Ribociclib (LEE011)

For research use only. Not for use in humans.

目录号：S7440 中文名称：瑞博西利，瑞博西林

Ribociclib (LEE011) Chemical Structure

CAS No. 1211441-98-3

Ribociclib (LEE011) 是一种具有口服活性的、高度特异性的CDK4和CDK6抑制剂，对应的IC50值分别为10 nM和39 nM。Phase 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
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客户使用Selleck生产的Ribociclib (LEE011)发表文献54篇：

产品安全说明书

CDK抑制剂选择性比较

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CDK4和CDK6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 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\tXVI1KGh? NWP0U3BoT0l3ME2yO|Yhdk1? NGT0V4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi1NlA2QCd-MkW4OVIxPTh:L3G+
Myoblast NGLxT3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2CySVczKGh? MojHTWM2OD1zMEO1JI5O MmfLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MUCzO|UoRjJ3OEGwN|c2RC:jPh?=
IMRS NVTKV5RKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWG0WG9bPzJiaB?= MmLsTWM2OD16N{Ogcm0> NU[zU2NwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
SKNAS MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVewN2ZIPzJiaB?= NV7YUIU4UUN3MP-8olExODByIH7N NV\hN5JORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
Rh28 NHLqc4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHVO|IhcA>? MlrYTWM2OD16NEWgcm0> M1fqdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEGwN|c2Lz5{NUixNFM4PTxxYU6=
Rh41 NXHUWIhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYO3NkBp MkXNTWM2OD15MUi3JI5O NEjETFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
CW9019 M1[wN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\ZWVczKGh? MXTJR|UxRTl7MUKgcm0> Mmj4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MUCzO|UoRjJ3OEGwN|c2RC:jPh?=
Rh5 NUTyVFVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NID0cGQ4OiCq Mk\2TWM2OO,:nkGwNFAxKG6P Mo\qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MUCzO|UoRjJ3OEGwN|c2RC:jPh?=
Rh30 NFW0RmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPTeVlCPzJiaB?= MkDuTWM2OO,:nkGwNFAxKG6P M4DrVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEGwN|c2Lz5{NUixNFM4PTxxYU6=
778 Mo\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVy3NkBp NFv0NGNqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NYLqXm9KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
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LP3 NH3tT|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFH6SJI4OiCq MVzpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NXS5NJNRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
LP6 NF\PV5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\3eo44OiCq MYXpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NIrHT3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyPFQ3QSd-MkWwNlg1Pjl:L3G+
LP8 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUK3NkBp M1PHRolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NWjqOmlERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
LPS141 NWP1RmE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXWVXc4OiCq NYLu[|B[cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? Mn\6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMki0OlkoRjJ3MEK4OFY6RC:jPh?=
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449 MnLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX:zMlM{KM7:TR?= M17v[|I1KGh? MYnk[YNz\WG|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG|ZR?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB{OES2PUc,OjVyMki0Olk9N2F-
LP3 M1O0eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fyUVMvOzNizszN M4rOfVI1KGh? Morv[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= MnnDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMki0OlkoRjJ3MEK4OFY6RC:jPh?=
LP6 MkXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3QcXY{NjN|IN88US=> NYDocYJFOjRiaB?= MkCy[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NYTzbnR1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
LP8 NXfOSWxvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPNd5YxOy5|MzFOwG0> MWSyOEBp MnjM[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy|IHnuJHMheGijc3W= NVS5WpY6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
LPS141 NUDNXWI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIi1eHc{NjN|IN88US=> MXqyOEBp NULRbmpY\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U> NUfJXGlRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
IMR5 NVLsVpc6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVn5OHluOjRiaB?= MXjEUXNQ MlfqTWM2OD1zMk[gcm0> Ml7IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNEWxO|koRjJ2MES1NVc6RC:jPh?=
BE2C NXTidXpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrYNlQhcA>? NELiOpFFVVOR M1\MNmlEPTB;MUO0JI5O M2DRdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
1643 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjlNlQhcA>? NEX0bVdFVVOR NVWyRnB2UUN3ME2xOFchdk1? M{W2TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
SKNSH MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoizNlQhcA>? MVrEUXNQ MnTwTWM2OD1zNEigcm0> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO|k9N2F-
SY5Y NUfWPWZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV2xXotMOjRiaB?= MV3EUXNQ MYPJR|UxRTF3NDDuUS=> NXLsUWJqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
NGP M33rSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUCyOEBp M1PoeGROW09? NH3nW4FKSzVyPUG3OUBvVQ>? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO|k9N2F-
KELLY M3rmZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPxNlQhcA>? NHTEO3FFVVOR M4PzdmlEPTB;MkKwJI5O MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO|k9N2F-
CHP134 MorxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzVPGlNOjRiaB?= MkfmSG1UVw>? MofNTWM2OD1{N{Ogcm0> M{\3R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
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H1299 NGTvR5pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF3ycXg4OiCqcoO= NFf5WIlIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJOTJ7OTDj[YxteyCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBES0t6IHHzd4F6NCCLQ{WwJF0hPy54M{eg{txONg>? NVn3eGxxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2OVE6PzlpPkK4OlUyQTd7PD;hQi=>
KOPN8 NFL0O4ZCeG:ydH;zbZMh[XO|YYm= NXvaTYtZOC53IIXN NHm1b2g{KGi{cx?= NFPLV5RKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFvPVG45KGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBkdGWjdnXkJHBCWlBibHX2[Ywh[XRiMD61JJVOKGGodHXyJFMhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NVTHWYJ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzVpPkK5OFA4QTd3PD;hQi=>
KOPN8 MlnrRZBweHSxc3nzJIF{e2G7 NXTsfYtZOC53IIXN Ml;5NlQhcHK| NVjnZmVlUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDLU3BPQCClZXzsd{Bie3Onc4Pl[EBieyC3cILl[5Vt[XSrb36gc4Yh[2ynYY\l[EBRSVKSIHzleoVtKGG2IECuOUB2VSCycnWteJJm[XSnZDD3bZRpKE6DQzDmc5IhOSCqcjDhcoQhdWWjc4Xy[YQh[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? Ml7YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2MEe5O|UoRjJ7NEC3PVc2RC:jPh?=
Hep3B NWeyNmZrS2WubDDjfYNt\SCjc4PhfS=> M3fkU|I1KGi{cx?= MkjLR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gTIVxO0JiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdyL1exJJBp[XOnIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oKGKjc3XkJIZtd3diY4n0c41mfHK7 NVjzR4lQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
HepG2 NFXQfHhE\WyuIHP5Z4xmKGG|c3H5 NF;STWQzPCCqcoO= M1ywSGNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG|c3Xzd4VlKGG|IHHjZ5VufWyjdHnvckBifCCJMD;HNUBxcGG|ZTDh[pRmeiB{NDDodpMh[nlicILvdIllcXWvIHnv[Ill\SC|dHHpcolv\yCkYYPl[EBndG:5IHP5eI9u\XS{eR?= MmG1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N|EzRC:jPh?=
A549 NWjP[WVzS2WubDDjfYNt\SCjc4PhfS=> MX6yOEBpenN? Mkf1R4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzBxR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcoch[mG|ZXSg[oxwfyCleYTvcYV1enl? M4LVVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N|EzLz5{OUWxPFMyOjxxYU6=
NCI-H460 NGTyS49E\WyuIHP5Z4xmKGG|c3H5 NXrhWFNxOjRiaILz MY\D[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDOR2kuUDR4MDDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{CvS|EheGijc3WgZYZ1\XJiMkSgbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdiYnHz[YQh\myxdzDjfZRwdWW2com= MmPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N|EzRC:jPh?=
T47D NWDOPJU4S2WubDDjfYNt\SCjc4PhfS=> NW\yTYdmOjRiaILz NULyNJl6S2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hXDR5RDDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{CvS|EheGijc3WgZYZ1\XJiMkSgbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdiYnHz[YQh\myxdzDjfZRwdWW2com= M{jnWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N|EzLz5{OUWxPFMyOjxxYU6=
MDA-MB-231 MUPD[YxtKGO7Y3zlJIF{e2G7 MofuNlQhcHK| NYmwXm1SS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzBxR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcoch[mG|ZXSg[oxwfyCleYTvcYV1enl? Mn\6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N|EzRC:jPh?=
Fluc-labeled 4T1 NV\Ee4FiSW62aYT1cY9zKGG|c3H5 NF;S[HMyOzBibXevb4c> M{e1[VE5KGSjeYO= NGn5e4FCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBud3W|ZTDGcJVkNWyjYnXs[YQhPFRzIHPlcIx{KGmvcHzhcpRm\CCrbjDCZYxjN2NibX;1d4Uh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJJR2dW:{IIflbYdpfCCjdDCxN|AhdWdxa3esJIlxKGGmbXnubZN1\XKnZDDkZYltgSCob4KgNVgh\GG7czDt[YF{fXKnZDDh[pRmeiB6IITvJFI2KGSjeYO= M33LdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N|EzLz5{OUWxPFMyOjxxYU6=
T47D NUm3bmlDS2WubDDjfYNt\SCjc4PhfS=> MWeyOEBpenN? NUjHVVFMUW6mdXP0bY9vKG:oIHPlcIwh[3mlbHWgZZJz\XO2IHnuJIh2dWGwIGS0O2Qh[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iR{CvS|EheGijc3WgZYNkfW23bHH0bY9vKGmwY4XiZZRm\CCob4KgNlQhcHK|IHL5JIZtd3diY4n0c41mfHK7 NXr0OpdORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2OVE6PzlpPkK4OlUyQTd7PD;hQi=>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP; 

PubMed: 29789630     


Effect of ribociclib on pRB and G1 cell cycle regulating protein expressions in C666-1 and HK1 cells. Cells were treated with ribociclib in 2 concentrations, one of them near their corresponding IC50, for 24 and 48 hours. Phosphorylation of Rb in all cell䲧疝Ỵ疞㧀疜膉痘 瘿뾠ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ⟸෕䐺痖暼瘿⟸෕ᾰƌ ⟸෕Ð㺣痖⟸෕€𢡄⟼෕€䀷痗⟼෕౴⟼෕

29789630
Growth inhibition assay
Cell viability ; 

PubMed: 26390342     


Effects of palbociclib and ribociclib on viability of H157, H2170, H520 and H596 cells after 72 hours of drug treatment and IC50 values for inhibition of 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]
- 合并
  • 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。


    (Only for Reference)
动物实验：

[1]
- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 7 mg/mL (16.1 mM)
Water Insoluble
Ethanol Insoluble

* 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 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 只
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
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) March 2021 --
NCT04315233 Recruiting Drug: Ribociclib|Drug: Belinostat Metastatic Breast Cancer|Recurrent Ovarian Carcinoma University of Utah|Novartis|Acrotech Biopharma October 29 2020 Phase 1
NCT03834740 Recruiting Drug: Ribociclib|Drug: Everolimus Glioblastoma Multiforme|Glioma of Brain St. Joseph''s Hospital and Medical Center Phoenix|Ivy Brain Tumor Center|Barrow Neurological Institute December 21 2018 Early Phase 1
NCT03701334 Active not recruiting Drug: Ribociclib|Other: Endocrine Therapy Early Breast Cancer Novartis Pharmaceuticals|Translational Research in Oncology|Novartis December 7 2018 Phase 3
NCT03613220 Completed Drug: ribociclib|Drug: letrozole HR+ HER2 Breast Cancer Novartis Pharmaceuticals|Novartis December 28 2018 Phase 2

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
Selleck产品目录册

CDK Signaling Pathway Map

相关CDK产品

  • SU9516 New

    SU9516是一种3位取代的吲哚酮类CDK抑制剂，对CDK2，CDK1，和CDK4的IC50分别为22 nM，40 nM，和200 nM。

  • Ro-3306 New

    RO-3306是一种ATP竞争性的选择性 CDK1 抑制剂，Ki 为20 nM，选择性是其他各种人类激酶的15倍多。RO-3306可增强p53介导的 Bax 激活和线粒体的凋亡。

  • Purvalanol A New

    Purvalanol A 是一种有效的，细胞渗透性 CDK 抑制剂，对cdc2-cyclin B，cdk2-cyclin A，cdk2-cyclin E，和 cdk4-cyclin D1的 IC50 分别为 4 nM，70 nM，35 nM，和 850 nM。Purvalanol A 可诱导内质网应激介导的凋亡与自噬。

  • Palbociclib (PD-0332991) HCl

    Palbociclib (PD-0332991) HCl是一种高度选择性的CDK4/6抑制剂，无细胞试验中IC50分别为11 nM/16 nM。它对CDK1/2/5，EGFR，FGFR，PDGFR，InsR等没有抑制活性。Phase 3。

    Features:PD-0332991作为有应用前景的工具测定CDK激酶是否具有明显的治疗价值。

  • Palbociclib (PD0332991) Isethionate

    Palbociclib (PD0332991) Isethionate是一种高度选择性的CDK4/6抑制剂，无细胞试验中IC50为11 nM/16 nM，对CDK1/2/5，EGFR，FGFR，PDGFR， InsR等没有抑制活性。Phase 3。

    Features:PD 0332991治疗多种癌症，特异性抑制CDK4/6，是第一种有前途的抑制剂。

  • Dinaciclib (SCH727965)

    Dinaciclib (SCH727965, PS-095760) 是一种新型有效的CDK抑制剂，作用于CDK2，CDK5，CDK1和CDK9，无细胞试验中IC50分别为1 nM，1 nM，3 nM和4 nM。它也会阻断胸甘(dThd) DNA整合。Dinaciclib 可通过激活caspases 8和caspases 9来诱导细胞凋亡。Phase 3。

    Features:[1]

  • Flavopiridol (L86-8275) HCl

    Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033)与ATP竞争性抑制CDKs，作用于CDK1，CDK2，CDK4和CDK6，无细胞试验中IC50为~40 nM。作用于CDK1/2/4/6比作用于CDK7选择性高7.5倍。Flavopiridol最初被发现可抑制EGFR和PKA。Flavopiridol HCl 可诱导自噬和内质网应激反应。Flavopiridol HCl 可阻止HIV-1的复制。Phase 1/2。

  • Roscovitine (CYC202)

    Roscovitine (CYC202, Seliciclib, R-roscovitine)是一种有效的，选择性CDK抑制剂，作用于Cdc2，CDK2和CDK5时，无细胞试验中IC50分别为0.65 μM，0.7 μM和0.16 μM，对CDK4/6几乎没有作用。Phase 2。

  • Abemaciclib mesylate (LY2835219)

    Abemaciclib (LY2835219)是一种有效的，选择性CDK4和CDK6抑制剂，无细胞试验中IC50分别为2 nM和10 nM。Phase 3。

  • SNS-032 (BMS-387032)

    SNS-032 (BMS-387032)最初被描述为选择性CDK2抑制剂，无细胞试验中IC50为48 nM，比作用于CDK1/CDK4选择性高10和20倍。它也对CDK7/9敏感，IC50为62 nM/4 nM，对CDK6几乎没有抑制效果。SNS-032 (BMS-387032)可诱导凋亡。Phase 1。

    Features:SNS-032是新一代CDK抑制剂,具有更高的选择性和更弱的毒性。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID