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 218 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 M1HKVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXRfWVkTE2VTx?= NVyzcYFFUUN3ME2yNE41KM7:TR?= NF7tcI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm5PVM2Oid-MkW5PVk{PTJ:L3G+
CLL PBMCs M2XV[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrUVW9FVVOR MWjJR|UxRTJwOTDuUS=> NGGzcYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUmxO|I3Pyd-MkW5NVczPjd:L3G+
U266 MkPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHS1ems1OCEQvF2= MlKwOFghcA>? MX63PU42LSCrbnjpZol1cW:wIILheIU> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN|OUOzNkc,OjV|M{mzN|I9N2F-
K562 M2O2eWZ2dmO2aX;uJGF{e2G7 NVXrPWR6OSEQvF2= MYGzJIg> MVnJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NV\ZdWVvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
K562 NUXRZ5U6TnWwY4Tpc44hSXO|YYm= NHzYVGsyKM7:TR?= M4nLV|MhcA>? NFrtWWhKdmirYnn0bY9vKG:oIGC3NHM3UyCyaH;zdIhwenmuYYTpc44> NYXQeYIyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
K562 NW\nb5h5TnWwY4Tpc44hSXO|YYm= M1HoZ|Eh|ryP MVWzJIg> M3zXO2lvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= MnLVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUS3O|UoRjJ3MEG0O|c2RC:jPh?=
K562 NEW1c2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\iVoI6OSEQvF2= NXHQXlIyPzJiaB?= NV7MTYt5UW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9v NWnYS40zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
Primary AML cell M4K5XWZ2dmO2aX;uJGF{e2G7 NVH4dWhoOSEQvF2= NVLuSlhMOyCq NYjjUHAzUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u NFjJZXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Primary AML cell M1zpV2Z2dmO2aX;uJGF{e2G7 M4TwXFEh|ryP M4XJT|MhcA>? MkPBTY5pcWKrdHnvckBw\iCSN{DTOmsheGixc4Doc5J6dGG2aX;u NIjPdWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Primary AML cell M4DTS2Z2dmO2aX;uJGF{e2G7 NG\q[GYyKM7:TR?= NV3TNXM5OyCq NIrHOWlKdmirYnn0bY9vKG:oIFfTT|MheGixc4Doc5J6dGG2aX;u MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTBzNEe3OUc,OjVyMUS3O|U9N2F-
Primary AML cell MnL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LTclEh|ryP NEnVXHo{KGh? NXKyZXpxW3WycILld5Nqd25ib3[gdnJPSSC|eX70bIV{cXN? M3e2Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Microglia NGD0V4tHfW6ldHnvckBCe3OjeR?= NInUb282KM7:TR?= MX2xNEBp NYrXdGF2TE2VTx?= Mn3RSIVkemWjc3Wgc4YhXE6IYTDz[YNz\XSrb36g[pJwdSCOUGOtd5RqdXWuYYTl[EAheDFzMN80SFkyOEFxREmxNGEhdWmlcn;ncIli MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ{NU[4OEc,OjR4MkW2PFQ9N2F-
Primary CLL cell MUnGeY5kfGmxbjDBd5NigQ>? NXHtW484OSEQvF2= MoTmNVUhdWmw M1S2dWROW09? NXTY[oNpSmyxY3vzJGJEWi2rbnT1Z4VlKEyFUEGgd4VzcW6nLUWgZYN1cX[jdHnvci=> NFLNPJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVI{Oyd-MkSwNFkzOzN:L3G+
JEKO-1 Ml3vSpVv[3Srb36gRZN{[Xl? MoLINUDPxE1? NEPXWZU4OiCq NXnrTGREUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJIlvKEmpTT3zeIlufWyjdHXkJGpGU09vMR?= MlXvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|NEG1OFEoRjJ|M{SxOVQyRC:jPh?=
Granta-519 MXLGeY5kfGmxbjDBd5NigQ>? M3y5WlEh|ryP Ml\1NkBp MmXMTY5pcWKrdHnvckBw\iCDa4SoeFMxQClicHjvd5Bpd3K7bHH0bY9v NEDKSHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O0NVU1OSd-MkOzOFE2PDF:L3G+
Granta-519 NVv6UXRHTnWwY4Tpc44hSXO|YYm= M4LWcFEh|ryP MV6yJIg> MVPJcohq[mm2aX;uJI9nKEGtdDjzOFc{MSCyaH;zdIhwenmuYYTpc44> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN2MUW0NUc,OjN|NEG1OFE9N2F-
JEKO-1 M2DUPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml6yNVAh|ryP MmX3O|IhcA>? MkDMTY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJJNtcWeqdHz5 NYjzfZZ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOFE2PDFpPkKzN|QyPTRzPD;hQi=>
JEKO-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfJXpFmPSEQvF2= MUW3NkBp NWDaSo9E\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? NF3RWIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[3OlIzOCd-MkO2O|YzOjB:L3G+
MAVER-1 MmrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PsWlUh|ryP MmDhO|IhcA>? MULkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz M3j6elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nke2NlIxLz5{M{[3OlIzODxxYU6=
MINO NX3Xe3JKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWi1JO69VQ>? MVm3NkBp NXnwbmIz\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? Mly3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4N{[yNlAoRjJ|Nke2NlIxRC:jPh?=
SP53 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmwMlEh|ryP NF[3WYs4OiCq M2fIS4Rw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> M4DGSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nke2NlIxLz5{M{[3OlIzODxxYU6=
HH NEXoRnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnuNVAh|ryP M3LxeFczKGh? NWDuN3A{TE2VTx?= NVTTNXpFUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDzcIlocHSueR?= NUOw[XJERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
Myla MmSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPtXFM6OTBizszN NGr1NnY4OiCq MkHWSG1UVw>? MlPF[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NU[0N4pjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
SR786 NF;wbJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\mfXcyOCEQvF2= M1OyNFczKGh? MXzEUXNQ MnrG[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyMUm1PUc,OjJ6MEG5OVk9N2F-
HuT78 NX;iW2FTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzrblkyOCEQvF2= MXe3NkBp NV\CUHJkTE2VTx?= MU\kc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| NYrsdWJpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
MJ MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmi4NVAh|ryP MXq3NkBp MVPEUXNQ MmX6[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NYjtSI1NRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
DERL7 MoX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3iT2NEOTBizszN M4ryWVczKGh? M2fsT2ROW09? M4rWW4Rw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= M{\1NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OECxPVU6Lz5{MkiwNVk2QTxxYU6=
L1236 NXTVR2VCTnWwY4Tpc44hSXO|YYm= MV:xNEDPxE1? MUmyJIg> NELSWItKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= MnjiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
L428 MkP0SpVv[3Srb36gRZN{[Xl? MmnUNVAh|ryP MXKyJIg> Mn\lTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NXzo[3VIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNVA5PzdpPkKyNlExQDd5PD;hQi=>
L591 NVTZe3lLTnWwY4Tpc44hSXO|YYm= M4H0U|ExKM7:TR?= NEftUlYzKGh? NI\EZVhKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= NWHOOm1wRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNVA5PzdpPkKyNlExQDd5PD;hQi=>
KMH-2 MnHhSpVv[3Srb36gRZN{[Xl? MW[xNEDPxE1? MUKyJIg> MWfJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NFnRSJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKxNFg4Pyd-MkKyNVA5Pzd:L3G+
L1236 MXPGeY5kfGmxbjDBd5NigQ>? Mk\OOUDPxE1? NECzWWYzPCCq MX\CcI9kc3Nic3XjdoV1cW:wIH;mJJRp\SCFQ1y1 M2j5XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
L591 MUHGeY5kfGmxbjDBd5NigQ>? M1LpT|Uh|ryP NE\GTnQzPCCq M2nZXmJtd2OtczDz[YNz\XSrb36gc4YhfGinIFPDUFU> MorOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
L1236 NXLscpM6SXCxcITvd4l{KEG|c3H5 MWq1JO69VQ>? NFjLUpUzPCCq MYPJcoR2[3Srb36gc4Yh[XCxcITvd4l{ M4TZNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
L591 M3GyVWFxd3C2b4Ppd{BCe3OjeR?= MnrIOUDPxE1? NHPKXYQzPCCq MUnJcoR2[3Srb36gc4Yh[XCxcITvd4l{ M2izUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
U-87MG MV\GeY5kfGmxbjDBd5NigQ>? NGjYSoIyODBibl2= MnXyNlQhcA>? NFrZbotFVVOR M3LUXWlvcGmkaYTpc44hd2ZiIHPlcIwhdWmpcnH0bY9v NIHUW2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3PVYxQSd-MkKwO|k3ODl:L3G+
SW1783 NIf1WHhHfW6ldHnvckBCe3OjeR?= NXLtOZhLOTByIH7N NXzp[ZdZOjRiaB?= NWfafI5nTE2VTx?= NFLmNpVKdmirYnn0bY9vKG:oIDDj[YxtKG2rZ4LheIlwdg>? NWnPUHh4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwO|k3ODlpPkKyNFc6PjB7PD;hQi=>
U-87MG NGHhVHdHfW6ldHnvckBCe3OjeR?= NXvxN2FnPSEQvF2= MXGyOEBp NXjkXo84TE2VTx?= NGnjUnRKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? M4LVWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEe5OlA6Lz5{MkC3PVYxQTxxYU6=
SW1783 NUnNW5lCTnWwY4Tpc44hSXO|YYm= NYHw[5lVPSEQvF2= NWXFfpA6OjRiaB?= MnjxSG1UVw>? M{LRTWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6 NIe2b4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3PVYxQSd-MkKwO|k3ODl:L3G+
U-373MG MYjGeY5kfGmxbjDBd5NigQ>? M{\n[VUh|ryP M4XkVlI1KGh? MVnEUXNQ MoL0TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NUPHU3V5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwO|k3ODlpPkKyNFc6PjB7PD;hQi=>
SK-MG3 MlnhSpVv[3Srb36gRZN{[Xl? MWO1JO69VQ>? M1nmWlI1KGh? MYrEUXNQ MkLETY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NF3VfGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3PVYxQSd-MkKwO|k3ODl:L3G+
SU-DHL-5 MXHGeY5kfGmxbjDBd5NigQ>? MYOxJO69VQ>? M2LnU|I1KGh? NIPyR4ZFVVOR NFPZNZVKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| MoTSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB7NUm2NFYoRjJyOUW5OlA3RC:jPh?=
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Pfeiffer NEnJ[JJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX\Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDQ[oVq\m[ncjDj[YxteyCkeTDDR2s5KGG|c3H5MEBIUTVyIE2gNE44PCEQvF2u Mke2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6M{W4NFUoRjJ6OEO1PFA2RC:jPh?=
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SUDHL6 MX\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M4XodFczKGi{cx?= NYfBWIxSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTWWRJVDZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNEUzhiYYPzZZktKEmFNUCgQUAxNjZ3IN88UU4> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV|NEmzOkc,Ojl3M{S5N|Y9N2F-
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Raji M{\KbmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M4G4WVczKGi{cx?= NEn5T3lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLhbokh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEmuPVUh|ryPLh?= NFmzO5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWzOFk{Pid-Mkm1N|Q6OzZ:L3G+
SU-DHL6 Ml;6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MorkS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gV3UuTEiONjDj[YxteyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBIUTVyIE2gNE4xPDJizszNMi=> MlXlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4MEG5PVEoRjJ7NkCxPVkyRC:jPh?=
MOLM13 NVL5O4xHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUK3NkBpenN? MlnIS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUW9NVTF|IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JIF{e2G7LDDHTVUxKD1iMT63JO69VS5? NGjPbVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC1N|czOSd-M{CwOVM4OjF:L3G+
MOLM14 M2TxO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{DPNFczKGi{cx?= NGfNSJRIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOV0yPMUSgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[XO|YYmsJGdKPTBiPTC2MlQh|ryPLh?= MlK1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByNUO3NlEoRjNyMEWzO|IyRC:jPh?=
MOLM14 M4e1NmFvfGm2dX3vdkBie3OjeR?= NW\kfY84OTByIH3nM4to MlL3NVQh\GG7cx?= NUCx[WJHSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUW9NVTF2IHPlcIx{KHinbn;ndoFnfGWmIHnuJI52N263IH3veZNmKGG|c3Xzd4VlKGG|IIT1cY9zKGe{b4f0bEBqdmirYnn0bY9vKGG2IEGwNEBu\y:tZzygdI8h[WSvaX7pd5RmemWmIHThbYx6KH[rYTDnZZZi\2ViZH;z[YQh\m:{IEG0JIRigXNiYX7kJI1m[XO3cnXkJIRicWy7IHT1dolv\yClb33wc5Vv\CCmb4PpcochemWuYYTpeoUhfG9iY3;ueJJwdA>? NXPZeIwzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwOVM4OjFpPkOwNFU{PzJzPD;hQi=>
MOLM14 MYXBcpRqfHWvb4KgZZN{[Xl? NYfMOJRYOTByIH3nM4to NUL2NXBuOTRiZHH5dy=> Mn3jRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV;MUVE1KGOnbHzzJJhmdm:pcnHmeIVlKGmwIH71M452KG2xdYPlJIF{e2W|c3XkJIF{KGmwZIXjeIlwdiCxZjDhdI9xfG:|aYOgZZQhOTByIH3nM4toNCCybzDh[I1qdmm|dHXy[YQh\GGrbImgeoliKGejdnHn[UBld3OnZDDmc5IhOTRiZHH5d{BidmRibXXhd5Vz\WRiZHHpcJkh\HW{aX7nJINwdXCxdX7kJIRwe2mwZzDifUBVXU6HTDDiZZNm\CCjc4PhfS=> NFjhWlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC1N|czOSd-M{CwOVM4OjF:L3G+
MOLM14 NVjVZ4s6SW62aYT1cY9zKGG|c3H5 NWr0dWZXOTByIH3nM4to NVPVVXhtOTRiZHH5dy=> NIfDb49CdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xOOTRiY3XscJMhgGWwb3fyZYZ1\WRiaX6gcpUwdnVibX;1d4Uh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB1fW2xcjDwdo9tcW[ncnH0bY9vKDFyMDDt[{9s\yxicH:gZYRucW6rc4TldoVlKGSjaXz5JJZq[SCpYY\h[4Uh\G:|ZXSg[o9zKDF2IHThfZMh[W6mIH3lZZN2emWmIHThbYx6KGS3cnnu[{Bkd22yb4Xu[EBld3OrbnegZpkhU2lvNkegcIFj\WyuaX7nJIJie2WmIHntcZVvd2h? MnTjQIEhfGG{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 Active not recruiting Drug: Idelalisib Follicular Non-Hodgkin''s Lymphoma Refractory Gilead Sciences May 25 2018 --

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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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