Idelalisib (CAL-101, GS-1101)

For research use only. Not for use in humans.

製品コードS2226

Idelalisib (CAL-101, GS-1101)化学構造

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.

サイズ 価格(税別)  
10mM (1mL in DMSO) JPY 27800
JPY 21900
JPY 80000
JPY 212800
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バルク問合せ

文献中Selleckの製品使用例(193)

製品安全説明書

PI3K阻害剤の選択性比較

生物活性

製品説明 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.
ターゲット
p110δ [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
2.5 nM 89 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MEC1 M1XBc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfjV2tFVVOR MoXvTWM2OD1{MD60JO69VQ>? M12yXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUm5N|UzLz5{NUm5PVM2OjxxYU6=
CLL PBMCs MmjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVT6SnlHTE2VTx?= MmjPTWM2OD1{Lkmgcm0> NXq4OW8zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5NVczPjdpPkK1PVE4OjZ5PD;hQi=>
U266 NFrVNJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWr3NYVwPDBizszN NV\RdoNIPDhiaB?= NUW2OldzPzlwNTWgbY5pcWKrdHnvckBz[XSn MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN|OUOzNkc,OjV|M{mzN|I9N2F-
K562 MojKSpVv[3Srb36gRZN{[Xl? NInKVooyKM7:TR?= NYLFPG5OOyCq MXvJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NGjTOVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
K562 NH7W[ItHfW6ldHnvckBCe3OjeR?= NGT5NnEyKM7:TR?= M2flblMhcA>? NVrTNFN1UW6qaXLpeIlwdiCxZjDQO|BUPkticHjvd5Bpd3K7bHH0bY9v M1fkeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
K562 M1O5OmZ2dmO2aX;uJGF{e2G7 MV:xJO69VQ>? NG\NPIc{KGh? NYjs[3JyUW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=> M2XWZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
K562 MmG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;L[VRqOSEQvF2= MkXEO|IhcA>? NGnLeotKdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44> M{LBelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Primary AML cell MYjGeY5kfGmxbjDBd5NigQ>? MmThNUDPxE1? M{\3XFMhcA>? MoXOTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NGXRXFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Primary AML cell Mnr4SpVv[3Srb36gRZN{[Xl? M{m3NFEh|ryP MWWzJIg> NF[xRYJKdmirYnn0bY9vKG:oIGC3NHM3UyCyaH;zdIhwenmuYYTpc44> M1W1RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Primary AML cell MYLGeY5kfGmxbjDBd5NigQ>? MmXnNUDPxE1? M1vIO|MhcA>? MXrJcohq[mm2aX;uJI9nKEeVS{OgdIhwe3Cqb4L5cIF1cW:w NIPL[Yo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Primary AML cell MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOxJO69VQ>? M2jEPVMhcA>? NGfaXm9UfXCycnXzd4lwdiCxZjDyVm5CKHO7boTo[ZNqew>? NWrNXpZ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
Microglia NV33Uo1zTnWwY4Tpc44hSXO|YYm= MkK1OUDPxE1? NED1UWoyOCCq MYLEUXNQ MlexSIVkemWjc3Wgc4YhXE6IYTDz[YNz\XSrb36g[pJwdSCOUGOtd5RqdXWuYYTl[EAheDFzMN80SFkyOEFxREmxNGEhdWmlcn;ncIli MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ{NU[4OEc,OjR4MkW2PFQ9N2F-
Primary CLL cell M{GzVWZ2dmO2aX;uJGF{e2G7 M1K4RlEh|ryP MUSxOUBucW5? NHjNNHpFVVOR M2TCVmJtd2OtczDCR3IucW6mdXPl[EBNS1BzIIPldolv\S13IHHjeIl3[XSrb36= NUDs[3JSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkzOzNpPkK0NFA6OjN|PD;hQi=>
JEKO-1 MWTGeY5kfGmxbjDBd5NigQ>? NV2wUJRTOSEQvF2= NFvLOZc4OiCq MXvJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25iaX6gTYdONXO2aX31cIF1\WRiSlXLU{0y NHnXU4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O0NVU1OSd-MkOzOFE2PDF:L3G+
Granta-519 M{DCcmZ2dmO2aX;uJGF{e2G7 NWnJdoNMOSEQvF2= MlqzNkBp MUHJcohq[mm2aX;uJI9nKEGtdDj0N|A5MSCyaH;zdIhwenmuYYTpc44> NEXlVI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O0NVU1OSd-MkOzOFE2PDF:L3G+
Granta-519 NV7CbXFYTnWwY4Tpc44hSXO|YYm= M2jrRVEh|ryP M2T3XVIhcA>? NX7hdZAxUW6qaXLpeIlwdiCxZjDBb5QpezR5MzmgdIhwe3Cqb4L5cIF1cW:w NUD3eo9PRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOFE2PDFpPkKzN|QyPTRzPD;hQi=>
JEKO-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXexNEDPxE1? NIPmb2o4OiCq NWSwU|dvUW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9vKHOuaXfoeIx6 MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN2MUW0NUc,OjN|NEG1OFE9N2F-
JEKO-1 M4DTWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUC1JO69VQ>? M1nkdlczKGh? MXfkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5NkKyNEc,OjN4N{[yNlA9N2F-
MAVER-1 NXHndXBRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLWdos2KM7:TR?= M4XtdFczKGh? MWHkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz NXfRN25yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2O|YzOjBpPkKzOlc3OjJyPD;hQi=>
MINO Mm\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYi1JO69VQ>? NWjEfIZPPzJiaB?= NWDEUnNl\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? M4LYfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nke2NlIxLz5{M{[3OlIzODxxYU6=
SP53 M{fLVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvIWY5FOC5zIN88US=> NWX1eGg5PzJiaB?= NUXkc4pv\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? NXrkOY5[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2O|YzOjBpPkKzOlc3OjJyPD;hQi=>
HH MnT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1j1d|ExKM7:TR?= M4TUUFczKGh? NVzvTpRiTE2VTx?= MWnJcoR2[3Srb36gc4Yh[XCxcITvd4l{KHOuaXfoeIx6 M{C5NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OECxPVU6Lz5{MkiwNVk2QTxxYU6=
Myla NGHMN|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPwNVAh|ryP NEmzNJA4OiCq Mk\5SG1UVw>? NHHvOpZld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz NX7KOm1SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
SR786 MofES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXzcpoyOCEQvF2= NX\ZZ4hMPzJiaB?= NWS0UGtiTE2VTx?= MXXkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MlTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
