Idelalisib

目录号:S2226 别名: CAL-101, GS-1101 中文名称:艾代拉里斯,艾代拉利司

仅限科研使用

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。

Idelalisib  Chemical Structure

CAS: 870281-82-6

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
大包装 有超大折扣
大剂量询单有大折扣!

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Idelalisib 发表文献231篇:

产品安全说明书

PI3K抑制剂选择性比较

相关PI3K产品

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 M1zneGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzmelBFVVOR M4nadmlEPTB;MkCuOEDPxE1? MlqxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7OUmzOVIoRjJ3OUm5N|UzRC:jPh?=
CLL PBMCs M4DKSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTGSG1UVw>? NU\4V2N1UUN3ME2yMlkhdk1? M4[zVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUG3NlY4Lz5{NUmxO|I3PzxxYU6=
U266 NV20PXVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4WwV|QxKM7:TR?= MkHWOFghcA>? NYXtUnhkPzlwNTWgbY5pcWKrdHnvckBz[XSn MknpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|M{mzN|IoRjJ3M{O5N|MzRC:jPh?=
K562 NHKycWRHfW6ldHnvckBCe3OjeR?= MWCxJO69VQ>? M2TjVFMhcA>? MoHmTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w MlPMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUS3O|UoRjJ3MEG0O|c2RC:jPh?=
K562 Mn22SpVv[3Srb36gRZN{[Xl? MnewNUDPxE1? NH3EUoE{KGh? M2T0WmlvcGmkaYTpc44hd2ZiUEewV|ZMKHCqb4PwbI9zgWyjdHnvci=> NGn3elk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
K562 MVTGeY5kfGmxbjDBd5NigQ>? M12zNVEh|ryP NYX6NIlLOyCq M2PT[GlvcGmkaYTpc44hd2ZiR2PLN{BxcG:|cHjvdplt[XSrb36= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTBzNEe3OUc,OjVyMUS3O|U9N2F-
K562 M{HwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTJZnR5OSEQvF2= NEW1OpE4OiCq MmPITY5pcWKrdHnvckBw\iCycn;sbYZmemG2aX;u M{PLWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Primary AML cell M1\zdGZ2dmO2aX;uJGF{e2G7 MoO4NUDPxE1? NF;rPYE{KGh? NX\t[GcyUW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u M3y1RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEG0O|c2Lz5{NUCxOFc4PTxxYU6=
Primary AML cell Mo[5SpVv[3Srb36gRZN{[Xl? NG\TTZAyKM7:TR?= MVKzJIg> M4\xOGlvcGmkaYTpc44hd2ZiUEewV|ZMKHCqb4PwbI9zgWyjdHnvci=> MnjzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUS3O|UoRjJ3MEG0O|c2RC:jPh?=
Primary AML cell MUfGeY5kfGmxbjDBd5NigQ>? NHvPXJgyKM7:TR?= M33zdVMhcA>? MmPZTY5pcWKrdHnvckBw\iCJU1uzJJBpd3OyaH;yfYxifGmxbh?= MkXOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUS3O|UoRjJ3MEG0O|c2RC:jPh?=
Primary AML cell NXnHZ|h2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PZblEh|ryP MlLvN{Bp M36yXXN2eHC{ZYPzbY9vKG:oIILSUmEhe3mwdHjld4l{ MnfJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUS3O|UoRjJ3MEG0O|c2RC:jPh?=
Microglia NWPtdXlMTnWwY4Tpc44hSXO|YYm= M1:0WVUh|ryP NULBcWNPOTBiaB?= MX\EUXNQ M4nDTGRm[3KnYYPlJI9nKFSQRnGgd4VkemW2aX;uJIZzd21iTGDTMZN1cW23bHH0[YQhKHBzMUFOuGQ6OTCDL1S5NVBCKG2rY4Lv[4xq[Q>? NYD6dFd1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2NlU3QDRpPkK0OlI2Pjh2PD;hQi=>
Primary CLL cell M4LvOGZ2dmO2aX;uJGF{e2G7 MlPNNUDPxE1? MmHHNVUhdWmw NXftbJVDTE2VTx?= NIrse2ZDdG:la4OgRmNTNWmwZIXj[YQhVEOSMTDz[ZJqdmVvNTDhZ5RqfmG2aX;u Ml7GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmyN|MoRjJ2MEC5NlM{RC:jPh?=
JEKO-1 MW\GeY5kfGmxbjDBd5NigQ>? NHyzXVEyKM7:TR?= MYG3NkBp MkO1TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHnuJGloVS2|dHnteYxifGWmIFrFT28uOQ>? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN2MUW0NUc,OjN|NEG1OFE9N2F-
Granta-519 NGjyXJNHfW6ldHnvckBCe3OjeR?= MXyxJO69VQ>? NEjWeXYzKGh? NHfPWJhKdmirYnn0bY9vKG:oIFHreEh1OzB6KTDwbI9{eGixconsZZRqd25? NXzNOWVVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOFE2PDFpPkKzN|QyPTRzPD;hQi=>
Granta-519 NXnhUpE5TnWwY4Tpc44hSXO|YYm= MmDhNUDPxE1? NX\WdHZwOiCq M1nNUGlvcGmkaYTpc44hd2ZiQXv0LJM1PzNrIIDoc5NxcG:{eXzheIlwdg>? M4Ljc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{SxOVQyLz5{M{O0NVU1OTxxYU6=
