Idelalisib (CAL-101, GS-1101)

For research use only. Not for use in humans.

目录号:S2226 中文名称:艾代拉里斯,艾代拉利司

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

CAS No. 870281-82-6

Idelalisib (CAL-101, GS-1101) 是选择性p110δ抑制剂,在无细胞试验中IC50为 2.5 nM;对 p110δ 表现出的选择性是对 p110α/β/γ 的 40 到 300 倍,对p110δ的选择性是对 C2β,hVPS34,DNA-PK 和 mTOR的400到4000倍。Idelalisib 还可诱导自噬。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1279.19 现货
RMB 972.85 现货
RMB 3867.24 现货
RMB 10401.3 现货
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客户使用Selleck生产的Idelalisib (CAL-101, GS-1101)发表文献187篇:

产品安全说明书

PI3K抑制剂选择性比较

生物活性

产品描述 Idelalisib (CAL-101, GS-1101) 是选择性p110δ抑制剂,在无细胞试验中IC50为 2.5 nM;对 p110δ 表现出的选择性是对 p110α/β/γ 的 40 到 300 倍,对p110δ的选择性是对 C2β,hVPS34,DNA-PK 和 mTOR的400到4000倍。Idelalisib 还可诱导自噬。
特性 Calistoga 暗示 CAL-101治疗血液恶性肿瘤可能有更广泛的应用价值。
靶点
p110δ [1]
(Cell-free assay)
p110γ [1]
(Cell-free assay)
2.5 nM 89 nM
体外研究

CAL-101 对p110α, p110β,和p110γ作用效果不大。CAL-101作用于原代嗜碱细胞特定阻断FcϵR1 p110δ调节的 CD63表达,EC50 为8 nM。与急性髓性白血病(AML) 和骨髓增生性肿瘤(MPN) 细胞相比,CAL-101 作用于B-cell急性淋巴细胞白血病(B-ALL)和慢性淋巴细胞白血病(CLL) 细胞时显示更强的活性。CAL-101 作用于SU-DHL-5, KARPAS-422 和CCRF-SB细胞,降低pAktS473, pAktT308, 和下游靶点S6, EC50为0.1到1.0 μM。 [1] CAL-101 作用于CLL细胞,诱导选择性细胞毒性,不是通过突变状态或间期细胞遗传学,主要通过caspase依赖机制。与正常B细胞相比,CAL-101作用于CLL 细胞优先产生细胞毒性,和LY294002相比,作用于其他造血细胞不会产生毒性。CAL-101 作用于T 细胞和天然杀伤细胞 缺乏直接的细胞毒性潜能。CAL-101抑制炎症细胞因子的产生,比如 IL-6, IL-10, TNF-α,和IFN-γ,且激活诱导的细胞因子,如CD40L。CAL-101 也抗CD40L调节的CLL细胞存活。[2] CAL-101 作用于L1236和L591细胞, 诱导细胞在G1期积累,在S期下降,说明 CAL-101可以作为治疗霍杰金淋巴瘤(HL)的一种新策略。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MEC1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TDUWROW09? M2HRbGlEPTB;MkCuOEDPxE1? NHXEUnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm5PVM2Oid-MkW5PVk{PTJ:L3G+
CLL PBMCs NX;zcohuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXycppFVVOR M2nk[WlEPTB;Mj65JI5O NHLv[5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUmxO|I3Pyd-MkW5NVczPjd:L3G+
U266 M3f0dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjyb3A1OCEQvF2= NI\Yb5c1QCCq MlvoO|kvPSViaX7obYJqfGmxbjDyZZRm M{TwbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{O5N|MzLz5{NUOzPVM{OjxxYU6=
K562 MlP1SpVv[3Srb36gRZN{[Xl? MYSxJO69VQ>? MX[zJIg> NYfrbpJYUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u M4fRWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
K562 M1T5SWZ2dmO2aX;uJGF{e2G7 MYexJO69VQ>? NWTDWXp6OyCq MYHJcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:|cHjvdplt[XSrb36= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTBzNEe3OUc,OjVyMUS3O|U9N2F-
K562 M1LvXmZ2dmO2aX;uJGF{e2G7 MmToNUDPxE1? NVvQTWxXOyCq NWjJVHhxUW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=> M4fGN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
K562 Mly2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;jUlA2OSEQvF2= NIDYemc4OiCq MYHJcohq[mm2aX;uJI9nKHC{b3zp[oVz[XSrb36= NFLje4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Primary AML cell MmnxSpVv[3Srb36gRZN{[Xl? NETSd4MyKM7:TR?= M1zCWlMhcA>? NHLpNJBKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= MkTqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUS3O|UoRjJ3MEG0O|c2RC:jPh?=
Primary AML cell NHT3e5dHfW6ldHnvckBCe3OjeR?= MWOxJO69VQ>? NEKzUIY{KGh? MX;Jcohq[mm2aX;uJI9nKFB5MGO2T{BxcG:|cHjvdplt[XSrb36= M{G3[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Primary AML cell MWjGeY5kfGmxbjDBd5NigQ>? M3PhU|Eh|ryP MVyzJIg> NV3IZZFKUW6qaXLpeIlwdiCxZjDHV2s{KHCqb4PwbI9zgWyjdHnvci=> NWD3PGdKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
Primary AML cell MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmniNUDPxE1? MXOzJIg> NEXqVHhUfXCycnXzd4lwdiCxZjDyVm5CKHO7boTo[ZNqew>? NEK0W4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Microglia M3TFdGZ2dmO2aX;uJGF{e2G7 M1nIU|Uh|ryP NULjV3VSOTBiaB?= MX;EUXNQ M3[yW2Rm[3KnYYPlJI9nKFSQRnGgd4VkemW2aX;uJIZzd21iTGDTMZN1cW23bHH0[YQhKHBzMUFOuGQ6OTCDL1S5NVBCKG2rY4Lv[4xq[Q>? NYLW[495RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NlU3QDRpPkK0OlI2Pjh2PD;hQi=>
Primary CLL cell MkTESpVv[3Srb36gRZN{[Xl? M2XLflEh|ryP NH;OTFIyPSCvaX6= MkPoSG1UVw>? NE\RWpVDdG:la4OgRmNTNWmwZIXj[YQhVEOSMTDz[ZJqdmVvNTDhZ5RqfmG2aX;u MmPwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmyN|MoRjJ2MEC5NlM{RC:jPh?=
JEKO-1 NWLxdJZbTnWwY4Tpc44hSXO|YYm= MUGxJO69VQ>? NELJWlI4OiCq MkfFTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHnuJGloVS2|dHnteYxifGWmIFrFT28uOQ>? NGHDXo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O0NVU1OSd-MkOzOFE2PDF:L3G+
Granta-519 M4nLcmZ2dmO2aX;uJGF{e2G7 MonPNUDPxE1? NET0VlYzKGh? M3OwXmlvcGmkaYTpc44hd2ZiQXv0LJQ{ODhrIIDoc5NxcG:{eXzheIlwdg>? M4\6bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{SxOVQyLz5{M{O0NVU1OTxxYU6=
Granta-519 NHvvZ4lHfW6ldHnvckBCe3OjeR?= M1\0[|Eh|ryP MlvpNkBp NYjzbYhuUW6qaXLpeIlwdiCxZjDBb5QpezR5MzmgdIhwe3Cqb4L5cIF1cW:w M{TjOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{SxOVQyLz5{M{O0NVU1OTxxYU6=
JEKO-1 M1jRZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTsNVAh|ryP MXK3NkBp NHX3ZW9KdmirYnn0bY9vKG:oIIDyc4xq\mW{YYTpc44he2yrZ3j0cJk> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN2MUW0NUc,OjN|NEG1OFE9N2F-
JEKO-1 NFj0d5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYG1JO69VQ>? NGDKenY4OiCq M3K3TYRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5NkKyNEc,OjN4N{[yNlA9N2F-
MAVER-1 NGLBSpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXBOUDPxE1? NHzMdmg4OiCq MmDq[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> NFriW2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[3OlIzOCd-MkO2O|YzOjB:L3G+
MINO NEHYW3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGO4NmE2KM7:TR?= MWq3NkBp M3WyeoRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> NYGxR|J3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2O|YzOjBpPkKzOlc3OjJyPD;hQi=>
SP53 M4DYS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXkNE4yKM7:TR?= MYq3NkBp NGPjdFNld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ NWfGWVVyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2O|YzOjBpPkKzOlc3OjJyPD;hQi=>
HH M1fXcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV2xNEDPxE1? NUm3R|B5PzJiaB?= NEW0TYFFVVOR M4TwdGlv\HWldHnvckBw\iCjcH;weI9{cXNic3zp[4h1dHl? NGjvOXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiwNVk2QSd-MkK4NFE6PTl:L3G+
Myla MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\nd3ExOTBizszN MVW3NkBp M2PhU2ROW09? MYnkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| NF;PWJg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiwNVk2QSd-MkK4NFE6PTl:L3G+
SR786 Mo\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnlNnUyOCEQvF2= MVq3NkBp NVPpcJZHTE2VTx?= NIToWnVld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyMUm1PUc,OjJ6MEG5OVk9N2F-
HuT78 NFHSc2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUOxNEDPxE1? MW[3NkBp MUjEUXNQ NWHzVGpJ\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> MmDvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
