Ribociclib (LEE011)

目录号:S7440 中文名称:瑞博西利,瑞博西林

仅限科研使用

Ribociclib (LEE011) 是一种具有口服活性的、高度特异性的CDK4CDK6抑制剂,对应的IC50值分别为10 nM和39 nM。Phase 3。

Ribociclib (LEE011) Chemical Structure

CAS: 1211441-98-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2432.43 现货
RMB 1614.88 现货
RMB 4832.1 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Ribociclib (LEE011)发表文献64篇:

产品安全说明书

CDK抑制剂选择性比较

相关CDK产品

生物活性

产品描述 Ribociclib (LEE011) 是一种具有口服活性的、高度特异性的CDK4CDK6抑制剂,对应的IC50值分别为10 nM和39 nM。Phase 3。
特性 口服生物有效的CDK4/6选择性抑制剂,处于Ⅲ期临床测试,用于晚期乳腺癌的治疗。
靶点
CDK4 [2]
(Cell-free assay)
CDK6 [2]
(Cell-free assay)
10 nM 39 nM
体外研究

LEE011是一种CDK4/CDK6的双重抑制剂,能够显著抑制17种神经细胞瘤中的12种的生长,平均IC50值是307 nM。对神经细胞瘤的抑制主要是抑制细胞的生长,受到G1细胞周期阻滞和细胞衰老的调控。

