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

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233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 MlXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnwbmxxTE2VTx?= MkTjTWM2OD1{MD60JO69VQ>? Ml6yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7OUmzOVIoRjJ3OUm5N|UzRC:jPh?=
CLL PBMCs Ml6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PFN2ROW09? M2HhTWlEPTB;Mj65JI5O MmjvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7MUeyOlcoRjJ3OUG3NlY4RC:jPh?=
U266 NEDV[VBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYm0NEDPxE1? NEjXUYE1QCCq Mn\UO|kvPSViaX7obYJqfGmxbjDyZZRm NX3VdGFiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzN|k{OzJpPkK1N|M6OzN{PD;hQi=>
K562 MXHGeY5kfGmxbjDBd5NigQ>? MoC2NUDPxE1? MWSzJIg> MoLqTY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:w NYDtTZJGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNVQ4PzVpPkK1NFE1Pzd3PD;hQi=>
K562 M2DNPWZ2dmO2aX;uJGF{e2G7 MV:xJO69VQ>? NGrsO4E{KGh? NIrZN5pKdmirYnn0bY9vKG:oIGC3NHM3UyCyaH;zdIhwenmuYYTpc44> NFPxXm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
K562 NWH3flJETnWwY4Tpc44hSXO|YYm= MUixJO69VQ>? MmezN{Bp NIm1bGJKdmirYnn0bY9vKG:oIFfTT|MheGixc4Doc5J6dGG2aX;u MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTBzNEe3OUc,OjVyMUS3O|U9N2F-
K562 NVLaPYs3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWexJO69VQ>? MUG3NkBp NWXzUoNSUW6qaXLpeIlwdiCxZjDwdo9tcW[ncnH0bY9v NF;m[YI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Primary AML cell MkO3SpVv[3Srb36gRZN{[Xl? NVvsRXZvOSEQvF2= M1PkSFMhcA>? M2LLVmlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTBzNEe3OUc,OjVyMUS3O|U9N2F-
Primary AML cell M4T4TmZ2dmO2aX;uJGF{e2G7 NV;w[ZZSOSEQvF2= MYGzJIg> NEfMUoVKdmirYnn0bY9vKG:oIGC3NHM3UyCyaH;zdIhwenmuYYTpc44> Mkf5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUS3O|UoRjJ3MEG0O|c2RC:jPh?=
Primary AML cell M3jTdmZ2dmO2aX;uJGF{e2G7 NEjCV5IyKM7:TR?= MlK0N{Bp NI\OTYhKdmirYnn0bY9vKG:oIFfTT|MheGixc4Doc5J6dGG2aX;u MmrZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMUS3O|UoRjJ3MEG0O|c2RC:jPh?=
Primary AML cell NF7GVWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGqwbW8yKM7:TR?= MnW5N{Bp MUDTeZBxemW|c3nvckBw\iC{Ul7BJJN6dnSqZYPpdy=> NIDYcJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCxOFc4PSd-MkWwNVQ4PzV:L3G+
Microglia M4nLcmZ2dmO2aX;uJGF{e2G7 MYO1JO69VQ>? MY[xNEBp NVn2UIlkTE2VTx?= NHz5PXBF\WO{ZXHz[UBw\iCWTl\hJJNm[3KndHnvckBnem:vIFzQV{1{fGmvdXzheIVlKCCyMUGw{tRFQTFyQT;EPVExSSCvaXPyc4dtcWF? M3jJPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkK1Olg1Lz5{NE[yOVY5PDxxYU6=
Primary CLL cell MlTmSpVv[3Srb36gRZN{[Xl? M4LiRVEh|ryP MYexOUBucW5? MUjEUXNQ MnHVRoxw[2u|IFLDVk1qdmS3Y3XkJGxEWDFic3XybY5mNTViYXP0bZZifGmxbh?= NIDscZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVI{Oyd-MkSwNFkzOzN:L3G+
JEKO-1 MmGzSpVv[3Srb36gRZN{[Xl? MWixJO69VQ>? Mlr1O|IhcA>? Mlz0TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHnuJGloVS2|dHnteYxifGWmIFrFT28uOQ>? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN2MUW0NUc,OjN|NEG1OFE9N2F-
Granta-519 NX\TepZ1TnWwY4Tpc44hSXO|YYm= MVixJO69VQ>? MUWyJIg> NE\QZVVKdmirYnn0bY9vKG:oIFHreEh1OzB6KTDwbI9{eGixconsZZRqd25? Ml;iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|NEG1OFEoRjJ|M{SxOVQyRC:jPh?=
Granta-519 MV3GeY5kfGmxbjDBd5NigQ>? NXnyN2d{OSEQvF2= NYrYZoJiOiCq MYXJcohq[mm2aX;uJI9nKEGtdDjzOFc{MSCyaH;zdIhwenmuYYTpc44> M1TtelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{SxOVQyLz5{M{O0NVU1OTxxYU6=
JEKO-1 NGfXeXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjMb412OTBizszN MV[3NkBp MXzJcohq[mm2aX;uJI9nKHC{b3zp[oVz[XSrb36gd4xq\2i2bIm= NH3zSng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O0NVU1OSd-MkOzOFE2PDF:L3G+
JEKO-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;6dFUh|ryP M1LkZ|czKGh? MnLQ[I9meyCwb4SgbY5lfWOnIHPlcIwh[3mlbHWgZZJz\XO2IH;yJIFxd3C2b4Ppdy=> MkjiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4N{[yNlAoRjJ|Nke2NlIxRC:jPh?=
MAVER-1 M4HESGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnkRoo2KM7:TR?= NWDYVZpqPzJiaB?= NE\H[VZld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ MoPTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4N{[yNlAoRjJ|Nke2NlIxRC:jPh?=
MINO MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[1JO69VQ>? NHXaOnc4OiCq MVPkc4V{KG6xdDDpcoR2[2ViY3XscEBkgWOuZTDhdpJme3Rib4KgZZBweHSxc3nz MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ5NkKyNEc,OjN4N{[yNlA9N2F-
SP53 MlHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;Wd|AvOSEQvF2= M1v0[FczKGh? NGrUUIpld2W|IH7veEBqdmS3Y3WgZ4VtdCCleXPs[UBienKnc4Sgc5Ih[XCxcITvd4l{ M3O5UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nke2NlIxLz5{M{[3OlIzODxxYU6=
HH M3rHR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm[4NVAh|ryP M2n0NlczKGh? MWrEUXNQ M4XNW2lv\HWldHnvckBw\iCjcH;weI9{cXNic3zp[4h1dHl? NYLZcYJjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
Myla NULxTpFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXFdoMyOCEQvF2= MWO3NkBp M17WXGROW09? NH[wWpFld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz NVvvRlgyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
SR786 M4nPc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfreYkyOCEQvF2= M4\QSFczKGh? NUjwcpZVTE2VTx?= MojU[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= M3\JU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OECxPVU6Lz5{MkiwNVk2QTxxYU6=
HuT78 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVWxNEDPxE1? NV6wPHJ[PzJiaB?= MUPEUXNQ MmO5[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NXG4NHJrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
MJ NGq3SI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXwUHQyOCEQvF2= NF3OSYM4OiCq NX;RN4JSTE2VTx?= NHvDO|hld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz Mln5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MEG5OVkoRjJ{OECxPVU6RC:jPh?=
DERL7 NHTSSmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LEc|ExKM7:TR?= NYfudY5pPzJiaB?= NGPpV3FFVVOR NVLyXJVp\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> NWq2T2l4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NFE6PTlpPkKyPFAyQTV7PD;hQi=>
L1236 M1ywUmZ2dmO2aX;uJGF{e2G7 MXuxNEDPxE1? M2rqeVIhcA>? NXLEVpN7UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJzMEi3O{c,OjJ{MUC4O|c9N2F-
L428 MXPGeY5kfGmxbjDBd5NigQ>? MYWxNEDPxE1? NHnJeJczKGh? M1S5VGlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= NX3xWIN7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNVA5PzdpPkKyNlExQDd5PD;hQi=>
L591 NILmPXFHfW6ldHnvckBCe3OjeR?= MkGzNVAh|ryP NFL4TIczKGh? M3;heGlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbh?= MlPEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
KMH-2 NIH5VmZHfW6ldHnvckBCe3OjeR?= MmnuNVAh|ryP NF63e|gzKGh? NXO3XmM1UW6qaXLpeIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;u NGPrSVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKxNFg4Pyd-MkKyNVA5Pzd:L3G+
L1236 NVi2ToY1TnWwY4Tpc44hSXO|YYm= NXOzbXlNPSEQvF2= MV:yOEBp MmG5Roxw[2u|IIPlZ5JmfGmxbjDv[kB1cGViQ1PMOS=> MkfJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
L591 M2\0O2Z2dmO2aX;uJGF{e2G7 MlLoOUDPxE1? NWX2dZVwOjRiaB?= NV\jXoVOSmyxY3vzJJNm[3KndHnvckBw\iC2aHWgR2NNPQ>? MnfvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
L1236 NYPLcZc6SXCxcITvd4l{KEG|c3H5 M2LadFUh|ryP NXvReIhLOjRiaB?= NWfNbnFrUW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= MlLIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MUC4O|coRjJ{MkGwPFc4RC:jPh?=
L591 MlvIRZBweHSxc3nzJGF{e2G7 MoHJOUDPxE1? NX3CVpNHOjRiaB?= NVnmVZU3UW6mdXP0bY9vKG:oIHHwc5B1d3Orcx?= M{LKVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkGwPFc4Lz5{MkKxNFg4PzxxYU6=
U-87MG MmW2SpVv[3Srb36gRZN{[Xl? MkLnNVAxKG6P M1LMO|I1KGh? NY\ycIVCTE2VTx?= MV7Jcohq[mm2aX;uJI9nKCClZXzsJI1q\3KjdHnvci=> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
SW1783 MoG3SpVv[3Srb36gRZN{[Xl? MVyxNFAhdk1? M1n6elI1KGh? M3rqfmROW09? Mn\VTY5pcWKrdHnvckBw\iBiY3XscEBucWe{YYTpc44> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
U-87MG M4S0eWZ2dmO2aX;uJGF{e2G7 M1v4c|Uh|ryP NGToT4gzPCCq NGXkdJFFVVOR M13FT2lvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDzeYJ{fGGwdHnhcIx6 MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjB5OU[wPUc,OjJyN{m2NFk9N2F-
SW1783 Mmf6SpVv[3Srb36gRZN{[Xl? NUGwPHJ7PSEQvF2= MUiyOEBp MXvEUXNQ NGfrd4VKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gd5Vje3SjboTpZYxtgQ>? M{DW[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEe5OlA6Lz5{MkC3PVYxQTxxYU6=
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LAN-5 NGrCNXlyUFSVIHHzd4F6 Mn3ydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| NIPWd5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SUDHL6 MnKxRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NF3Me444OiCqcoO= MoPpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVVVTIUFYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPDT|gh[XO|YYmsJGlEPTBiPTCwMlY2KM7:TT6= NG\5do49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWzOFk{Pid-Mkm1N|Q6OzZ:L3G+
RPMI8226 NYfmTmpPSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M4fZPVczKGi{cx?= MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKSTVm4NlI3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTC1MlQ6KM7:TT6= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV|NEmzOkc,Ojl3M{S5N|Y9N2F-
Raji MmnzRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MXu3NkBpenN? M2q4SmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUnHqbUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iOT65OUDPxE1w NEnhbXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWzOFk{Pid-Mkm1N|Q6OzZ:L3G+
SU-DHL6 M13zO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVnHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDTWU1FUEx4IHPlcIx{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGdKPTBiPTCwMlA1OiEQvF2u M{XxfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NkCxPVkyLz5{OU[wNVk6OTxxYU6=
MOLM13 MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4nyV|czKGi{cx?= NVjJTGV7T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OTUGzJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGG|c3H5MEBIUTVyIE2gNU44KM7:TT6= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB3M{eyNUc,OzByNUO3NlE9N2F-
MOLM14 NEL2c|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHPPdo44OiCqcoO= MkXYS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUW9NVTF2IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JIF{e2G7LDDHTVUxKD1iNj60JO69VS5? MlnMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByNUO3NlEoRjNyMEWzO|IyRC:jPh?=
MOLM14 MVTBcpRqfHWvb4KgZZN{[Xl? MlP4NVAxKG2pL3vn M2T2VVE1KGSjeYO= MUnBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVQh[2WubIOgfIVvd2e{YX\0[YQhcW5iboWvcpUhdW:3c3WgZZN{\XO|ZXSgZZMhfHWvb4Kg[5Jwf3SqIHnubIljcXSrb36gZZQhOTByIH3nM4toNCCybzDh[I1qdmm|dHXy[YQh\GGrbImgeoliKGejdnHn[UBld3OnZDDmc5IhOTRiZHH5d{BidmRibXXhd5Vz\WRiZHHpcJkh\HW{aX7nJINwdXCxdX7kJIRwe2mwZzDy[YxifGm4ZTD0c{Bkd262cn;s MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB3M{eyNUc,OzByNUO3NlE9N2F-
MOLM14 MWTBcpRqfHWvb4KgZZN{[Xl? Mnn6NVAxKG2pL3vn MXyxOEBl[Xm| MVHBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVQh[2WubIOgfIVvd2e{YX\0[YQhcW5iboWvcpUhdW:3c3WgZZN{\XO|ZXSgZZMhcW6mdXP0bY9vKG:oIHHwc5B1d3OrczDheEAyODBibXevb4ctKHCxIHHkcYlvcXO2ZYLl[EBl[WmueTD2bYEh\2G4YXflJIRwe2WmIH\vdkAyPCCmYYnzJIFv\CCvZXHzeZJm\CCmYXnsfUBlfXKrbnegZ49ueG:3bnSg[I9{cW6pIHL5JHRWVkWOIHLhd4VlKGG|c3H5 M3LXU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEWzO|IyLz5|MEC1N|czOTxxYU6=
MOLM14 M1;HVGFvfGm2dX3vdkBie3OjeR?= MV:xNFAhdWdxa3e= MW[xOEBl[Xm| MULBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVQh[2WubIOgfIVvd2e{YX\0[YQhcW5iboWvcpUhdW:3c3WgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD0eY1weiCycn;sbYZmemG2aX;uJFExOCCvZz;r[{wheG9iYXTtbY5qe3SncnXkJIRicWy7II\pZUBo[X[jZ3Wg[I9{\WRiZn;yJFE1KGSjeYOgZY5lKG2nYYP1doVlKGSjaXz5JIR2emmwZzDjc41xd3WwZDDkc5NqdmdiYomgT4kuPjdibHHi[YxtcW6pIHLhd4VlKGmvbYXuc4g> NGfTeIQ9[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

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 2022-08-01)

技术支持

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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

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