MJ NGTSb4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3K0WFExKM7:TR?= MUG3NkBp MlLqSG1UVw>? MWXkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| M1vmfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OECxPVU6Lz5{MkiwNVk2QTxxYU6=
DERL7 NHfle|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV[5NI1xOTBizszN M1\icFczKGh? NITxXFdFVVOR NFjYN5Vld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MmPCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
L1236 NIHoV4JHfW6ldHnvckBCe3OjeR?= NFLuOWcyOCEQvF2= NGGwZoUzKGh? NV\JT2huUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L428 MWfGeY5kfGmxbjDBd5NigQ>? MYqxNEDPxE1? Ml\QNkBp NV7pe3lGUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u MnjlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
L591 NF\Sbm9HfW6ldHnvckBCe3OjeR?= M3fVbVExKM7:TR?= NX\rUnN6OiCq M{LaNmlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= NEnaZ|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKxNFg4Pyd-MkKyNVA5Pzd:L3G+
KMH-2 M3nySmZ2dmO2aX;uJGF{e2G7 Ml3rNVAh|ryP NXuzcFY3OiCq NILwe5pKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= M1vofFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
L1236 M3i5RWZ2dmO2aX;uJGF{e2G7 NFnyR5M2KM7:TR?= MWCyOEBp MUHCcI9kc3Nic3XjdoV1cW:wIH;mJJRp\SCFQ1y1 NVryWZNtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNVA5PzdpPkKyNlExQDd5PD;hQi=>
L591 M2XNOmZ2dmO2aX;uJGF{e2G7 NFv4TXM2KM7:TR?= MV2yOEBp NFrjOI9DdG:la4Ogd4VkemW2aX;uJI9nKHSqZTDDR2w2 M3zoRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
L1236 NFnVPHJCeG:ydH;zbZMhSXO|YYm= NEHVSlA2KM7:TR?= NEK3ZXUzPCCq M4\HO2lv\HWldHnvckBw\iCjcH;weI9{cXN? NFjqSWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKxNFg4Pyd-MkKyNVA5Pzd:L3G+
L591 NW\VWJg5SXCxcITvd4l{KEG|c3H5 M4rmN|Uh|ryP Mmf1NlQhcA>? NELnT2FKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| M4TK[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
U-87MG M1\6dmZ2dmO2aX;uJGF{e2G7 MWKxNFAhdk1? NHnTWFUzPCCq NHTaZnVFVVOR MVfJcohq[mm2aX;uJI9nKCClZXzsJI1q\3KjdHnvci=> M4jXfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEe5OlA6Lz5{MkC3PVYxQTxxYU6=
SW1783 M1ryRmZ2dmO2aX;uJGF{e2G7 MYixNFAhdk1? MWCyOEBp NWTIWIJ[TE2VTx?= MofxTY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> MlfVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{m2NFkoRjJ{MEe5OlA6RC:jPh?=
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SW1783 NULnR3A3TnWwY4Tpc44hSXO|YYm= Mm\WOUDPxE1? MnnDNlQhcA>? NH\rNYdFVVOR M{XyNWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6 Ml7RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJyN{m2NFkoRjJ{MEe5OlA6RC:jPh?=
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LAN-5 MkHhdWhVWyCjc4PhfS=> M371e5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= MkfmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SUDHL6 NF\sO2RCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M2jrdlczKGi{cx?= M2m2UmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2XETGw3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDDR2s5KGG|c3H5MEBKSzVyIE2gNE43PSEQvF2u M3z0ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUO0PVM3Lz5{OUWzOFk{PjxxYU6=
RPMI8226 NWfSdo1[SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NVS0R25qPzJiaILz Mlq1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUUF3JPFIzPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gOU41QSEQvF2u MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV|NEmzOkc,Ojl3M{S5N|Y9N2F-
Raji M4O3dWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mnn2O|IhcHK| NFja[FJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLhbokh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEmuPVUh|ryPLh?= M1OwVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUO0PVM3Lz5{OUWzOFk{PjxxYU6=
SU-DHL6 NUX4bYU4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX30SIRET3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hW1VvRFjMOkBk\WyuczDifUBE\WyuVHn0[ZIuT2yxIHHzd4F6NCCJSUWwJF0hOC5yNEKg{txONg>? MkHUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4MEG5PVEoRjJ7NkCxPVkyRC:jPh?=
MOLM13 NWPZ[nk{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NU\xe|JKPzJiaILz MmLCS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUW9NVTF|IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JIF{e2G7LDDHTVUxKD1iMT63JO69VS5? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB3M{eyNUc,OzByNUO3NlE9N2F-
MOLM14 NHTyS4FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MW[3NkBpenN? Ml7MS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUW9NVTF2IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JIF{e2G7LDDHTVUxKD1iNj60JO69VS5? MkjlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByNUO3NlEoRjNyMEWzO|IyRC:jPh?=
MOLM14 NIDseoRCdnSrdIXtc5Ih[XO|YYm= M1j1SVExOCCvZz;r[y=> NV7rOmw4OTRiZHH5dy=> MVHBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVQh[2WubIOgfIVvd2e{YX\0[YQhcW5iboWvcpUhdW:3c3WgZZN{\XO|ZXSgZZMhfHWvb4Kg[5Jwf3SqIHnubIljcXSrb36gZZQhOTByIH3nM4toNCCybzDh[I1qdmm|dHXy[YQh\GGrbImgeoliKGejdnHn[UBld3OnZDDmc5IhOTRiZHH5d{BidmRibXXhd5Vz\WRiZHHpcJkh\HW{aX7nJINwdXCxdX7kJIRwe2mwZzDy[YxifGm4ZTD0c{Bkd262cn;s NHLBN3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC1N|czOSd-M{CwOVM4OjF:L3G+
MOLM14 MX;BcpRqfHWvb4KgZZN{[Xl? M3rVfVExOCCvZz;r[y=> NV\tcIExOTRiZHH5dy=> M4X1RmFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUG0yPCClZXzsd{B5\W6xZ4Lh[pRm\CCrbjDueU9vfSCvb4Xz[UBie3Onc4Pl[EBieyCrbnT1Z5Rqd25ib3[gZZBweHSxc3nzJIF1KDFyMDDt[{9s\yxicH:gZYRucW6rc4TldoVlKGSjaXz5JJZq[SCpYY\h[4Uh\G:|ZXSg[o9zKDF2IHThfZMh[W6mIH3lZZN2emWmIHThbYx6KGS3cnnu[{Bkd22yb4Xu[EBld3OrbnegZpkhXFWQRVygZoF{\WRiYYPzZZk> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB3M{eyNUc,OzByNUO3NlE9N2F-
MOLM14 NFvyVJdCdnSrdIXtc5Ih[XO|YYm= M3j3b|ExOCCvZz;r[y=> M3;BUVE1KGSjeYO= NYjl[FAxSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUW9NVTF2IHPlcIx{KHinbn;ndoFnfGWmIHnuJI52N263IH3veZNmKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhfHWvb4KgdJJwdGmoZYLheIlwdiBzMECgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCmYXnsfUB3cWFiZ3H2ZYdmKGSxc3XkJIZweiBzNDDkZZl{KGGwZDDt[YF{fXKnZDDkZYltgSCmdYLpcoch[2:vcH;1coQh\G:|aX7nJIJ6KEurLU[3JIxi[mWubHnu[{Bj[XOnZDDpcY12dm:q M1PUeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEWzO|IyLz5|MEC1N|czOTxxYU6=

... 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

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[2]
- 合并

PI3K实验:

用全CLL和正常B细胞溶解物进行PI3K实验。 进行PI3K ELISA 实验。全细胞抽提物加到PI(4,5)P2 底物和反应 buffer(包含 ATP)的混合物中,在室温下温育。加入 PI(3,4,5)P3 探测器和 EDTA混合,反应终止,在室温下温育1小时。混合物转移到PI3K ELISA板上,再温育1小时。 冲洗反应板,然后和第二探测器再温育30分钟。再次冲洗反应板, 加入3,3′,5,5′-四甲基联苯胺溶液 ,反应5分钟,加入H2SO4 终止反应。在450纳米处读数。
细胞实验:[2]
- 合并
  • Cell lines: CLL B 细胞或健康志愿者的T细胞或NK细胞
  • Concentrations: 0.01-100 μM
  • Incubation Time: 48小时
  • Method: 进行MTT实验测定细胞毒性。1×105个细胞和CAL-101一起温育。加入MTT试剂, 再次温育20小时,然后用溶于PBS的硫酸鱼精蛋白冲洗。加入DMSO, 用分光光度计在540纳米处测定吸光度。使用膜联蛋白/PI液式细胞计检查在不同时间点测定细胞存活力,分析数据。每个样本至少计数104个细胞。以全部阳性细胞与未处理细胞之比百分数的形式来表示实验结果。加入100 μM Z-VAD检测caspase-依赖的细胞凋亡。加入 1 μg/mL CD40L, 800 U/mL IL-4, 50 ng/mL BAFF, 20 ng/mL TNF-α测定存活信号, 或者共培养在纤连蛋白或 HS-5 细胞系基质包被的板上。 基质共培养 在75cm2培养瓶 (80%-100% 融合率) 培养24 小时,然后加入CLL细胞。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 83 mg/mL warmed (199.79 mM)
Ethanol 23 mg/mL (55.36 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+20%PEG 300+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 415.42
化学式

C22H18FN7O

CAS号 870281-82-6
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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 --

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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 Signaling Pathway Map

PI3K Inhibitors with Unique Features

相关PI3K产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID