Idelalisib (CAL-101, GS-1101)

Catalog No.S2226

For research use only.

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.

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

CAS No. 870281-82-6

Selleck's Idelalisib (CAL-101, GS-1101) has been cited by 222 publications

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. 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 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13ObWROW09? NVnOU5BZUUN3ME2yNE41KM7:TR?= NU\kTVg4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5PVk{PTJpPkK1PVk6OzV{PD;hQi=>
CLL PBMCs MnPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXmSVdFVVOR NIq1TG1KSzVyPUKuPUBvVQ>? NXKyd5BzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5NVczPjdpPkK1PVE4OjZ5PD;hQi=>
U266 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXO0NEDPxE1? MkHoOFghcA>? Mny2O|kvPSViaX7obYJqfGmxbjDyZZRm M4G5d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{O5N|MzLz5{NUOzPVM{OjxxYU6=
K562 M1i1eWZ2dmO2aX;uJGF{e2G7 MmXSNUDPxE1? NWjMdFJbOyCq Mo\XTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NFXidog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
K562 M4niPWZ2dmO2aX;uJGF{e2G7 NV\HWVFjOSEQvF2= MY[zJIg> NGjrdXFKdmirYnn0bY9vKG:oIGC3NHM3UyCyaH;zdIhwenmuYYTpc44> NHOzSlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
K562 M3H3dGZ2dmO2aX;uJGF{e2G7 NFnl[G0yKM7:TR?= NUjTWYlFOyCq M{XIc2lvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTBzNEe3OUc,OjVyMUS3O|U9N2F-
K562 NVX2WGRvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LzZ|Eh|ryP M4L4WVczKGh? NWDUdllJUW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9v MkLlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUS3O|UoRjJ3MEG0O|c2RC:jPh?=
Primary AML cell NIW3[4xHfW6ldHnvckBCe3OjeR?= MUWxJO69VQ>? NEnVelI{KGh? NXXoWms1UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u NEPwU4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Primary AML cell MXfGeY5kfGmxbjDBd5NigQ>? NEHqZZAyKM7:TR?= MYGzJIg> MXTJcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:|cHjvdplt[XSrb36= MluwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUS3O|UoRjJ3MEG0O|c2RC:jPh?=
Primary AML cell M33LcmZ2dmO2aX;uJGF{e2G7 NUnqOIQ2OSEQvF2= NU\qSFdtOyCq M1nUbWlvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= NG\qO4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Primary AML cell NUjlPWpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjXUYwyOSEQvF2= NHi2XZM{KGh? NFG1VYhUfXCycnXzd4lwdiCxZjDyVm5CKHO7boTo[ZNqew>? NETsT4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Microglia MVTGeY5kfGmxbjDBd5NigQ>? NET6e2U2KM7:TR?= MVKxNEBp M4[3U2ROW09? M1z0fGRm[3KnYYPlJI9nKFSQRnGgd4VkemW2aX;uJIZzd21iTGDTMZN1cW23bHH0[YQhKHBzMUFOuGQ6OTCDL1S5NVBCKG2rY4Lv[4xq[Q>? NYn2XIc4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NlU3QDRpPkK0OlI2Pjh2PD;hQi=>
Primary CLL cell NHvDWFBHfW6ldHnvckBCe3OjeR?= NYDLcnNEOSEQvF2= NInqW3oyPSCvaX6= M3q4ZWROW09? NV;2fHhvSmyxY3vzJGJEWi2rbnT1Z4VlKEyFUEGgd4VzcW6nLUWgZYN1cX[jdHnvci=> NHTwUYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVI{Oyd-MkSwNFkzOzN:L3G+
JEKO-1 NFyzTmxHfW6ldHnvckBCe3OjeR?= NV;ONFBiOSEQvF2= M{LVN|czKGh? MUTJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25iaX6gTYdONXO2aX31cIF1\WRiSlXLU{0y NFj2Zpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O0NVU1OSd-MkOzOFE2PDF:L3G+
Granta-519 NYrtWWdDTnWwY4Tpc44hSXO|YYm= NIfaS4YyKM7:TR?= M{H1PVIhcA>? MWHJcohq[mm2aX;uJI9nKEGtdDj0N|A5MSCyaH;zdIhwenmuYYTpc44> MmfsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|NEG1OFEoRjJ|M{SxOVQyRC:jPh?=
Granta-519 NUnBNWQ1TnWwY4Tpc44hSXO|YYm= NVT6[XF3OSEQvF2= NHfNOmUzKGh? NYjGNJJQUW6qaXLpeIlwdiCxZjDBb5QpezR5MzmgdIhwe3Cqb4L5cIF1cW:w M3G4dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{SxOVQyLz5{M{O0NVU1OTxxYU6=
JEKO-1 M4i1Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrpS48yOCEQvF2= MnT0O|IhcA>? MoruTY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJJNtcWeqdHz5 M2CySlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{SxOVQyLz5{M{O0NVU1OTxxYU6=
JEKO-1 M{mxOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVS1JO69VQ>? M4nD[|czKGh? M3f0[IRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> MoTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4N{[yNlAoRjJ|Nke2NlIxRC:jPh?=
MAVER-1 NFrDcGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\IOUDPxE1? MYW3NkBp MoLp[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5NkKyNEc,OjN4N{[yNlA9N2F-
MINO NF70[odIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXS1JO69VQ>? MX[3NkBp NGfn[4xld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ M2\2UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nke2NlIxLz5{M{[3OlIzODxxYU6=
SP53 NX61NWlMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDpNmkxNjFizszN MWq3NkBp NXrWeXRL\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? NWnjcHBbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2O|YzOjBpPkKzOlc3OjJyPD;hQi=>
HH MkPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvu[pBHOTBizszN NHHYbmM4OiCq M4T2dGROW09? NX31OIFVUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDzcIlocHSueR?= NXfO[m5mRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
Myla MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPhNVAh|ryP M1zKR|czKGh? MWfEUXNQ MVnkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| NYPKVFVORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
SR786 MkWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTRTVYyOCEQvF2= MYq3NkBp NGLiO|BFVVOR NEPicnpld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz NF7HbnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiwNVk2QSd-MkK4NFE6PTl:L3G+
HuT78 MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrNcWEyOCEQvF2= MYG3NkBp NYHndGg1TE2VTx?= MkX3[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NH[zU5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiwNVk2QSd-MkK4NFE6PTl:L3G+
MJ M1jJfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTnNZoyOCEQvF2= NYLwU4d3PzJiaB?= Mn71SG1UVw>? MXrkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MoPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
DERL7 M1u2ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVmxNEDPxE1? MWO3NkBp NH73SHVFVVOR M{TVSYRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= MoTaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
L1236 NXj3[WhpTnWwY4Tpc44hSXO|YYm= M4LWWFExKM7:TR?= NIm5R5AzKGh? NXX6V5F2UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u M{K3T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
L428 MUXGeY5kfGmxbjDBd5NigQ>? MlLiNVAh|ryP MofkNkBp MXvJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L591 MWDGeY5kfGmxbjDBd5NigQ>? NWnHVnQ1OTBizszN MnjvNkBp MUXJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? M4nnPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
KMH-2 MkjNSpVv[3Srb36gRZN{[Xl? NYf5SmdoOTBizszN NX;IfHhtOiCq NELKPFNKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= M4jPblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
L1236 NIfXT4pHfW6ldHnvckBCe3OjeR?= NFjWO|g2KM7:TR?= MYGyOEBp MmDIRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> NH3LNoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKxNFg4Pyd-MkKyNVA5Pzd:L3G+
L591 NF3zVo5HfW6ldHnvckBCe3OjeR?= Mk\GOUDPxE1? MX6yOEBp MVHCcI9kc3Nic3XjdoV1cW:wIH;mJJRp\SCFQ1y1 NV;FcmQ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNVA5PzdpPkKyNlExQDd5PD;hQi=>
L1236 MlTLRZBweHSxc3nzJGF{e2G7 MkXHOUDPxE1? M3v2e|I1KGh? MoK4TY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? NUXLb5ZVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNVA5PzdpPkKyNlExQDd5PD;hQi=>
L591 MV\BdI9xfG:|aYOgRZN{[Xl? M4XOb|Uh|ryP M{nkZVI1KGh? Moe5TY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? NV;hN2F[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNVA5PzdpPkKyNlExQDd5PD;hQi=>
U-87MG MVjGeY5kfGmxbjDBd5NigQ>? NF3xUoYyODBibl2= M4HISVI1KGh? NFPxSm5FVVOR MnnXTY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> NFT5UW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3PVYxQSd-MkKwO|k3ODl:L3G+
SW1783 M1XJRmZ2dmO2aX;uJGF{e2G7 MlS5NVAxKG6P NEjheIszPCCq MXLEUXNQ NILjNWtKdmirYnn0bY9vKG:oIDDj[YxtKG2rZ4LheIlwdg>? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
U-87MG NWfET3RETnWwY4Tpc44hSXO|YYm= M1\m[lUh|ryP NIG2R4wzPCCq NHvqUlFFVVOR MnjMTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NX\jbJJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwO|k3ODlpPkKyNFc6PjB7PD;hQi=>
SW1783 MX3GeY5kfGmxbjDBd5NigQ>? NVnIfppWPSEQvF2= M4TuPVI1KGh? M1P6V2ROW09? NGLHSJpKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
U-373MG Mn\NSpVv[3Srb36gRZN{[Xl? MYm1JO69VQ>? M1PTOlI1KGh? NH7vN5lFVVOR NEGyeI9KdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? MkSwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{m2NFkoRjJ{MEe5OlA6RC:jPh?=
SK-MG3 MVLGeY5kfGmxbjDBd5NigQ>? NGKwWFQ2KM7:TR?= NH63VYYzPCCq M2DzXmROW09? NWn6dnZRUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? MmrsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{m2NFkoRjJ{MEe5OlA6RC:jPh?=
SU-DHL-5 NInLfI5HfW6ldHnvckBCe3OjeR?= NF3LOWMyKM7:TR?= NY[3bJJqOjRiaB?= NXvBe|ZWTE2VTx?= M2rm[Glv\HWldHnvckBw\iCjcH;weI9{cXN? NHrNNlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEm1PVYxPid-MkC5OVk3ODZ:L3G+
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SU-DHL6 NITPZ4lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEXjXYlIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBUXS2GSFy2JINmdGy|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEeLNUCgQUAxNjB2MjFOwG0v NWfiV5ZNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2NFE6QTFpPkK5OlAyQTlzPD;hQi=>
MOLM13 MlTpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MW[3NkBpenN? MlG3S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUW9NVTF|IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JIF{e2G7LDDHTVUxKD1iMT63JO69VS5? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB3M{eyNUc,OzByNUO3NlE9N2F-
MOLM14 M3ewdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3H6e|czKGi{cx?= M1XwVmdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1QVE1zNDDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW|Y3XueEBie3OjeTygS2k2OCB;IE[uOEDPxE1w MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB3M{eyNUc,OzByNUO3NlE9N2F-
MOLM14 NWDQWot1SW62aYT1cY9zKGG|c3H5 M2PVNFExOCCvZz;r[y=> M3nXZVE1KGSjeYO= MlLrRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV;MUVE1KGOnbHzzJJhmdm:pcnHmeIVlKGmwIH71M452KG2xdYPlJIF{e2W|c3XkJIF{KHS3bX;yJIdzd3e2aDDpcohq[mm2aX;uJIF1KDFyMDDt[{9s\yxicH:gZYRucW6rc4TldoVlKGSjaXz5JJZq[SCpYY\h[4Uh\G:|ZXSg[o9zKDF2IHThfZMh[W6mIH3lZZN2emWmIHThbYx6KGS3cnnu[{Bkd22yb4Xu[EBld3OrbnegdoVt[XSrdnWgeI8h[2:wdILvcC=> M33zcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEWzO|IyLz5|MEC1N|czOTxxYU6=
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MOLM14 M{XOU2FvfGm2dX3vdkBie3OjeR?= MnG3NVAxKG2pL3vn NHrYbVcyPCCmYYnz NXrrSYo6SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUW9NVTF2IHPlcIx{KHinbn;ndoFnfGWmIHnuJI52N263IH3veZNmKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhfHWvb4KgdJJwdGmoZYLheIlwdiBzMECgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCmYXnsfUB3cWFiZ3H2ZYdmKGSxc3XkJIZweiBzNDDkZZl{KGGwZDDt[YF{fXKnZDDkZYltgSCmdYLpcoch[2:vcH;1coQh\G:|aX7nJIJ6KEurLU[3JIxi[mWubHnu[{Bj[XOnZDDpcY12dm:q MnPLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByNUO3NlEoRjNyMEWzO|IyRC:jPh?=
Assay
Methods Test Index PMID
Western blot Akt(T308) / PDK1(S241) / GSK-3β(S9) ; p-FoxO3a / FoxO3a ; Mcl-1 / Bcl-2 / Bid / Bcl-xl / Noxa / Bak / Bax ; Cleaved caspase 3 / Cleaved caspase 9 ; p-AKT / AKT ; p-p65 ; Bim / Bcl-xl / Bid / Mcl-1 ; PUMA / p53 27342398 30224718 28008149
Growth inhibition assay Cell viability ; Cell viability 30224718 28008149

Protocol (from reference)

Kinase Assay:[2]
  • 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]
  • 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 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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 Completed Drug: Idelalisib Follicular Non-Hodgkin''s Lymphoma Refractory Gilead Sciences May 25 2018 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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