JEKO-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWT4TpNCOTBizszN MWi3NkBp M3fGemlvcGmkaYTpc44hd2ZicILvcIln\XKjdHnvckB{dGmpaITsfS=> NVPHVmRxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzOFE2PDFpPkKzN|QyPTRzPD;hQi=>
JEKO-1 NULwdGpJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HOTlUh|ryP NVSwRnhmPzJiaB?= NFrFfoZld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ NVXnRW06RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2O|YzOjBpPkKzOlc3OjJyPD;hQi=>
MAVER-1 MmLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPQOUDPxE1? Mlq2O|IhcA>? NWfwOY1u\G:nczDuc5QhcW6mdXPlJINmdGxiY4njcIUh[XK{ZYP0JI9zKGGyb4D0c5Nqew>? Mn\RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4N{[yNlAoRjJ|Nke2NlIxRC:jPh?=
MINO NVm5RXlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXPN|U2KM7:TR?= NGK0UZE4OiCq NFTx[3pld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5NkKyNEc,OjN4N{[yNlA9N2F-
SP53 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPr[JR2OC5zIN88US=> NHni[XU4OiCq M1jqT4Rw\XNibn;0JIlv\HWlZTDj[YxtKGO7Y3zlJIFzemW|dDDvdkBieG:ydH;zbZM> M4P4UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nke2NlIxLz5{M{[3OlIzODxxYU6=
HH NWjGOGxbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFX5Om8yOCEQvF2= MYC3NkBp MkHkSG1UVw>? MmLNTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyC|bHnnbJRtgQ>? NH7weoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkiwNVk2QSd-MkK4NFE6PTl:L3G+
Myla M3nM[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOxNEDPxE1? NG\OfGY4OiCq MYfEUXNQ M3uydYRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= NWDwNokzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
SR786 NEjERoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPoNVAh|ryP NF3KSHM4OiCq NU\lcphJTE2VTx?= MoL5[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhyMUm1PUc,OjJ6MEG5OVk9N2F-
HuT78 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnm1NVAh|ryP NFqxO3M4OiCq Mlf1SG1UVw>? M2nxUIRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= M1HoW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OECxPVU6Lz5{MkiwNVk2QTxxYU6=
MJ NITPRZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqxNEDPxE1? NXHLWolZPzJiaB?= NVjtRYNmTE2VTx?= NWH5PVBZ\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> Ml;hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
DERL7 Mn;KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\1dnMyOCEQvF2= M1La[|czKGh? NVXl[mhHTE2VTx?= MYTkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| M17BWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OECxPVU6Lz5{MkiwNVk2QTxxYU6=
L1236 NXLTS4FjTnWwY4Tpc44hSXO|YYm= NEH5UVUyOCEQvF2= NH7rRYIzKGh? MlzKTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L428 MWTGeY5kfGmxbjDBd5NigQ>? MmntNVAh|ryP NV\pZYM3OiCq NILQTm9KdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36= NVT6VFM5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNVA5PzdpPkKyNlExQDd5PD;hQi=>
L591 M2C2SGZ2dmO2aX;uJGF{e2G7 NUXRUItOOTBizszN NUi4bG9YOiCq M1HUU2lvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= M4q2VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
KMH-2 MUPGeY5kfGmxbjDBd5NigQ>? M2jIV|ExKM7:TR?= MV6yJIg> MoS5TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L1236 M4jRVmZ2dmO2aX;uJGF{e2G7 NXL6OI1xPSEQvF2= M1vzflI1KGh? MlzXRoxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> NFrQTJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKxNFg4Pyd-MkKyNVA5Pzd:L3G+
L591 NFnyUG9HfW6ldHnvckBCe3OjeR?= MUW1JO69VQ>? NFzFRo8zPCCq Mnf0Roxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> NWj0UoVwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNVA5PzdpPkKyNlExQDd5PD;hQi=>