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DFSP105 NWXvcYp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnNPW82OjRiaB?= M1jJbWdKPTB;Mke2JI5O MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh3MkC1PEc,OjV6NUKwOVg9N2F-
Myoblast M17wW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\SS|czKGh? NFfNb|lKSzVyPUGwN|Uhdk1? NWjISXRLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
IMRS MnzWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TqXFczKGh? MXvJR|UxRTh5MzDuUS=> NGrxc4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
SKNAS Mn\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jtXVczKGh? NF7m[WhKSzVy78{eNVAxODBibl2= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMEO3OUc,OjV6MUCzO|U9N2F-
Rh28 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXrRog4OiCq Mn:3TWM2OD16NEWgcm0> NF:2bJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
Rh41 M3f0fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPOO|IhcA>? NIHMUFFKSzVyPUexPFchdk1? M1uxSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEGwN|c2Lz5{NUixNFM4PTxxYU6=
CW9019 NImxV2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\HO|IhcA>? NWPQcnNmUUN3ME25PVEzKG6P NVfm[2o{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
Rh5 MnXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHvO|IhcA>? NHLZN4dKSzVy78{eNVAxODBibl2= MknjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MUCzO|UoRjJ3OEGwN|c2RC:jPh?=
Rh30 M1\3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYK3NkBp NIXQenlKSzVy78{eNVAxODBibl2= M1zS[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEGwN|c2Lz5{NUixNFM4PTxxYU6=
778 NG\MVpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlX1O|IhcA>? Mnm3bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MnzqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMki0OlkoRjJ3MEK4OFY6RC:jPh?=
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LP6 NHy4TYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDNO|IhcA>? NXzzfohVcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M{LlOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
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LPS141 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVy3NkBp NYXveHFDcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NYHRPGZSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
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449 NFLadmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3L3NlMvOzNizszN NVKxPXlUOjRiaB?= MXHk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= NXHPSFRKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
LP3 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjpPGRTOy5|MzFOwG0> NXLPc4M3OjRiaB?= Mm\Z[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB{OES2PUc,OjVyMki0Olk9N2F-
LP6 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4raNlMvOzNizszN Ml7SNlQhcA>? NHLTOVFl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> M{j6RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
LP8 M3zpRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrtV|RPOy5|MzFOwG0> Mn3ENlQhcA>? NIizRXNl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=> NH;jd|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyPFQ3QSd-MkWwNlg1Pjl:L3G+
LPS141 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoKzN{4{OyEQvF2= MU[yOEBp MmL5[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= M{X6T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
IMR5 MoLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWSyOEBp NV;YXGRyTE2VTx?= NX\KfYlVUUN3ME2xNlYhdk1? NGO2TFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
BE2C M4HGRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULLO452OjRiaB?= NXvnVnJKTE2VTx?= MXrJR|UxRTF|NDDuUS=> M2TFXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
1643 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWSyOEBp M2TrUmROW09? MoCzTWM2OD1zNEegcm0> NWTRbm9HRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
SKNSH NVvTV5RtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\6OVI1KGh? NInPWpJFVVOR NIrWfppKSzVyPUG0PEBvVQ>? M1faUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
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NGP MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHpSJRlOjRiaB?= M{K4[WROW09? MXHJR|UxRTF5NTDuUS=> Mn\xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNEWxO|koRjJ2MES1NVc6RC:jPh?=
KELLY NX\6RZJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jv[FI1KGh? Mmr0SG1UVw>? M3e2WWlEPTB;MkKwJI5O M2r3d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
CHP134 M2LJbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;oZZEzPCCq MkX0SG1UVw>? MoXjTWM2OD1{N{Ogcm0> NInZRXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
NLF NV3JfFJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXqV2QzPCCq NUH3VnI3TE2VTx?= NH36Z5dKSzVyPUOyPEBvVQ>? NELz[lA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
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NB69 NVqwUXpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVGyOEBp NHzu[FBFVVOR MVzJR|UxRTd|ODDuUS=> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO|k9N2F-
SKNDZ M1fUZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWmyOEBp NH;Ib2ZFVVOR M2L3V2lEPTB;OECxJI5O MlfVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNEWxO|koRjJ2MES1NVc6RC:jPh?=
NBSD MoC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[yOEBp NUDvfHE3TE2VTx?= M2O1bGlEPTB;MUmwNEBvVQ>? NEn1T|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
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HepG2 M3TpPGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mnj0O|IhcHK| MkDyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XsWIl1\XJvR3zvJIF{e2G7LDDFR|UxKD1iMD6yPFYzKM7:TT6= NFnaWlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSwO|k4PSd-Mkm0NFc6PzV:L3G+
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KOPN8 MU\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NXPUTGVGPzJiaILz MnnlRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNT2DOPEBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XsWIl1\XJvR3zvJIF{e2G7LDDFR|UxKD1iMD61NFA5KM7:TT6= M1SyVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEC3PVc2Lz5{OUSwO|k4PTxxYU6=
NCI-H1299 MoP0R5l1d3SxeHnjbZR6KGG|c3H5 MojkO|IhcHK| NYjCSlZVS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLVixNlk6KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhS0ONODDhd5NigSxiSVO1NEA:KDVwNE[g{txONg>? M3rYPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N|EzLz5{OUWxPFMyOjxxYU6=
T47D MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkjpO|IhcHK| M1\HPWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJHQ1P0RiY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgR2NMQCCjc4PhfUwhUUN3MDC9JFYvOjJ5IN88UU4> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ3MUm3PUc,Ojh4NUG5O|k9N2F-
T47D NHS5RmZEgXSxdH;4bYNqfHliYYPzZZk> NVLCfoJzPzJiaILz MlTwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWFQ4TCClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KEOFS{igZZN{[XluIFnDOVAhRSB4LkKzJO69VS5? M1vLOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N|EzLz5{OUWxPFMyOjxxYU6=
H1299 NUi5dZJXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{[0NlczKGi{cx?= NXeyfpl5T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUDF{OUmgZ4VtdHNiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhS0ONODDhd5NigSxiSVO1NEA:KDdwNkO3JO69VS5? Mn65QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4NUG5O|koRjJ6NkWxPVc6RC:jPh?=
KOPN8 M4K4dWFxd3C2b4Ppd{Bie3OjeR?= Ml\QNE42KHWP NVfv[o5ROyCqcoO= MlK0TY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCNT2DOPEBk\WyuczDhd5Nme3OnZDDhd{B2eHKnZ4XsZZRqd25ib3[gZ4xm[X[nZDDQRXJRKGyndnXsJIF1KDBwNTD1UUBi\nSncjCzJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O|U9N2F-
KOPN8 NGHEemJCeG:ydH;zbZMh[XO|YYm= M{LlVlAvPSC3TR?= NFftU2QzPCCqcoO= NV\Td245UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDLU3BPQCClZXzsd{Bie3Onc4Pl[EBieyC3cILl[5Vt[XSrb36gc4Yh[2ynYY\l[EBRSVKSIHzleoVtKGG2IECuOUB2VSCycnWteJJm[XSnZDD3bZRpKE6DQzDmc5IhOSCqcjDhcoQhdWWjc4Xy[YQh[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O|U9N2F-
Hep3B MkfhR4VtdCCleXPs[UBie3OjeR?= MkDuNlQhcHK| MkDmR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gTIVxO0JiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdyL1exJJBp[XOnIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oKGKjc3XkJIZtd3diY4n0c41mfHK7 NXPLdmdvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
HepG2 M4rtS2NmdGxiY4njcIUh[XO|YYm= NV7WTWFzOjRiaILz M4DB[GNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG|c3Xzd4VlKGG|IHHjZ5VufWyjdHnvckBifCCJMD;HNUBxcGG|ZTDh[pRmeiB{NDDodpMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\yCkYYPl[EBndG:5IHP5eI9u\XS{eR?= NIPlV3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
A549 MoTBR4VtdCCleXPs[UBie3OjeR?= NFLyNHIzPCCqcoO= M2e1UWNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdyL1exJJBp[XOnIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oKGKjc3XkJIZtd3diY4n0c41mfHK7 MmW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N|EzRC:jPh?=
NCI-H460 MVfD[YxtKGO7Y3zlJIF{e2G7 M3vnNFI1KGi{cx?= M13D[WNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJG5EUS2KNE[wJINmdGy|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCjdDDHNE9IOSCyaHHz[UBi\nSncjCyOEBpenNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZzDiZZNm\CCobH;3JIN6fG:vZYTyfS=> NVn5XFE3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
T47D MXPD[YxtKGO7Y3zlJIF{e2G7 M{PXW|I1KGi{cx?= NVTqe2M2S2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hXDR5RDDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{CvS|EheGijc3WgZYZ1\XJiMkSgbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdiYnHz[YQh\myxdzDjfZRwdWW2com= MkLrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N|EzRC:jPh?=
MDA-MB-231 MXfD[YxtKGO7Y3zlJIF{e2G7 M1GwfVI1KGi{cx?= NUniVHp1S2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzBxR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcoch[mG|ZXSg[oxwfyCleYTvcYV1enl? MnGzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N|EzRC:jPh?=
Fluc-labeled 4T1 NVrhVId6SW62aYT1cY9zKGG|c3H5 NU[xV5A3OTNyIH3nM4to NE\ydGoyQCCmYYnz MXTBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCIbIXjMYxi[mWuZXSgOHQyKGOnbHzzJIlueGyjboTl[EBqdiCEYXziM4MhdW:3c3WgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIIT1cY9zKHenaXfoeEBifCBzM{CgcYcwc2duIHnwJIFldWmwaYP0[ZJm\CCmYXnsfUBnd3JiMUig[IF6eyCvZXHzeZJm\CCjZoTldkA5KHSxIEK1JIRigXN? NELxcoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
T47D M3HrVmNmdGxiY4njcIUh[XO|YYm= NIDxdpozPCCqcoO= MnewTY5lfWO2aX;uJI9nKGOnbHygZ5lkdGViYYLy[ZN1KGmwIHj1cYFvKFR2N1SgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hTzBxR{GgdIhie2ViYXPjeY12dGG2aX;uJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IH\sc5ch[3m2b33leJJ6 Mn7pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4NUG5O|koRjJ6NkWxPVc6RC:jPh?=
Assay
Methods Test Index PMID
Western blot pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP 29789630
Growth inhibition assay Cell viability 26390342
体内研究

LEE011 (200 mg/kg 每日,口服)引起小鼠中的BE2C 或者 1643细胞显著的生长延迟,没有体重减轻或者其它的毒性症状。[1]

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)

细胞实验:

[1]

  • Cell lines: BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1细胞系。
  • Concentrations: 10 μM
  • Incubation Time: ~100小时
  • Method:

    将板中优先附着基底生长的神经母细胞瘤细胞系以一式三份种植于Xcelligence实时细胞电子传感系统,用4个剂量梯度的抑制剂和DMSO为对照处理细胞24小时。连续监测细胞约100个小时,IC50通过以下方法测得:通过绘制细胞指数为时间的函数产生生长曲线,以在治疗开始时细胞指数为1作为标准。从治疗开始到处理96小时后,生长曲线下的面积通过基线下面积为1(治疗开始时的细胞指数)进行计算。积分面积以DMSO处理的对照组作为背景。抑制剂比上对照组的值取非线性对数值来计算。所有的实验至少重复一次。

动物实验:

[1]

  • Animal Models: BE2C, NB-1643,或EBC1异种移植的小鼠。
  • Dosages: ~200毫克/千克 每天
  • Administration: 口服

溶解度(25°C)

体外

* 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 434.54
化学式

C23H30N8O

CAS号 1211441-98-3
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
NCT05429502 Not yet recruiting Drug: Topotecan|Drug: Temozolomide|Drug: Ribociclib Neuroblastoma Novartis Pharmaceuticals|Innovative Therapies For Children with Cancer Consortium|Novartis August 31 2022 Phase 1|Phase 2
NCT04657679 Recruiting Drug: Ribociclib Breast Cancer Georgetown University|Medstar Health Research Institute|Breast Cancer Research Foundation|Georgetown-Howard Universities Center for Clinical and Translational Science (GHUCCTS) May 20 2021 Phase 4
NCT04315233 Recruiting Drug: Ribociclib|Drug: Belinostat Metastatic Breast Cancer|Recurrent Ovarian Carcinoma University of Utah|Novartis|Acrotech Biopharma May 3 2021 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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