Idelalisib

Catalog No.S2226 Synonyms: CAL-101, GS-1101

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  Chemical Structure

CAS No. 870281-82-6

Selleck's Idelalisib has been cited by 233 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 NHjuV5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7ySG1UVw>? MXTJR|UxRTJyLkSg{txO MlLRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7OUmzOVIoRjJ3OUm5N|UzRC:jPh?=
CLL PBMCs M3:4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvUSG1UVw>? MVnJR|UxRTJwOTDuUS=> NWnoS5NRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5NVczPjdpPkK1PVE4OjZ5PD;hQi=>
U266 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWO0NEDPxE1? MUC0PEBp NHO3PXU4QS53JTDpcohq[mm2aX;uJJJifGV? M3;UdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{O5N|MzLz5{NUOzPVM{OjxxYU6=
K562 M4myb2Z2dmO2aX;uJGF{e2G7 MkLONUDPxE1? MU[zJIg> M3HPbGlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTBzNEe3OUc,OjVyMUS3O|U9N2F-
K562 M{XPPGZ2dmO2aX;uJGF{e2G7 NH\ndlMyKM7:TR?= MWizJIg> MVXJcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:|cHjvdplt[XSrb36= M2npRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
K562 NFrXTZNHfW6ldHnvckBCe3OjeR?= MlLwNUDPxE1? M4TEUlMhcA>? Mlu1TY5pcWKrdHnvckBw\iCJU1uzJJBpd3OyaH;yfYxifGmxbh?= Mnv2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUS3O|UoRjJ3MEG0O|c2RC:jPh?=
K562 NVviXFV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[xJO69VQ>? M{DldlczKGh? NXm5do9jUW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9v NXzhdWJHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
Primary AML cell MlK4SpVv[3Srb36gRZN{[Xl? M2fJXlEh|ryP MUWzJIg> NGrnTlBKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= M1PZRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Primary AML cell NEHPe3ZHfW6ldHnvckBCe3OjeR?= M4jEXFEh|ryP MUizJIg> NEPydm5KdmirYnn0bY9vKG:oIGC3NHM3UyCyaH;zdIhwenmuYYTpc44> M{G0c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Primary AML cell NUfVfnk1TnWwY4Tpc44hSXO|YYm= MVOxJO69VQ>? NVPwO2xTOyCq NI\vXohKdmirYnn0bY9vKG:oIFfTT|MheGixc4Doc5J6dGG2aX;u M4TG[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Primary AML cell NVfGTHpPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrzUXgyKM7:TR?= NWGzOGZmOyCq NViyS4xEW3WycILld5Nqd25ib3[gdnJPSSC|eX70bIV{cXN? NYXyNVdTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
Microglia MmHJSpVv[3Srb36gRZN{[Xl? Mn74OUDPxE1? M1rLUVExKGh? M2m0OWROW09? NYLDe|U2TGWlcnXhd4Uhd2ZiVF7GZUB{\WO{ZYTpc44h\nKxbTDMVHMue3SrbYXsZZRm\CBicEGxNO61TDlzMFGvSFkyOEFibXnjdo9odGmj MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ{NU[4OEc,OjR4MkW2PFQ9N2F-
Primary CLL cell NHq4cGdHfW6ldHnvckBCe3OjeR?= NH7ZN48yKM7:TR?= MYixOUBucW5? M2HtZ2ROW09? NVjpeYRQSmyxY3vzJGJEWi2rbnT1Z4VlKEyFUEGgd4VzcW6nLUWgZYN1cX[jdHnvci=> NH7uXlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVI{Oyd-MkSwNFkzOzN:L3G+
JEKO-1 MmTFSpVv[3Srb36gRZN{[Xl? NVS2fmV1OSEQvF2= MlTiO|IhcA>? M1vTcGlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDpckBK\01vc4TpcZVt[XSnZDDKSWtQNTF? NVP6eIxkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOFE2PDFpPkKzN|QyPTRzPD;hQi=>
Granta-519 M1fDN2Z2dmO2aX;uJGF{e2G7 M{TXPVEh|ryP NFrETpYzKGh? MmfJTY5pcWKrdHnvckBw\iCDa4SoeFMxQClicHjvd5Bpd3K7bHH0bY9v M3m1c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{SxOVQyLz5{M{O0NVU1OTxxYU6=
Granta-519 NF3ZNmFHfW6ldHnvckBCe3OjeR?= NITW[3oyKM7:TR?= MmrjNkBp MYPJcohq[mm2aX;uJI9nKEGtdDjzOFc{MSCyaH;zdIhwenmuYYTpc44> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN2MUW0NUc,OjN|NEG1OFE9N2F-
JEKO-1 NYPBfXJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHj1V5gyOCEQvF2= MkfDO|IhcA>? MoHMTY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJJNtcWeqdHz5 NHLJS2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O0NVU1OSd-MkOzOFE2PDF:L3G+
JEKO-1 NE\Oe4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTYTVFQPSEQvF2= M1ywS|czKGh? M17Pd4Rw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> MmqxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4N{[yNlAoRjJ|Nke2NlIxRC:jPh?=
MAVER-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWO1JO69VQ>? NF;iXWY4OiCq MWfkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz NEiw[3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[3OlIzOCd-MkO2O|YzOjB:L3G+
MINO MkLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXy1UG1WPSEQvF2= MXO3NkBp NIrWUXJld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ NXflUlFORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2O|YzOjBpPkKzOlc3OjJyPD;hQi=>
SP53 NUHpeW84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;rOIZuOC5zIN88US=> MXu3NkBp Mo[4[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5NkKyNEc,OjN4N{[yNlA9N2F-
HH NGPzTIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLj[W4yOCEQvF2= NF;wboI4OiCq NF\ncJhFVVOR NVjSeZF[UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDzcIlocHSueR?= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyMUm1PUc,OjJ6MEG5OVk9N2F-
Myla Mn:0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XtSFExKM7:TR?= M4fUeFczKGh? NELy[FBFVVOR M1;6cIRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= NG\IU2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiwNVk2QSd-MkK4NFE6PTl:L3G+
SR786 NWS5[GNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfXNVAh|ryP NYX5eHlMPzJiaB?= NVPxZ5RuTE2VTx?= NHjPNVFld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MoLjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
HuT78 MkHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVOxNEDPxE1? NE\XepU4OiCq MYnEUXNQ MX\kc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MojiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
MJ NF32c5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVGxNEDPxE1? NUf2OWtGPzJiaB?= MYnEUXNQ MVTkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyMUm1PUc,OjJ6MEG5OVk9N2F-
DERL7 NEnvZmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV20WFNQOTBizszN NIDjR|k4OiCq MnL5SG1UVw>? NF\XTphld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyMUm1PUc,OjJ6MEG5OVk9N2F-
L1236 NUTuT4tZTnWwY4Tpc44hSXO|YYm= NVzadlBsOTBizszN MVmyJIg> NIL1TVFKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L428 M2rodGZ2dmO2aX;uJGF{e2G7 M3vGN|ExKM7:TR?= NFS1e5MzKGh? MYnJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NHnlUnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKxNFg4Pyd-MkKyNVA5Pzd:L3G+
L591 MkDHSpVv[3Srb36gRZN{[Xl? M4\LN|ExKM7:TR?= M1Hje|IhcA>? NYjJZ5NoUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u NITlZ2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKxNFg4Pyd-MkKyNVA5Pzd:L3G+
KMH-2 MV\GeY5kfGmxbjDBd5NigQ>? M2raXVExKM7:TR?= M1P6VlIhcA>? NFHK[JZKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L1236 NYG4ZXpNTnWwY4Tpc44hSXO|YYm= MnrlOUDPxE1? M2XPblI1KGh? NETCWGtDdG:la4Ogd4VkemW2aX;uJI9nKHSqZTDDR2w2 MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L591 MojZSpVv[3Srb36gRZN{[Xl? NHW2UVE2KM7:TR?= NGDRV|IzPCCq M1PWUmJtd2OtczDz[YNz\XSrb36gc4YhfGinIFPDUFU> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L1236 NX;VSplrSXCxcITvd4l{KEG|c3H5 MYe1JO69VQ>? MWeyOEBp MYPJcoR2[3Srb36gc4Yh[XCxcITvd4l{ MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L591 NYO2Wo94SXCxcITvd4l{KEG|c3H5 NVv2d5pMPSEQvF2= MmDNNlQhcA>? MkjkTY5lfWO2aX;uJI9nKGGyb4D0c5Nqew>? MlzjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
U-87MG NXzkcHFNTnWwY4Tpc44hSXO|YYm= MXWxNFAhdk1? MX:yOEBp NFzLTJJFVVOR NIDmUo5KdmirYnn0bY9vKG:oIDDj[YxtKG2rZ4LheIlwdg>? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
SW1783 M{nUUGZ2dmO2aX;uJGF{e2G7 MW[xNFAhdk1? MUGyOEBp NF\NTFJFVVOR MV7Jcohq[mm2aX;uJI9nKCClZXzsJI1q\3KjdHnvci=> NGO3d3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3PVYxQSd-MkKwO|k3ODl:L3G+
U-87MG MUfGeY5kfGmxbjDBd5NigQ>? NWK5RWI4PSEQvF2= MYCyOEBp NGTqeI9FVVOR NGHERmVKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
SW1783 NE\tRlZHfW6ldHnvckBCe3OjeR?= MkfqOUDPxE1? MXeyOEBp MUnEUXNQ NI[xfWNKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? M2TFfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEe5OlA6Lz5{MkC3PVYxQTxxYU6=
U-373MG MlzJSpVv[3Srb36gRZN{[Xl? NVnxVmZkPSEQvF2= MXOyOEBp MYjEUXNQ NXrMbGdjUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? M4S0cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEe5OlA6Lz5{MkC3PVYxQTxxYU6=
SK-MG3 NGruOWpHfW6ldHnvckBCe3OjeR?= MXq1JO69VQ>? NYHWSmhlOjRiaB?= MmHMSG1UVw>? MUnJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25ic4Xid5RidnSrYXzsfS=> MnL1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{m2NFkoRjJ{MEe5OlA6RC:jPh?=
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SU-DHL6 NXHNcIdtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGLhSIxIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBUXS2GSFy2JINmdGy|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEeLNUCgQUAxNjB2MjFOwG0v NFjMNFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[wNVk6OSd-Mkm2NFE6QTF:L3G+
MOLM13 M4nvR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{PLN|czKGi{cx?= Mm\YS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUW9NVTF|IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JIF{e2G7LDDHTVUxKD1iMT63JO69VS5? M{TxNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEWzO|IyLz5|MEC1N|czOTxxYU6=
MOLM14 NFrPXmdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF;4UI84OiCqcoO= M3PS[2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1QVE1zNDDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW|Y3XueEBie3OjeTygS2k2OCB;IE[uOEDPxE1w MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB3M{eyNUc,OzByNUO3NlE9N2F-
MOLM14 M3H6bmFvfGm2dX3vdkBie3OjeR?= MXKxNFAhdWdxa3e= NHPzeGoyPCCmYYnz NWHw[nBzSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUW9NVTF2IHPlcIx{KHinbn;ndoFnfGWmIHnuJI52N263IH3veZNmKGG|c3Xzd4VlKGG|IIT1cY9zKGe{b4f0bEBqdmirYnn0bY9vKGG2IEGwNEBu\y:tZzygdI8h[WSvaX7pd5RmemWmIHThbYx6KH[rYTDnZZZi\2ViZH;z[YQh\m:{IEG0JIRigXNiYX7kJI1m[XO3cnXkJIRicWy7IHT1dolv\yClb33wc5Vv\CCmb4PpcochemWuYYTpeoUhfG9iY3;ueJJwdA>? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB3M{eyNUc,OzByNUO3NlE9N2F-
MOLM14 NHn4R4FCdnSrdIXtc5Ih[XO|YYm= M2XWd|ExOCCvZz;r[y=> MU[xOEBl[Xm| M4T5fGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUG0yPCClZXzsd{B5\W6xZ4Lh[pRm\CCrbjDueU9vfSCvb4Xz[UBie3Onc4Pl[EBieyCrbnT1Z5Rqd25ib3[gZZBweHSxc3nzJIF1KDFyMDDt[{9s\yxicH:gZYRucW6rc4TldoVlKGSjaXz5JJZq[SCpYY\h[4Uh\G:|ZXSg[o9zKDF2IHThfZMh[W6mIH3lZZN2emWmIHThbYx6KGS3cnnu[{Bkd22yb4Xu[EBld3OrbnegZpkhXFWQRVygZoF{\WRiYYPzZZk> MkS1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByNUO3NlEoRjNyMEWzO|IyRC:jPh?=
MOLM14 M3TGNGFvfGm2dX3vdkBie3OjeR?= NIXiNYEyODBibXevb4c> NUPnW2JkOTRiZHH5dy=> M2PsbmFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUG0yPCClZXzsd{B5\W6xZ4Lh[pRm\CCrbjDueU9vfSCvb4Xz[UBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJR2dW:{IIDyc4xq\mW{YYTpc44hOTByIH3nM4toNCCybzDh[I1qdmm|dHXy[YQh\GGrbImgeoliKGejdnHn[UBld3OnZDDmc5IhOTRiZHH5d{BidmRibXXhd5Vz\WRiZHHpcJkh\HW{aX7nJINwdXCxdX7kJIRwe2mwZzDifUBMcS14NzDsZYJmdGyrbnegZoF{\WRiaX3teY5wcA>? NIXGboQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC1N|czOSd-M{CwOVM4OjF:L3G+
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.

Solubility (25°C)

In vitro

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

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 2022-08-01)

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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