates autophagy.
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 MoXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzJSG1UVw>? NV\YTIJjUUN3ME2yNE41KM7:TR?= NWPFXmxjOjV7OUmzOVI>
CLL PBMCs MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDEUXNQ Mk\yTWM2OD1{Lkmgcm0> MUOyOVkyPzJ4Nx?=
U266 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXhOFAh|ryP M4f2OVQ5KGh? MnW4O|kvPSViaX7obYJqfGmxbjDyZZRm MoH2NlU{Ozl|M{K=
K562 NIfSXFJHfW6ldHnvckBCe3OjeR?= NHvYUlMyKM7:TR?= MmfsN{Bp NHTvNphKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= MUGyOVAyPDd5NR?=
K562 NVryeGJuTnWwY4Tpc44hSXO|YYm= MlzSNUDPxE1? MVqzJIg> NUXRZoFGUW6qaXLpeIlwdiCxZjDQO|BUPkticHjvd5Bpd3K7bHH0bY9v M1fyfVI2ODF2N{e1
K562 NIPZUoZHfW6ldHnvckBCe3OjeR?= M4nxSVEh|ryP M2\xe|MhcA>? M3;GeWlvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= MlnMNlUxOTR5N{W=
K562 NVvmV5NLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zVblEh|ryP NIDLWG04OiCq M2KzTmlvcGmkaYTpc44hd2ZicILvcIln\XKjdHnvci=> NIfCVpAzPTBzNEe3OS=>
Primary AML cell NVz5XmtxTnWwY4Tpc44hSXO|YYm= NGXKTmYyKM7:TR?= NHPRS5M{KGh? MUnJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NIHl[JozPTBzNEe3OS=>
Primary AML cell MkTzSpVv[3Srb36gRZN{[Xl? MVSxJO69VQ>? NUG3eFZqOyCq MnLlTY5pcWKrdHnvckBw\iCSN{DTOmsheGixc4Doc5J6dGG2aX;u NUjsbXZ2OjVyMUS3O|U>
Primary AML cell M4DmTWZ2dmO2aX;uJGF{e2G7 NYn6RYVEOSEQvF2= NUnVSldsOyCq NWrM[HRsUW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=> NGnlS|kzPTBzNEe3OS=>
Primary AML cell NUHmTWk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYexJO69VQ>? NWPvcIRsOyCq M3nndHN2eHC{ZYPzbY9vKG:oIILSUmEhe3mwdHjld4l{ NWfTeXVrOjVyMUS3O|U>
Microglia NYroZop6TnWwY4Tpc44hSXO|YYm= M{f6eVUh|ryP MlrzNVAhcA>? Mly5SG1UVw>? NVq2OIJCTGWlcnXhd4Uhd2ZiVF7GZUB{\WO{ZYTpc44h\nKxbTDMVHMue3SrbYXsZZRm\CBicEGxNO61TDlzMFGvSFkyOEFibXnjdo9odGmj M2L6cVI1PjJ3Nki0
Primary CLL cell MWXGeY5kfGmxbjDBd5NigQ>? NWXHXpRzOSEQvF2= MojONVUhdWmw NFLve25FVVOR MVTCcI9kc3NiQlPSMYlv\HWlZXSgUGNROSC|ZYLpcoUuPSCjY4TpeoF1cW:w NFXOZYozPDByOUKzNy=>
JEKO-1 NHvGPHJHfW6ldHnvckBCe3OjeR?= NWq5VJA5OSEQvF2= MYW3NkBp MnnrTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHnuJGloVS2|dHnteYxifGWmIFrFT28uOQ>? NITjO|UzOzN2MUW0NS=>
Granta-519 NVfCW|NPTnWwY4Tpc44hSXO|YYm= NHfSfZQyKM7:TR?= NXHN[pRvOiCq MVrJcohq[mm2aX;uJI9nKEGtdDj0N|A5MSCyaH;zdIhwenmuYYTpc44> NXz1eYU3OjN|NEG1OFE>
Granta-519 MW\GeY5kfGmxbjDBd5NigQ>? M4W4b|Eh|ryP MUmyJIg> MoPtTY5pcWKrdHnvckBw\iCDa4Sod|Q4OylicHjvd5Bpd3K7bHH0bY9v MWGyN|M1OTV2MR?=
JEKO-1 M1rSemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPiNVAh|ryP M3HS[VczKGh? NYXNZZRiUW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9vKHOuaXfoeIx6 NVnOZoJQOjN|NEG1OFE>
JEKO-1 NX7RT3VpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvCe|Z7PSEQvF2= Mmr5O|IhcA>? NYq3e|Vw\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? NEX2eFMzOzZ5NkKyNC=>
MAVER-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\MeZZxPSEQvF2= MVO3NkBp NYT6dIhw\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? NWPkUIltOjN4N{[yNlA>
MINO NV;ZWJJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUK1JO69VQ>? NXLJWnF1PzJiaB?= MVvkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz MXqyN|Y4PjJ{MB?=
SP53 NVXWS|F2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXj6WmllOC5zIN88US=> NVXoTlRjPzJiaB?= NUTjT4Rb\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? M1;FblI{Pjd4MkKw
HH NVS2bG5zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXoW|MyOCEQvF2= Mo\BO|IhcA>? NIjEc4VFVVOR NYX1doRxUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDzcIlocHSueR?= M161SVIzQDBzOUW5
Myla NVvsNWNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33vflExKM7:TR?= M3:3UFczKGh? MkLrSG1UVw>? NVPEd4Jw\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> MonVNlI5ODF7NUm=
SR786 NILFTJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7pNVAh|ryP NFG0b4c4OiCq MnHqSG1UVw>? M2XyZYRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= M2\LflIzQDBzOUW5
HuT78 NX7RfJVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWCxNEDPxE1? MXK3NkBp MY\EUXNQ MWDkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| NUDafnNIOjJ6MEG5OVk>
MJ NYXBZpBLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PiXVExKM7:TR?= MVW3NkBp NEHISJFFVVOR MmnX[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= MX2yNlgxOTl3OR?=
DERL7 NXW5fFNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfIcZRsOTBizszN MYq3NkBp MoK3SG1UVw>? NXGzNJUx\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> NXnCfmxqOjJ6MEG5OVk>
L1236 NXLJTWNJTnWwY4Tpc44hSXO|YYm= NEfEOpYyOCEQvF2= NGTPd5AzKGh? MoDsTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NITEWFkzOjJzMEi3Oy=>
L428 NF\W[YpHfW6ldHnvckBCe3OjeR?= Mn74NVAh|ryP MXSyJIg> MXrJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NU\IVYNCOjJ{MUC4O|c>
L591 MoP5SpVv[3Srb36gRZN{[Xl? NY\4[JFYOTBizszN NUX3ZVJ4OiCq NV3hWol1UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u MojxNlIzOTB6N{e=
KMH-2 NWP3d|hpTnWwY4Tpc44hSXO|YYm= MUmxNEDPxE1? MljkNkBp MnL6TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w M2O1blIzOjFyOEe3
L1236 MlPYSpVv[3Srb36gRZN{[Xl? MUS1JO69VQ>? NIDxZ|czPCCq NELvfZRDdG:la4Ogd4VkemW2aX;uJI9nKHSqZTDDR2w2 MV2yNlIyODh5Nx?=
L591 NHHBfI5HfW6ldHnvckBCe3OjeR?= M1W3VFUh|ryP MVKyOEBp NYPDem1qSmyxY3vzJJNm[3KndHnvckBw\iC2aHWgR2NNPQ>? NWjvOpBMOjJ{MUC4O|c>
L1236 NWLSNnZpSXCxcITvd4l{KEG|c3H5 NWjNU|A2PSEQvF2= M4iyOVI1KGh? NUf3ZmhOUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= M2GxeVIzOjFyOEe3
L591 MlnYRZBweHSxc3nzJGF{e2G7 M1LLdlUh|ryP MX6yOEBp NWPJfHBEUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= M1;mWlIzOjFyOEe3
U-87MG MkPRSpVv[3Srb36gRZN{[Xl? M4TScFExOCCwTR?= M{LNU|I1KGh? NW\DTnh[TE2VTx?= MnPtTY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> M2q3fVIzODd7NkC5
SW1783 NGLnU|hHfW6ldHnvckBCe3OjeR?= M37HNFExOCCwTR?= NUnyNXZ5OjRiaB?= NIHWeINFVVOR NVqyXoZiUW6qaXLpeIlwdiCxZjCgZ4VtdCCvaXfyZZRqd25? M3qw[|IzODd7NkC5
U-87MG MnfiSpVv[3Srb36gRZN{[Xl? NHezVG42KM7:TR?= MmrYNlQhcA>? NECyOItFVVOR NHLLWWdKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? M4rsS|IzODd7NkC5
SW1783 M33vbGZ2dmO2aX;uJGF{e2G7 M3HQUVUh|ryP NETWPVYzPCCq MnvFSG1UVw>? MnLZTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> MnfzNlIxPzl4MEm=
U-373MG M1PkVmZ2dmO2aX;uJGF{e2G7 NUXFcVdlPSEQvF2= NI\1OVUzPCCq NIXHbmZFVVOR M{fpdmlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6 M3HyeFIzODd7NkC5
SK-MG3 NG\nTYNHfW6ldHnvckBCe3OjeR?= NIPCTmg2KM7:TR?= NFf6PZczPCCq MnPSSG1UVw>? MoXlTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NIDQTYIzOjB5OU[wPS=>
SU-DHL-5 M2HJOGZ2dmO2aX;uJGF{e2G7 MXOxJO69VQ>? MnL4NlQhcA>? MmDoSG1UVw>? M2\SVmlv\HWldHnvckBw\iCjcH;weI9{cXN? M2PWR|IxQTV7NkC2
WSU-NHL MVnGeY5kfGmxbjDBd5NigQ>? MVSxJO69VQ>? MUWyOEBp Mmq4SG1UVw>? MnzUTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? NEPC[owzODl3OU[wOi=>
CCRF-SB NED3Z5pHfW6ldHnvckBCe3OjeR?= NGC5fIoyKM7:TR?= M1LRXVI1KGh? NXfrVWtITE2VTx?= NUHuZ2FMUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= MmnONlA6PTl4ME[=
INA-6 NEDHNIJHfW6ldHnvckBCe3OjeR?= Mn6wOUDPxE1? MVy2JIg> MljhTY5pcWKrdHnvckBw\iCSSUPLM2FsfCCjbnSgSXJMKHCjdHj3ZZk> M4XhfFIxPTB3MUW4
LB MljYSpVv[3Srb36gRZN{[Xl? NWX4e2l6PSEQvF2= M1LGeVYhcA>? MW\Jcohq[mm2aX;uJI9nKFCLNFuvRYt1KGGwZDDFVmsheGG2aIfhfS=> MVWyNFUxPTF3OB?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PUMA / p53 ; 

PubMed: 28008149     


Parental and p53-KD HCT116 cells were treated with 10 μmol/L idelalisib for 24 hours. PUMA expression was analyzed by Western blotting.

Bim / Bcl-xl / Bid / Mcl-1; 

PubMed: 28008149     


HCT116 cells treated with 10 μmol/L idelalisib at indicated time point. The expression of indicated Bcl-2 family members was analyzed by Western blotting.

p-p65; 

PubMed: 28008149     


HCT116 cells were treated with 10 μmol/L idelalisib at indicated time point. p-p65 (S536) and p65 expression was analyzed by Western blotting.

p-AKT / AKT; 

PubMed: 28008149     


HCT116 cells were treated with 10 μmol/L idelalisib at indicated time point. Total AKT and p-AKT expression was analyzed Western blotting.

Cleaved caspase 3 / Cleaved caspase 9; 

PubMed: 28008149     


HepG2 cells were treated with 5μmol/L idelalisib at indicated time point. Cleaved-caspase 3 and 9 were analyzed by western blotting.

Mcl-1 / Bcl-2 / Bid / Bcl-xl / Noxa / Bak / Bax ; 

PubMed: 30224718     


HepG2 cells were treated with 5 μmol/L idelalisib at indicated time points. The expression of indicated Bcl-2 family members was analyzed by western blotting and normalized to β-actin. The data represent the mean ± SD of three independent experiments. **P < 0.01 (one-way ANOVA with Tukey’s post hoc test).

p-FoxO3a / FoxO3a; 

PubMed: 30224718     


HepG2 cells were treated with 5 μmol/L idelalisib for 24 h. Indicated protein expression was analyzed by western blotting and p-FoxO3a normalized to FoxO3a, p-AKT normalized to AKT. The data represent the mean ± SD of three independent experiments. **P < 0.01 (one-way ANOVA with Tukey’s post hoc test). 

Akt(T308) / PDK1(S241) / GSK-3β(S9); 

PubMed: 27342398     


JeKo-1, Mino, and Granta 519 cells or cells from four different MCL patients were serum-starved for 1h and then treated with DMSO, or with 0.5, 1, or 3μM for 1h; the cells were then co-cultured with IgM (10ng/μL) for 15min before harvesting. Cell extracts were prepared, and 30μg (cell lines) or 50μg (primary cells) protein was loaded for immunoblot analyses. The effects of idelalisib on Akt (Thr308) and total Akt, PDK1 (Ser241) and total PDK1, GS3K-3β (Ser9) and total GSK-3β protein expression levels were detected in (A) JeKo-1, Mino and Granta 519 cells.

28008149 30224718 27342398
Growth inhibition assay
Cell viability; 

PubMed: 28008149     


Indicated cell lines were treated with different concentrations of idelalisib for 72 hours. Cell proliferation was determined by MTS assay. Results were expressed as means ± SD of three independent experiments.

Cell viability; 

PubMed: 30224718     


The indicated cell lines were treated with increasing concentrations of idelalisib for 72 h. Cell viability was determined by MTS assay.

28008149 30224718

Protocol

Kinase Assay:[2]
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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:[2]
- Collapse
  • 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):
2% DMSO+20%PEG 300+ddH2O
For best results, use promptly after mixing.
5mg/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
Smiles CCC(C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03582098 Completed Drug: Idelalisib|Drug: Rituximab Chronic Lymphocytic Leukaemia Gilead Sciences September 12 2018 --
NCT03151057 Active not recruiting Drug: Idelalisib 100 MG|Drug: Placebo Oral Tablet B Cells-Tumors|B Cell Chronic Lymphocytic Leukemia|Follicular Lymphoma|Mantle Cell Lymphoma|Large B-Cell Diffuse Lymphoma of Bone (Diagnosis) Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Gilead Sciences July 31 2018 Phase 1
NCT03568929 Recruiting Drug: Idelalisib Follicular Non-Hodgkin''s Lymphoma Refractory Gilead Sciences May 25 2018 --

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID