Idelalisib (CAL-101, GS-1101)

For research use only.

Catalog No.S2226

192 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 192 publications

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. 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 MkD4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTEUXNQ NHi4SVBKSzVyPUKwMlQh|ryP M4f0[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUm5N|UzLz5{NUm5PVM2OjxxYU6=
CLL PBMCs M2DuUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;4N5pFVVOR NIDMT|dKSzVyPUKuPUBvVQ>? M4LKflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUG3NlY4Lz5{NUmxO|I3PzxxYU6=
U266 NYqyUoVwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHj3WpU1OCEQvF2= MWq0PEBp NFHNOHQ4QS53JTDpcohq[mm2aX;uJJJifGV? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN|OUOzNkc,OjV|M{mzN|I9N2F-
K562 MmrTSpVv[3Srb36gRZN{[Xl? NGrtUXcyKM7:TR?= NUPtTG1MOyCq NFmyOo1KdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= NWXQPI9zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
K562 MknBSpVv[3Srb36gRZN{[Xl? MXexJO69VQ>? NX;WR|BIOyCq NYrVXJJxUW6qaXLpeIlwdiCxZjDQO|BUPkticHjvd5Bpd3K7bHH0bY9v M3nIZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
K562 MkTDSpVv[3Srb36gRZN{[Xl? MV2xJO69VQ>? M4K3[FMhcA>? Mnm3TY5pcWKrdHnvckBw\iCJU1uzJJBpd3OyaH;yfYxifGmxbh?= NV3KNo9uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
K562 NVu2ZYljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVS5fmx3OSEQvF2= MVG3NkBp NG[5PXNKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44> NHzuT249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Primary AML cell NVq0cJp{TnWwY4Tpc44hSXO|YYm= MoXDNUDPxE1? MlT2N{Bp MVrJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? M2rrPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Primary AML cell Mn3hSpVv[3Srb36gRZN{[Xl? MUWxJO69VQ>? NWK3cHF4OyCq NGqw[3NKdmirYnn0bY9vKG:oIGC3NHM3UyCyaH;zdIhwenmuYYTpc44> M1OxNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Primary AML cell NH;zcWRHfW6ldHnvckBCe3OjeR?= NVzEVot1OSEQvF2= MoKzN{Bp NFSyd4xKdmirYnn0bY9vKG:oIFfTT|MheGixc4Doc5J6dGG2aX;u MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTBzNEe3OUc,OjVyMUS3O|U9N2F-
Primary AML cell MoDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nrW|Eh|ryP NXT2U|JiOyCq M3GzOHN2eHC{ZYPzbY9vKG:oIILSUmEhe3mwdHjld4l{ MlXSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUS3O|UoRjJ3MEG0O|c2RC:jPh?=
Microglia NFvHPFhHfW6ldHnvckBCe3OjeR?= NXLVXW1SPSEQvF2= NFq5V3oyOCCq NXPyOG9HTE2VTx?= Mkn6SIVkemWjc3Wgc4YhXE6IYTDz[YNz\XSrb36g[pJwdSCOUGOtd5RqdXWuYYTl[EAheDFzMN80SFkyOEFxREmxNGEhdWmlcn;ncIli NX71OGtSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NlU3QDRpPkK0OlI2Pjh2PD;hQi=>
Primary CLL cell NGDkcmRHfW6ldHnvckBCe3OjeR?= M1zxOVEh|ryP Mm\YNVUhdWmw MoDYSG1UVw>? MYjCcI9kc3NiQlPSMYlv\HWlZXSgUGNROSC|ZYLpcoUuPSCjY4TpeoF1cW:w MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUKzN{c,OjRyMEmyN|M9N2F-
JEKO-1 MXzGeY5kfGmxbjDBd5NigQ>? MlfyNUDPxE1? NY\GeWtlPzJiaB?= MmDDTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHnuJGloVS2|dHnteYxifGWmIFrFT28uOQ>? NV7zTIg{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOFE2PDFpPkKzN|QyPTRzPD;hQi=>
Granta-519 NV3P[o5YTnWwY4Tpc44hSXO|YYm= NYXN[Zo{OSEQvF2= MWmyJIg> MUTJcohq[mm2aX;uJI9nKEGtdDj0N|A5MSCyaH;zdIhwenmuYYTpc44> NGPsWlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O0NVU1OSd-MkOzOFE2PDF:L3G+
Granta-519 NEXaVmJHfW6ldHnvckBCe3OjeR?= NIjheXIyKM7:TR?= M{fpSFIhcA>? MX\Jcohq[mm2aX;uJI9nKEGtdDjzOFc{MSCyaH;zdIhwenmuYYTpc44> NVjxWpRlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOFE2PDFpPkKzN|QyPTRzPD;hQi=>
JEKO-1 NX;vXGI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYCxNEDPxE1? M3f5cVczKGh? M1vrZWlvcGmkaYTpc44hd2ZicILvcIln\XKjdHnvckB{dGmpaITsfS=> NF7CNVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O0NVU1OSd-MkOzOFE2PDF:L3G+
JEKO-1 NE\1botIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HqT|Uh|ryP NInrbJc4OiCq NUPvfG9k\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? NYqwSndVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2O|YzOjBpPkKzOlc3OjJyPD;hQi=>
MAVER-1 NVvHTY5ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7VcoVzPSEQvF2= MoLPO|IhcA>? NF\h[m5ld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5NkKyNEc,OjN4N{[yNlA9N2F-
MINO NHXYXHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVe1JO69VQ>? M3HXSFczKGh? NVLPXYhG\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? M3XuclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nke2NlIxLz5{M{[3OlIzODxxYU6=
SP53 NWjLdYR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonnNE4yKM7:TR?= NUfaSndoPzJiaB?= MYXkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz NGjLZ3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[3OlIzOCd-MkO2O|YzOjB:L3G+
HH M3j3NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vLXVExKM7:TR?= MV[3NkBp MWLEUXNQ NID2SoZKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IIPsbYdpfGy7 MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyMUm1PUc,OjJ6MEG5OVk9N2F-
Myla NH3nbIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUCxNEDPxE1? MlPMO|IhcA>? NHPm[WJFVVOR NWDQU5Qy\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> M2H4SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OECxPVU6Lz5{MkiwNVk2QTxxYU6=
SR786 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjNWnQyOCEQvF2= MoHZO|IhcA>? M3j5WGROW09? MkfF[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyMUm1PUc,OjJ6MEG5OVk9N2F-
HuT78 NHnTSY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXyxNEDPxE1? MW[3NkBp NHLtU5NFVVOR NYPTWmVO\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyMUm1PUc,OjJ6MEG5OVk9N2F-
MJ MkTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrDdFB{OTBizszN NXjNTlk{PzJiaB?= MVrEUXNQ NY\0dlg2\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> MkPvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
DERL7 MlzxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXHNVAh|ryP M1j6OlczKGh? NYj3bHZLTE2VTx?= Mo[1[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= M4fWclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OECxPVU6Lz5{MkiwNVk2QTxxYU6=
L1236 NIjUVGZHfW6ldHnvckBCe3OjeR?= M3jue|ExKM7:TR?= MVSyJIg> NYnDSlJwUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u NYjvRYlORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNVA5PzdpPkKyNlExQDd5PD;hQi=>
L428 NXTiU41TTnWwY4Tpc44hSXO|YYm= NUDCT4pQOTBizszN NXXoOI17OiCq M2L5c2lvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= Mn3WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
L591 Ml:zSpVv[3Srb36gRZN{[Xl? MlXjNVAh|ryP NYX2dVBCOiCq MoXwTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w M4XDclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
KMH-2 Mn3FSpVv[3Srb36gRZN{[Xl? NVG5T|dQOTBizszN MoPvNkBp NX:4SpFYUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u M3\xe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
L1236 NYGzVI45TnWwY4Tpc44hSXO|YYm= M3LJV|Uh|ryP M3\RU|I1KGh? M1y3OmJtd2OtczDz[YNz\XSrb36gc4YhfGinIFPDUFU> NGLucYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKxNFg4Pyd-MkKyNVA5Pzd:L3G+
L591 M{LWVGZ2dmO2aX;uJGF{e2G7 M1zacFUh|ryP M{nJcVI1KGh? NYnGRm9GSmyxY3vzJJNm[3KndHnvckBw\iC2aHWgR2NNPQ>? MlHHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
L1236 NIjpNGtCeG:ydH;zbZMhSXO|YYm= NYTNUFRoPSEQvF2= MlTvNlQhcA>? NWHqeWZnUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L591 M2XsOWFxd3C2b4Ppd{BCe3OjeR?= NWjtd3I{PSEQvF2= NFTWVZQzPCCq MUjJcoR2[3Srb36gc4Yh[XCxcITvd4l{ MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
U-87MG MoTOSpVv[3Srb36gRZN{[Xl? NUXy[HNzOTByIH7N M1L1XFI1KGh? NHPVTI5FVVOR MVXJcohq[mm2aX;uJI9nKCClZXzsJI1q\3KjdHnvci=> M2nFUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEe5OlA6Lz5{MkC3PVYxQTxxYU6=
SW1783 MonoSpVv[3Srb36gRZN{[Xl? NXLsO5NHOTByIH7N NHziZm8zPCCq NYrKfIhrTE2VTx?= MnXGTY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
U-87MG NXvP[oE2TnWwY4Tpc44hSXO|YYm= MX61JO69VQ>? NYm2TlBzOjRiaB?= MWrEUXNQ NWDKfopLUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
SW1783 M33iSmZ2dmO2aX;uJGF{e2G7 NFPCcJA2KM7:TR?= M3\E[VI1KGh? M4TVOmROW09? NXLLbpZKUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? Mnj4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{m2NFkoRjJ{MEe5OlA6RC:jPh?=
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SK-MG3 NHfGSVdHfW6ldHnvckBCe3OjeR?= NH23XIs2KM7:TR?= MUWyOEBp NXLMfIZqTE2VTx?= MnmyTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
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LAN-5 NGK0NoNyUFSVIHHzd4F6 NGS0fY5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO= Mkm2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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RPMI8226 MV7BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M1r1fFczKGi{cx?= MoH4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUUF3JPFIzPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gOU41QSEQvF2u MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV|NEmzOkc,Ojl3M{S5N|Y9N2F-
Raji NWm3TppTSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NGraRVg4OiCqcoO= MnS2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUYXrpJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB7Lkm1JO69VS5? M3foWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUO0PVM3Lz5{OUWzOFk{PjxxYU6=
SU-DHL6 MlzSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlfQS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gV3UuTEiONjDj[YxteyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBIUTVyIE2gNE4xPDJizszNMi=> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZyMUm5NUc,Ojl4MEG5PVE9N2F-
MOLM13 MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGXMPYo4OiCqcoO= MXrHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNU2xOOTNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZZN{[XluIFfJOVAhRSBzLkeg{txONg>? M3vFPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEWzO|IyLz5|MEC1N|czOTxxYU6=
MOLM14 MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIC3fHk4OiCqcoO= NHuyNoRIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOV0yPMUSgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[XO|YYmsJGdKPTBiPTC2MlQh|ryPLh?= NVvofIVtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwOVM4OjFpPkOwNFU{PzJzPD;hQi=>
MOLM14 MYLBcpRqfHWvb4KgZZN{[Xl? MmjaNVAxKG2pL3vn NEjqZZgyPCCmYYnz M1iwTWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUG0yPCClZXzsd{B5\W6xZ4Lh[pRm\CCrbjDueU9vfSCvb4Xz[UBie3Onc4Pl[EBieyC2dX3vdkBoem:5dHigbY5pcWKrdHnvckBifCBzMECgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCmYXnsfUB3cWFiZ3H2ZYdmKGSxc3XkJIZweiBzNDDkZZl{KGGwZDDt[YF{fXKnZDDkZYltgSCmdYLpcoch[2:vcH;1coQh\G:|aX7nJJJmdGG2aY\lJJRwKGOxboTyc4w> NWm1Z|BIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwOVM4OjFpPkOwNFU{PzJzPD;hQi=>
MOLM14 NXvQdW5wSW62aYT1cY9zKGG|c3H5 M1y4d|ExOCCvZz;r[y=> NH3KNYMyPCCmYYnz MWPBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVQh[2WubIOgfIVvd2e{YX\0[YQhcW5iboWvcpUhdW:3c3WgZZN{\XO|ZXSgZZMhcW6mdXP0bY9vKG:oIHHwc5B1d3OrczDheEAyODBibXevb4ctKHCxIHHkcYlvcXO2ZYLl[EBl[WmueTD2bYEh\2G4YXflJIRwe2WmIH\vdkAyPCCmYYnzJIFv\CCvZXHzeZJm\CCmYXnsfUBlfXKrbnegZ49ueG:3bnSg[I9{cW6pIHL5JHRWVkWOIHLhd4VlKGG|c3H5 MmTLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByNUO3NlEoRjNyMEWzO|IyRC:jPh?=
MOLM14 M2nKRmFvfGm2dX3vdkBie3OjeR?= MkK5NVAxKG2pL3vn M1\ac|E1KGSjeYO= MVXBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVQh[2WubIOgfIVvd2e{YX\0[YQhcW5iboWvcpUhdW:3c3WgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD0eY1weiCycn;sbYZmemG2aX;uJFExOCCvZz;r[{wheG9iYXTtbY5qe3SncnXkJIRicWy7II\pZUBo[X[jZ3Wg[I9{\WRiZn;yJFE1KGSjeYOgZY5lKG2nYYP1doVlKGSjaXz5JIR2emmwZzDjc41xd3WwZDDkc5NqdmdiYomgT4kuPjdibHHi[YxtcW6pIHLhd4VlKGmvbYXuc4g> NI\afGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC1N|czOSd-M{CwOVM4OjF:L3G+

... 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]
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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 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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