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192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 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPoSG1UVw>? NEfZbVJKSzVyPUKwMlQh|ryP MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl7OUO1Nkc,OjV7OUmzOVI9N2F-
CLL PBMCs MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTwZVQ3TE2VTx?= MlrUTWM2OD1{Lkmgcm0> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTlzN{K2O{c,OjV7MUeyOlc9N2F-
U266 M33ze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnyNVhsPDBizszN M4jQVVQ5KGh? MnLRO|kvPSViaX7obYJqfGmxbjDyZZRm MnrVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{mzN|IoRjJ3M{O5N|MzRC:jPh?=
K562 MYXGeY5kfGmxbjDBd5NigQ>? NF\DflMyKM7:TR?= MUSzJIg> M1L6WmlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= NYDO[Yc2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
K562 NGPjeZRHfW6ldHnvckBCe3OjeR?= MY[xJO69VQ>? M2TzdlMhcA>? M4\HcmlvcGmkaYTpc44hd2ZiUEewV|ZMKHCqb4PwbI9zgWyjdHnvci=> NXXrXm9rRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
K562 M2DjbmZ2dmO2aX;uJGF{e2G7 MYqxJO69VQ>? NHXSZ2M{KGh? MoLPTY5pcWKrdHnvckBw\iCJU1uzJJBpd3OyaH;yfYxifGmxbh?= NH\XdZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
K562 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofvNUDPxE1? MYS3NkBp MWDJcohq[mm2aX;uJI9nKHC{b3zp[oVz[XSrb36= M1TEVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Primary AML cell NUTp[3F{TnWwY4Tpc44hSXO|YYm= M2Dy[lEh|ryP NHnDR|c{KGh? NUj2T4Z2UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u NXvHc|hWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
Primary AML cell MVTGeY5kfGmxbjDBd5NigQ>? NY\wWI9[OSEQvF2= M{fST|MhcA>? MoDxTY5pcWKrdHnvckBw\iCSN{DTOmsheGixc4Doc5J6dGG2aX;u M33YeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Primary AML cell M17ZXmZ2dmO2aX;uJGF{e2G7 Ml7sNUDPxE1? M1v5TVMhcA>? NHfDNXdKdmirYnn0bY9vKG:oIFfTT|MheGixc4Doc5J6dGG2aX;u NFrEfYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Primary AML cell NFfpUG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\UNlEh|ryP NW\xT25GOyCq MV3TeZBxemW|c3nvckBw\iC{Ul7BJJN6dnSqZYPpdy=> M{HRbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Microglia M4rrR2Z2dmO2aX;uJGF{e2G7 MUO1JO69VQ>? MUGxNEBp NWTXZpdOTE2VTx?= NEC0ZnNF\WO{ZXHz[UBw\iCWTl\hJJNm[3KndHnvckBnem:vIFzQV{1{fGmvdXzheIVlKCCyMUGw{tRFQTFyQT;EPVExSSCvaXPyc4dtcWF? NXfiV5l7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NlU3QDRpPkK0OlI2Pjh2PD;hQi=>
Primary CLL cell MYnGeY5kfGmxbjDBd5NigQ>? MUGxJO69VQ>? M33PXFE2KG2rbh?= M4LPbWROW09? MoDFRoxw[2u|IFLDVk1qdmS3Y3XkJGxEWDFic3XybY5mNTViYXP0bZZifGmxbh?= M1yyeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NlM{Lz5{NECwPVI{OzxxYU6=
JEKO-1 MlzoSpVv[3Srb36gRZN{[Xl? M1PiflEh|ryP NVHsU5R3PzJiaB?= M37E[2lvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDpckBK\01vc4TpcZVt[XSnZDDKSWtQNTF? NIexe3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O0NVU1OSd-MkOzOFE2PDF:L3G+
Granta-519 NWfSV|JjTnWwY4Tpc44hSXO|YYm= M37oWFEh|ryP M4CybFIhcA>? NV;WcmZsUW6qaXLpeIlwdiCxZjDBb5QpfDNyODmgdIhwe3Cqb4L5cIF1cW:w MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN2MUW0NUc,OjN|NEG1OFE9N2F-
Granta-519 NFPnNppHfW6ldHnvckBCe3OjeR?= M4KzNVEh|ryP MXWyJIg> NH\iZ|NKdmirYnn0bY9vKG:oIFHreEh{PDd|KTDwbI9{eGixconsZZRqd25? M3nONlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{SxOVQyLz5{M{O0NVU1OTxxYU6=
JEKO-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXe2V5Y3OTBizszN NGjGWGY4OiCq MlfyTY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;uJJNtcWeqdHz5 MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN2MUW0NUc,OjN|NEG1OFE9N2F-
JEKO-1 M1PDNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXqOUDPxE1? NWfOepJPPzJiaB?= MkfZ[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> NXzoVphpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2O|YzOjBpPkKzOlc3OjJyPD;hQi=>
MAVER-1 NIKxVXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPpbI82KM7:TR?= NEjCWnA4OiCq M{jufIRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> NFzNWXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[3OlIzOCd-MkO2O|YzOjB:L3G+
MINO NIjuWmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUL6fI4yPSEQvF2= NYTjdHVHPzJiaB?= M1foXoRw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> NIm4c|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[3OlIzOCd-MkO2O|YzOjB:L3G+
SP53 NUfqXndHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;s[pUxNjFizszN MWm3NkBp NILve2Zld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5NkKyNEc,OjN4N{[yNlA9N2F-
HH MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;Rd3ZuOTBizszN NEK0[nE4OiCq NFLpcm1FVVOR M3P6Vmlv\HWldHnvckBw\iCjcH;weI9{cXNic3zp[4h1dHl? MnfUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
Myla NVjJemEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU[xNEDPxE1? MUG3NkBp NG\DfmdFVVOR MXHkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MlXmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
SR786 MlHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnvOI0yOCEQvF2= M1HaXVczKGh? NXLF[4xGTE2VTx?= MkXo[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NVS1NJhCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
HuT78 NI\KeppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XEcFExKM7:TR?= NVHFfnJ[PzJiaB?= NETmOpdFVVOR Ml[z[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyMUm1PUc,OjJ6MEG5OVk9N2F-
MJ NF;HU5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWOxNEDPxE1? MUG3NkBp NIHER3hFVVOR MXHkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyMUm1PUc,OjJ6MEG5OVk9N2F-
DERL7 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv6W3kyOCEQvF2= M2Txc|czKGh? NHnzVlVFVVOR NF;ZPXNld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MkHSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
L1236 MYnGeY5kfGmxbjDBd5NigQ>? M1ntblExKM7:TR?= MlnaNkBp MVXJcohq[mm2aX;uJI9nKEGtdDDwbI9{eGixconsZZRqd25? NXPsbHNWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNVA5PzdpPkKyNlExQDd5PD;hQi=>
L428 NVjmPZN1TnWwY4Tpc44hSXO|YYm= MYWxNEDPxE1? M324OFIhcA>? M3y3fGlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L591 MUTGeY5kfGmxbjDBd5NigQ>? NWT6N251OTBizszN MYWyJIg> NV;wcpRrUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u MoHwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
KMH-2 M33SR2Z2dmO2aX;uJGF{e2G7 MUCxNEDPxE1? NU\tSZRwOiCq M{LQXmlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L1236 Ml3TSpVv[3Srb36gRZN{[Xl? MYW1JO69VQ>? MkHDNlQhcA>? MUXCcI9kc3Nic3XjdoV1cW:wIH;mJJRp\SCFQ1y1 MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L591 MkDZSpVv[3Srb36gRZN{[Xl? NVPJTpVYPSEQvF2= MluyNlQhcA>? MUDCcI9kc3Nic3XjdoV1cW:wIH;mJJRp\SCFQ1y1 Mn3MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
L1236 NFXMOJhCeG:ydH;zbZMhSXO|YYm= M1m3SlUh|ryP NGDBSZIzPCCq NF3y[oVKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L591 M{XteGFxd3C2b4Ppd{BCe3OjeR?= M2Dxc|Uh|ryP MViyOEBp MXjJcoR2[3Srb36gc4Yh[XCxcITvd4l{ NEDQPFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKxNFg4Pyd-MkKyNVA5Pzd:L3G+
U-87MG NVvQW4lMTnWwY4Tpc44hSXO|YYm= MlzMNVAxKG6P NUXu[ItCOjRiaB?= NH;PeHVFVVOR Mm\XTY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
SW1783 Mor3SpVv[3Srb36gRZN{[Xl? NFXCNogyODBibl2= NV7JXYxmOjRiaB?= NIS0[mxFVVOR M2rUO2lvcGmkaYTpc44hd2ZiIHPlcIwhdWmpcnH0bY9v MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
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SW1783 MXrGeY5kfGmxbjDBd5NigQ>? NXnuWpF5PSEQvF2= MVqyOEBp NUjTVpRRTE2VTx?= Ml[5TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIIP1ZpN1[W62aXHscJk> NISzRpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkC3PVYxQSd-MkKwO|k3ODl:L3G+
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LAN-5 NEnWNHZyUFSVIHHzd4F6 MoXrdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SUDHL6 NVXHVXdGSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M4qzO|czKGi{cx?= NXzpW2VxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTWWRJVDZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNEUzhiYYPzZZktKEmFNUCgQUAxNjZ3IN88UU4> M3XmVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUO0PVM3Lz5{OUWzOFk{PjxxYU6=
RPMI8226 MUnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MlrmO|IhcHK| MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKSTVm4NlI3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTC1MlQ6KM7:TT6= M{W2dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUO0PVM3Lz5{OUWzOFk{PjxxYU6=
Raji NU\2UIVmSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NI\vUoY4OiCqcoO= Mn;5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUYXrpJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB7Lkm1JO69VS5? NInqNVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWzOFk{Pid-Mkm1N|Q6OzZ:L3G+
SU-DHL6 MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1vvfGdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJHNWNUSKTE[gZ4VtdHNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhT0l3MDC9JFAvODR{IN88UU4> NXfzbYJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2NFE6QTFpPkK5OlAyQTlzPD;hQi=>
MOLM13 MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1zRSFczKGi{cx?= NGrrTYxIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOV0yPMUOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[XO|YYmsJGdKPTBiPTCxMlch|ryPLh?= NWi5cJBxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CwOVM4OjFpPkOwNFU{PzJzPD;hQi=>
MOLM14 MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1uwd|czKGi{cx?= MXLHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNU2xOOTRiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZZN{[XluIFfJOVAhRSB4LkSg{txONg>? MljWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByNUO3NlEoRjNyMEWzO|IyRC:jPh?=
MOLM14 NWLncJlvSW62aYT1cY9zKGG|c3H5 M3j0SFExOCCvZz;r[y=> NWfSR5FYOTRiZHH5dy=> MUPBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVQh[2WubIOgfIVvd2e{YX\0[YQhcW5iboWvcpUhdW:3c3WgZZN{\XO|ZXSgZZMhfHWvb4Kg[5Jwf3SqIHnubIljcXSrb36gZZQhOTByIH3nM4toNCCybzDh[I1qdmm|dHXy[YQh\GGrbImgeoliKGejdnHn[UBld3OnZDDmc5IhOTRiZHH5d{BidmRibXXhd5Vz\WRiZHHpcJkh\HW{aX7nJINwdXCxdX7kJIRwe2mwZzDy[YxifGm4ZTD0c{Bkd262cn;s NESye|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC1N|czOSd-M{CwOVM4OjF:L3G+
MOLM14 MWDBcpRqfHWvb4KgZZN{[Xl? MljENVAxKG2pL3vn MUixOEBl[Xm| M3e4SWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUG0yPCClZXzsd{B5\W6xZ4Lh[pRm\CCrbjDueU9vfSCvb4Xz[UBie3Onc4Pl[EBieyCrbnT1Z5Rqd25ib3[gZZBweHSxc3nzJIF1KDFyMDDt[{9s\yxicH:gZYRucW6rc4TldoVlKGSjaXz5JJZq[SCpYY\h[4Uh\G:|ZXSg[o9zKDF2IHThfZMh[W6mIH3lZZN2emWmIHThbYx6KGS3cnnu[{Bkd22yb4Xu[EBld3OrbnegZpkhXFWQRVygZoF{\WRiYYPzZZk> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB3M{eyNUc,OzByNUO3NlE9N2F-
MOLM14 MmnCRY51cXS3bX;yJIF{e2G7 Mn\pNVAxKG2pL3vn M2DrfFE1KGSjeYO= MnToRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV;MUVE1KGOnbHzzJJhmdm:pcnHmeIVlKGmwIH71M452KG2xdYPlJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geJVud3JicILvcIln\XKjdHnvckAyODBibXevb4ctKHCxIHHkcYlvcXO2ZYLl[EBl[WmueTD2bYEh\2G4YXflJIRwe2WmIH\vdkAyPCCmYYnzJIFv\CCvZXHzeZJm\CCmYXnsfUBlfXKrbnegZ49ueG:3bnSg[I9{cW6pIHL5JGtqNTZ5IHzhZoVtdGmwZzDiZZNm\CCrbX31co9p M124U|xiKHSjcnfleF0oZ2KuYX7rK{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