L1236 MYHBdI9xfG:|aYOgRZN{[Xl? MYG1JO69VQ>? MU[yOEBp MYLJcoR2[3Srb36gc4Yh[XCxcITvd4l{ MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L591 NELiRoNCeG:ydH;zbZMhSXO|YYm= M1mwN|Uh|ryP MX:yOEBp NHPVcXVKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m| NEPRW4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKxNFg4Pyd-MkKyNVA5Pzd:L3G+
U-87MG M2HmXWZ2dmO2aX;uJGF{e2G7 NIjQdHoyODBibl2= NF;mV4gzPCCq MXjEUXNQ MVrJcohq[mm2aX;uJI9nKCClZXzsJI1q\3KjdHnvci=> NXraVGVuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwO|k3ODlpPkKyNFc6PjB7PD;hQi=>
SW1783 NHrEdlhHfW6ldHnvckBCe3OjeR?= NWLQUHpTOTByIH7N MYqyOEBp NV;GenNETE2VTx?= M3j2OGlvcGmkaYTpc44hd2ZiIHPlcIwhdWmpcnH0bY9v MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
U-87MG NHH2TJJHfW6ldHnvckBCe3OjeR?= NEnNW2M2KM7:TR?= NHXYTI0zPCCq M{C3dGROW09? NIK2WoVKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? NV7QNWFiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwO|k3ODlpPkKyNFc6PjB7PD;hQi=>
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B-cells NUnF[oZVTnWwY4Tpc44h[XO|YYm= MUjJcohq[mm2aX;uJI9nKFCLM1vk[Yx1[SCrbjDCMYNmdGy|IHL5JJBzd2yrZnXyZZRqd25iYYPzZZktKEmFNUCgQUAxNjByNkGg{txONg>? NHfJcVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmyOFY5QCd-MkK5NlQ3QDh:L3G+
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MV4-11 Mny4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NYDORZdzOyCmYYnz NEnlNZpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3WOE0yOSClZXzsd{Bi\nSncjCzJIRigXNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3MDC9JFYvOyEQvF2u NE\MelA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{e3OFEzPyd-Mke3O|QyOjd:L3G+
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insect cells M3rxZmZ2dmO2aX;uJIF{e2G7 NH;yR2VKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIH\1cIwhdGWwZ4ToJGhqey22YXfn[YQhWEl|S3LleIEh\XiycnXzd4VlKGmwIHnud4VkfCClZXzsd{whUUN3MDC9JFAvPTZ3IN88UU4> NEnhTnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{i0OlQ2OSd-Mke4OFY1PTF:L3G+
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Pfeiffer M2[xOWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NYiycnI5PzJiaILz NHv1SnVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDm[Yln\mW{IHPlcIx{KG2nYYP1doVlKGGodHXyJFczKGi{czDifUBidGGvYYKgZox2\SCjc4PhfUwhUUN3MDC9JFYvQCEQvF2u MoT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6NE[0OVEoRjJ5OES2OFUyRC:jPh?=
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Raji NEf3[oZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MVy3NkBpenN? Mn;RRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUYXrpJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkCwPVk2KM7:TT6= M3PXXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{K1OlAyLz5{OEOyOVYxOTxxYU6=
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Pfeiffer NHvCeodIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWiyNpIyT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hWG[naX\m[ZIh[2WubIOgZpkhS0ONODDhd5NigSxiR1m1NEA:KDBwN{Sg{txONg>? NEf1SGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEizOVgxPSd-Mki4N|U5ODV:L3G+
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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

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]
  • 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]
  • 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。

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

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 Completed Drug: Idelalisib Follicular Non-Hodgkin''s Lymphoma Refractory Gilead Sciences May 25 2018 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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操作手册

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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