HuT78 NYHxfYN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\OV3JVOTBizszN M1HUSFczKGh? Ml3BSG1UVw>? MoXj[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= M3rne|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OECxPVU6Lz5{MkiwNVk2QTxxYU6=
MJ NXT3d21TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYruTlhHOTBizszN NHT0e4M4OiCq MWDEUXNQ NGDifIlld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyMUm1PUc,OjJ6MEG5OVk9N2F-
DERL7 M33XSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;Qb2MyOCEQvF2= MmDBO|IhcA>? MULEUXNQ M3zVNoRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= NInkdYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiwNVk2QSd-MkK4NFE6PTl:L3G+
L1236 M4flU2Z2dmO2aX;uJGF{e2G7 NGPFcmYyOCEQvF2= NH2wc48zKGh? NUfERmFFUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L428 NV\IcJo5TnWwY4Tpc44hSXO|YYm= NWK1SYpIOTBizszN MW[yJIg> NXvNW3o5UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L591 MXvGeY5kfGmxbjDBd5NigQ>? M2rkb|ExKM7:TR?= Mn;KNkBp NIL6NYxKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= NGTUTo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKxNFg4Pyd-MkKyNVA5Pzd:L3G+
KMH-2 MULGeY5kfGmxbjDBd5NigQ>? NYe2O4dbOTBizszN M1vGOVIhcA>? NFzzN4ZKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L1236 NI\LRodHfW6ldHnvckBCe3OjeR?= NH;SS|U2KM7:TR?= M3rtZlI1KGh? MnPVRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> NUT4XG01RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNVA5PzdpPkKyNlExQDd5PD;hQi=>
L591 MlP1SpVv[3Srb36gRZN{[Xl? MnTrOUDPxE1? MnLNNlQhcA>? NILFPWNDdG:la4Ogd4VkemW2aX;uJI9nKHSqZTDDR2w2 MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L1236 NI\IbWlCeG:ydH;zbZMhSXO|YYm= MkHyOUDPxE1? NFfJPXYzPCCq MV3JcoR2[3Srb36gc4Yh[XCxcITvd4l{ Moq4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
L591 Mn35RZBweHSxc3nzJGF{e2G7 MkTROUDPxE1? MnfXNlQhcA>? M{L5TGlv\HWldHnvckBw\iCjcH;weI9{cXN? MnywQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
U-87MG NE\uN3JHfW6ldHnvckBCe3OjeR?= M3nEeVExOCCwTR?= NUP1N4hVOjRiaB?= M2LPN2ROW09? NHOyO2RKdmirYnn0bY9vKG:oIDDj[YxtKG2rZ4LheIlwdg>? NUDz[W1pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwO|k3ODlpPkKyNFc6PjB7PD;hQi=>
SW1783 M1XHR2Z2dmO2aX;uJGF{e2G7 NVjySmxYOTByIH7N NV\MdJBEOjRiaB?= NVXIR5BRTE2VTx?= Mlu2TY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> M4fVVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEe5OlA6Lz5{MkC3PVYxQTxxYU6=
U-87MG MVrGeY5kfGmxbjDBd5NigQ>? MXW1JO69VQ>? MkXhNlQhcA>? MX;EUXNQ NUKyW2N4UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? NIju[JQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3PVYxQSd-MkKwO|k3ODl:L3G+
SW1783 MnjuSpVv[3Srb36gRZN{[Xl? MkfsOUDPxE1? Ml;YNlQhcA>? MV\EUXNQ MmXyTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NVixUYR3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwO|k3ODlpPkKyNFc6PjB7PD;hQi=>
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SK-MG3 M1zFR2Z2dmO2aX;uJGF{e2G7 Mm\VOUDPxE1? NVHhWVhpOjRiaB?= NWjKTFQ3TE2VTx?= NYC2XY1XUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJJN2[nO2YX70bYFtdHl? MnTDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{m2NFkoRjJ{MEe5OlA6RC:jPh?=
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Raji NEDRbJlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MVq3NkBpenN? MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKjanmgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDlwOUWg{txONg>? Mn3TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3M{S5N|YoRjJ7NUO0PVM3RC:jPh?=
SU-DHL6 MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF7oR4lIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBUXS2GSFy2JINmdGy|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEeLNUCgQUAxNjB2MjFOwG0v NGTqeJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[wNVk6OSd-Mkm2NFE6QTF:L3G+
MOLM13 MmXTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml3CO|IhcHK| NGjCb2pIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOV0yPMUOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[XO|YYmsJGdKPTBiPTCxMlch|ryPLh?= M3f4XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEWzO|IyLz5|MEC1N|czOTxxYU6=
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MOLM14 NUTWTWFoSW62aYT1cY9zKGG|c3H5 Ml;3NVAxKG2pL3vn NIfsOG4yPCCmYYnz MYDBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVQh[2WubIOgfIVvd2e{YX\0[YQhcW5iboWvcpUhdW:3c3WgZZN{\XO|ZXSgZZMhfHWvb4Kg[5Jwf3SqIHnubIljcXSrb36gZZQhOTByIH3nM4toNCCybzDh[I1qdmm|dHXy[YQh\GGrbImgeoliKGejdnHn[UBld3OnZDDmc5IhOTRiZHH5d{BidmRibXXhd5Vz\WRiZHHpcJkh\HW{aX7nJINwdXCxdX7kJIRwe2mwZzDy[YxifGm4ZTD0c{Bkd262cn;s MkTsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByNUO3NlEoRjNyMEWzO|IyRC:jPh?=
MOLM14 M{nQSWFvfGm2dX3vdkBie3OjeR?= M4HmW|ExOCCvZz;r[y=> M1PEVlE1KGSjeYO= NV[xZmZMSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUW9NVTF2IHPlcIx{KHinbn;ndoFnfGWmIHnuJI52N263IH3veZNmKGG|c3Xzd4VlKGG|IHnu[JVkfGmxbjDv[kBieG:ydH;zbZMh[XRiMUCwJI1oN2upLDDwc{Bi\G2rbnnzeIVz\WRiZHHpcJkhfmmjIHfheoFo\SCmb4Pl[EBnd3JiMUSg[IF6eyCjbnSgcYVie3W{ZXSg[IFqdHliZIXybY5oKGOxbYDveY5lKGSxc3nu[{BjgSCWVV7FUEBj[XOnZDDhd5NigQ>? NIXpOnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC1N|czOSd-M{CwOVM4OjF:L3G+
MOLM14 NVjGZ4RiSW62aYT1cY9zKGG|c3H5 MVSxNFAhdWdxa3e= Ml7oNVQh\GG7cx?= NVHBRnZPSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUW9NVTF2IHPlcIx{KHinbn;ndoFnfGWmIHnuJI52N263IH3veZNmKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhfHWvb4KgdJJwdGmoZYLheIlwdiBzMECgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCmYXnsfUB3cWFiZ3H2ZYdmKGSxc3XkJIZweiBzNDDkZZl{KGGwZDDt[YF{fXKnZDDkZYltgSCmdYLpcoch[2:vcH;1coQh\G:|aX7nJIJ6KEurLU[3JIxi[mWubHnu[{Bj[XOnZDDpcY12dm:q NVH2c5hFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwOVM4OjFpPkOwNFU{PzJzPD;hQi=>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
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

お薦めの試験操作(参考用のみ)

キナーゼ試験:[2]
- 合併

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.
細胞試験: [2]
- 合併
  • 細胞株: CLL B cells or healthy volunteer T cells or NK cells
  • 濃度: 0.01-100 μM
  • 反応時間: 48 hours
  • 実験の流れ: 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.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 83 mg/mL (199.79 mM) warming
Ethanol 23 mg/mL (55.36 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+20%PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 415.42
化学式

C22H18FN7O

CAS No. 870281-82-6
Storage powder
in solvent
別名 N/A
Smiles CCC(C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

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 --

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    What is the recommended dose of CAL-101 and the route of administration for mouse studies?

  • 回答:

    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

PI3Kシグナル伝達経路

PI3K Inhibitors with Unique Features

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Tags: Idelalisib (CAL-101, GS-1101)を買う | Idelalisib (CAL-101, GS-1101) ic50 | Idelalisib (CAL-101, GS-1101)供給者 | Idelalisib (CAL-101, GS-1101)を購入する | Idelalisib (CAL-101, GS-1101)費用 | Idelalisib (CAL-101, GS-1101)生産者 | オーダーIdelalisib (CAL-101, GS-1101) | Idelalisib (CAL-101, GS-1101)化学構造 | Idelalisib (CAL-101, GS-1101)分子量 | Idelalisib (CAL-101, GS-1101)代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID