Ribociclib (LEE011)

For research use only. Not for use in humans.

製品コードS7440

CAS No. 1211441-98-3

Ribociclib (LEE011) is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.

サイズ

価格(税別)

5mg	JPY 34700
10mg	JPY 51300
25mg	JPY 86960

最寄りの販売代理店を探す

東京
北海道
東北
北関東
南関東
東海
北信越
近畿
中国
四国
九州

お探しのディーラーが見当たらない場合は直接こちらのメールアドレスまでお問い合わせください：[email protected]

バルク問合せ

代表番号: 03-5615-9297 | 電子メール：[email protected]

文献中Selleckの製品使用例(49)

製品安全説明書

CDK阻害剤の選択性比較

生物活性

製品説明

Ribociclib (LEE011) is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3.

特性

Orally bioavailable CDK4/6-selective inhibitor that has been tested in Phase III clinical trials for treatment of advanced breast cancer.

ターゲット

CDK4 ^[2] (Cell-free assay)	CDK6 ^[2] (Cell-free assay)
10 nM	39 nM

体外試験

LEE011, as dual CDK4/CDK6 inhibitor, significantly inhibits the growth of 12 of 17 neuroblastoma cell lines with mean IC50 of 307 nM. The growth inhibition of neuroblastoma cell lines is primarily cytostatic and is mediated by a G1 cell-cycle arrest and cellular senescence. ^[1]

細胞データ

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
DFSP105	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NYTTdXlROjRiaB?=		MWXHTVUxRTJ5NjDuUS=>	NYLyUo9LRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4OVIxPThpPkK1PFUzODV6PD;hQi=>
Myoblast	MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NEjofVQ4OiCq		MWfJR\|UxRTFyM{Wgcm0>	NFjL[Y89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
IMRS	M1zUPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NIC5cmo4OiCq		NUXxW4JiUUN3ME24O\|Mhdk1?	NVjac5F5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
SKNAS	MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NF3TXZY4OiCq		MmfETWM2OO,:nkGwNFAxKG6P	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMEO3OUc,OjV6MUCzO\|U9N2F-
Rh28	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MkPUO\|IhcA>?		MlfGTWM2OD16NEWgcm0>	NVHUfIdTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
Rh41	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NFTO[Xo4OiCq		MWTJR\|UxRTdzOEegcm0>	NHrCXmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
CW9019	NWnYOpZCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MoK3O\|IhcA>?		M3;4d2lEPTB;OUmxNkBvVQ>?	MkDDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MUCzO\|UoRjJ3OEGwN\|c2RC:jPh?=
Rh5	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MlKyO\|IhcA>?		M2rNcWlEPTExvK6xNFAxOCCwTR?=	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMEO3OUc,OjV6MUCzO\|U9N2F-
Rh30	MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MonrO\|IhcA>?		Mn7nTWM2OO,:nkGwNFAxKG6P	Moe3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MUCzO\|UoRjJ3OEGwN\|c2RC:jPh?=
778	Ml\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M{XMNFczKGh?		NYXFVZVqcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>?	M3PpS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
449	M4np[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NF7zeoc4OiCq		NVGxNIJscW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>?	NED0eoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyPFQ3QSd-MkWwNlg1Pjl:L3G+
LP3	M{\XSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		Ml\iO\|IhcA>?		MnX1bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:\|ZTDk[ZBmdmSnboTsfS=>	NVu2V5RHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
LP6	NGTXVmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NIP4UVk4OiCq		MWfpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5	NFzteY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyPFQ3QSd-MkWwNlg1Pjl:L3G+
LP8	M3O5[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NWXIb4FOPzJiaB?=		M1W3T4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk>	M4nldlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
LPS141	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NIDTRng4OiCq		MlnUbY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:\|ZTDk[ZBmdmSnboTsfS=>	NFfhcHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyPFQ3QSd-MkWwNlg1Pjl:L3G+
778	Mm\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4DXe\|MvOzNizszN	MUKyOEBp		NHXDOVNl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=>	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB{OES2PUc,OjVyMki0Olk9N2F-
449	Ml3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGTm[\|c{NjN\|IN88US=>	M4G0TVI1KGh?		NHHwbXFl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=>	MkDLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMki0OlkoRjJ3MEK4OFY6RC:jPh?=
LP3	MnfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFT1e2M{NjN\|IN88US=>	MkXONlQhcA>?		M4DQOYRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl	M2nXVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
LP6	NUi4So1QT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHrpUoo{NjN\|IN88US=>	M1LWclI1KGh?		NEXMZ45l\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=>	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB{OES2PUc,OjVyMki0Olk9N2F-
LP8	NIrhWW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M2CzdFMvOzNizszN	MXSyOEBp		M1r0XYRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl	MnziQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMki0OlkoRjJ3MEK4OFY6RC:jPh?=
LPS141	M1nPO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkHSN{4{OyEQvF2=	MXOyOEBp		NXXTTIlJ\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U>	MlmzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMki0OlkoRjJ3MEK4OFY6RC:jPh?=
IMR5	M2O0Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M3LG[FI1KGh?	NXG0e4ZDTE2VTx?=	NFK0[GxKSzVyPUGyOkBvVQ>?	M4rzZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
BE2C	NGfpdJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MkT0NlQhcA>?	NFTxO3pFVVOR	NGTaV3RKSzVyPUGzOEBvVQ>?	NGT2NpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
1643	NHzKdGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MmnMNlQhcA>?	MUTEUXNQ	M2\tZmlEPTB;MUS3JI5O	NEfNTmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
SKNSH	MlT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NWP1NpA3OjRiaB?=	M37weWROW09?	M4XaemlEPTB;MUS4JI5O	M4W4U\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
SY5Y	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NFm3dVUzPCCq	NIm2Z5FFVVOR	NF;6emRKSzVyPUG1OEBvVQ>?	M3T2bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
NGP	MojoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NF7ldY8zPCCq	M4LYPWROW09?	MUTJR\|UxRTF5NTDuUS=>	M3PJ[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
KELLY	NWnWT49nT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MWeyOEBp	NXfwZWdqTE2VTx?=	NHKwfpFKSzVyPUKyNEBvVQ>?	NVTW[HB6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
CHP134	NGDkUFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MnTLNlQhcA>?	NHPDTWpFVVOR	M1jBcmlEPTB;MkezJI5O	Mmq1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNEWxO\|koRjJ2MES1NVc6RC:jPh?=
NLF	NFu5RXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MoXhNlQhcA>?	MYTEUXNQ	M2fnUGlEPTB;M{K4JI5O	NH;ONVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
LAN5	M2O3RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MYiyOEBp	Mk[2SG1UVw>?	NVvNbHc4UUN3ME20Nlkhdk1?	NHnmRnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
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SKNDZ	NEfBV3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MX:yOEBp	NF\L[nNFVVOR	MnnLTWM2OD16MEGgcm0>	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO\|k9N2F-
NBSD	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NEfuOm4zPCCq	NYDZeFV2TE2VTx?=	NILMPJhKSzVyPUG5NFAhdk1?	MnP4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNEWxO\|koRjJ2MES1NVc6RC:jPh?=
SKNF1	M1vyb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MUKyOEBp	NYfHTmJ4TE2VTx?=	M2S5cmlEPTB;M{WwNEBvVQ>?	NVHONXQxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
EBC1	NVzHZW1FT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NGTFWpkzPCCq	NYr4NmE3TE2VTx?=	MXXJR\|UxRTZ2MECgcm0>	MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO\|k9N2F-
SKNAS	Mn7kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M2P4VFI1KGh?	MXnEUXNQ	NULufFFxUUN3MP-8olExODByIH7N	NWO1fpFxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
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Sf21	MoD5SpVv[3Srb36gZZN{[Xl?		NH;GZ3MyOCCvaX7z		NF3lVnJKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIH\1cIwhdGWwZ4ToJGMufGW{bXnuZYwhPkircz30ZYdo\WRiQ1TLPU9EgWOuaX6tWFEh[29vZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKHOoMkGgZ4VtdHNidYPpcochWESNdHnk[UB{fWK\|dILheIUhcW5icILld4Vv[2Vib3[gX4didW2jM{PQYWFVWCCjZoTldkAyOCCvaX7zJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnegcYV1cG:mLDDJR\|UxKD1iMD6xPVch\|ryPLh?=	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVzOEOxNkc,Ojl3MUizNVI9N2F-
HepG2	NV;PSVRTSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NYnKcFlSPzJiaILz		MYXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy\|IHHmeIVzKDd{IHjyd{BjgSCFZXzUbZRmei2JbH:gZZN{[XluIFXDOVAhRSByLkK4OlIh\|ryPLh?=	M3HFdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEC3PVc2Lz5{OUSwO\|k4PTxxYU6=
SEM	MUHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		M{ftWVczKGi{cx?=		NV6wOot7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSW0h[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcHRqfGW{LVfsc{Bie3OjeTygSWM2OCB;IECuOFYxPSEQvF2u	NGfvPIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSwO\|k4PSd-Mkm0NFc6PzV:L3G+
KOPN8	NYf4c5NLSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		Mn3mO\|IhcHK\|		MojURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCNT2DOPEBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XsWIl1\XJvR3zvJIF{e2G7LDDFR\|UxKD1iMD61NFA5KM7:TT6=	NUHzVHhtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzVpPkK5OFA4QTd3PD;hQi=>
NCI-H1299	M4nGdmN6fG:2b4jpZ4l1gSCjc4PhfS=>		NXnxPGZWPzJiaILz		NXTXdnR4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLVixNlk6KGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhS0ONODDhd5NigSxiSVO1NEA:KDVwNE[g{txONg>?	NVT2dVd3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
T47D	MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NE\wS4c4OiCqcoO=		NWXjT2czT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hXDR5RDDj[YxteyCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBES0t6IHHzd4F6NCCLQ{WwJF0hPi5{Mkeg{txONg>?	M3rGd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkWxPVc6Lz5{OE[1NVk4QTxxYU6=
T47D	M33BdWN6fG:2b4jpZ4l1gSCjc4PhfS=>		NF;mcms4OiCqcoO=		NEWxdWlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVPDeGIHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB5MjDodpMh[nliQ1PLPEBie3OjeTygTWM2OCB;IE[uNlMh\|ryPLh?=	NIK4d3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
H1299	M1y5cGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MlvkO\|IhcHK\|		NH;zTYxIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJOTJ7OTDj[YxteyCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBES0t6IHHzd4F6NCCLQ{WwJF0hPy54M{eg{txONg>?	MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ3MUm3PUc,Ojh4NUG5O\|k9N2F-
KOPN8	NVTSPWRjSXCxcITvd4l{KGG\|c3H5	NVjkWJRHOC53IIXN	MUKzJIhzew>?		NWLQNJRZUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDLU3BPQCClZXzsd{Bie3Onc4Pl[EBieyC3cILl[5Vt[XSrb36gc4Yh[2ynYY\l[EBRSVKSIHzleoVtKGG2IECuOUB2VSCjZoTldkA{KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O\|U9N2F-
KOPN8	MYXBdI9xfG:\|aYOgZZN{[Xl?	NYi0XHhVOC53IIXN	MWCyOEBpenN?		NETMfWVKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m\|IHnuJIh2dWGwIFvPVG45KGOnbHzzJIF{e2W\|c3XkJIF{KHWycnXneYxifGmxbjDv[kBkdGWjdnXkJHBCWlBibHX2[Ywh[XRiMD61JJVOKHC{ZT30doVifGWmIIfpeIghVkGFIH\vdkAyKGi{IHHu[EBu\WG\|dYLl[EBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{	NEPBNpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSwO\|k4PSd-Mkm0NFc6PzV:L3G+
Hep3B	Mmq0R4VtdCCleXPs[UBie3OjeR?=		NYnVVXlXOjRiaILz		MnvrR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gTIVxO0JiY3XscJMh[XO\|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdyL1exJJBp[XOnIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oKGKjc3XkJIZtd3diY4n0c41mfHK7	Ml\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N\|EzRC:jPh?=
HepG2	M{\pbmNmdGxiY4njcIUh[XO\|YYm=		NYnnXpZpOjRiaILz		M3nQVWNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG\|c3Xzd4VlKGG\|IHHjZ5VufWyjdHnvckBifCCJMD;HNUBxcGG\|ZTDh[pRmeiB{NDDodpMh[nlicILvdIllcXWvIHnv[Ill\SC\|dHHpcolv\yCkYYPl[EBndG:5IHP5eI9u\XS{eR?=	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVzOEOxNkc,Ojl3MUizNVI9N2F-
A549	MXnD[YxtKGO7Y3zlJIF{e2G7		MUOyOEBpenN?		NVrSWHFPS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{CvS\|EheGijc3WgZYZ1\XJiMkSgbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdiYnHz[YQh\myxdzDjfZRwdWW2com=	MoDSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N\|EzRC:jPh?=
NCI-H460	MoTNR4VtdCCleXPs[UBie3OjeR?=		MVOyOEBpenN?		NGXhU2FE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBPS0lvSES2NEBk\WyuczDhd5Nme3OnZDDhd{Bi[2O3bYXsZZRqd25iYYSgS\|AwTzFicHjhd4Uh[W[2ZYKgNlQhcHK\|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnegZoF{\WRiZnzve{BkgXSxbXX0dpk>	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVzOEOxNkc,Ojl3MUizNVI9N2F-
T47D	MWrD[YxtKGO7Y3zlJIF{e2G7		NEO0UoczPCCqcoO=		NV;DSIZsS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hXDR5RDDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{CvS\|EheGijc3WgZYZ1\XJiMkSgbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdiYnHz[YQh\myxdzDjfZRwdWW2com=	MnvWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N\|EzRC:jPh?=
MDA-MB-231	NXSyUmZES2WubDDjfYNt\SCjc4PhfS=>		MnrUNlQhcHK\|		M{D4cGNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJG1FSS2PQj2yN\|Eh[2WubIOgZZN{\XO\|ZXSgZZMh[WOldX31cIF1cW:wIHH0JGcxN0dzIIDoZZNmKGGodHXyJFI1KGi{czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nJIJie2WmIH\sc5ch[3m2b33leJJ6	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVzOEOxNkc,Ojl3MUizNVI9N2F-
Fluc-labeled 4T1	MWPBcpRqfHWvb4KgZZN{[Xl?	MoLXNVMxKG2pL3vn	NEnyRocyQCCmYYnz		Mn;CRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViRnz1Z{1t[WKnbHXkJFRVOSClZXzsd{BqdXCuYX70[YQhcW5iQnHsZk9kKG2xdYPlJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjD0eY1weiC5ZXnnbJQh[XRiMUOwJI1oN2upLDDpdEBi\G2rbnnzeIVz\WRiZHHpcJkh\m:{IEG4JIRigXNibXXhd5Vz\WRiYX\0[ZIhQCC2bzCyOUBl[Xm\|	MoDCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N\|EzRC:jPh?=
T47D	M2LlNWNmdGxiY4njcIUh[XO\|YYm=		NVHjXVBwOjRiaILz		MUXJcoR2[3Srb36gc4Yh[2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hXDR5RDDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG\|ZTDpckBIOC:JMTDwbIF{\SCjY3P1cZVt[XSrb36gbY5kfWKjdHXkJIZweiB{NDDodpMh[nliZnzve{BkgXSxbXX0dpk>	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ3MUm3PUc,Ojh4NUG5O\|k9N2F-

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ

Methods	Test Index	PMID
Western blot	pRb(S807) / Rb / p53 / Cyclin E / Cyclin D1 / CDK4 / CDK6 / p27 / p21 / PARP; PubMed: 29789630 Sci Rep 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 ACS Chem Biol 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

体内試験

LEE011 (200 mg/kg daily, p.o.) significantly causes tumor growth delay in mice harboring the BE2C or 1643 xenografts with no weight loss or other signs of toxicity. ^[1]

お薦めの試験操作（参考用のみ）

細胞試験： ^[1]	- 合併細胞株： BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1 cell lines. 濃度： 10 μM 反応時間： ~100 hours 実験の流れ： A panel of neuroblastoma cell lines, selected based upon prior demonstration of substrate adherent growth, is plated in triplicate on the Xcelligence Real-Time Cell Electronic Sensing system and treated 24 hours later with a four-log dose range of inhibitor or with a dimethyl sulfoxide (DMSO) control. Cell indexes are monitored continuously for ~100 hours, and IC50 values are determined as follows: growth curves are generated by plotting the cell index as a function of time and are normalized to the cell index at the time of treatment for a baseline cell index of 1. The area under the normalized growth curve from the time of treatment to 96 hours posttreatment is then calculated using a baseline area of 1 (the cell index at the time of treatment). Areas are normalized to the DMSO control, and the resulting data are analyzed using a nonlinear log inhibitor versus normalized response function. All experiments are repeated at least once. (参考用のみ)
動物試験： ^[1]	- 合併動物モデル： Mice bearing BE2C, NB-1643, or EBC1 xenografts. 投薬量： ~200 mg/kg daily 投与方法： p.o. (参考用のみ)

細胞試験：

^[1]

- 合併

細胞株： BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1 cell lines.
濃度： 10 μM
反応時間： ~100 hours
実験の流れ：
A panel of neuroblastoma cell lines, selected based upon prior demonstration of substrate adherent growth, is plated in triplicate on the Xcelligence Real-Time Cell Electronic Sensing system and treated 24 hours later with a four-log dose range of inhibitor or with a dimethyl sulfoxide (DMSO) control. Cell indexes are monitored continuously for ~100 hours, and IC50 values are determined as follows: growth curves are generated by plotting the cell index as a function of time and are normalized to the cell index at the time of treatment for a baseline cell index of 1. The area under the normalized growth curve from the time of treatment to 96 hours posttreatment is then calculated using a baseline area of 1 (the cell index at the time of treatment). Areas are normalized to the DMSO control, and the resulting data are analyzed using a nonlinear log inhibitor versus normalized response function. All experiments are repeated at least once.

(参考用のみ)

動物試験：

^[1]

- 合併

動物モデル： Mice bearing BE2C, NB-1643, or EBC1 xenografts.
投薬量： ~200 mg/kg daily
投与方法： p.o.
(参考用のみ)

参考

溶解度 (25°C)

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

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報 Ribociclib (LEE011) SDFをダウンロードする

分子量	434.54
化学式	C₂₃H₃₀N₈O
CAS No.	1211441-98-3
Storage	3 years-20°C powder 2 years-80°C in solvent
別名	N/A
Smiles	CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5

投与溶媒組成計算器(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量

mg/kg

動物平均体重

投与体積（動物毎）

動物数

匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO+ % + % Tween 80+ % ddH₂O

計算リセット

計算結果:

投与溶媒濃度： mg/ml；

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL，注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。）

投与溶媒調製方法：μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

質量

濃度

体積

分子量
=

×

×

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA（製品ページで利用可能な）。

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます：

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます：C1V1 = C2V2 ( 入力出力 )

C1

V1

C2

V2
×

=

×

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA（オンラインで利用できる）で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

連続希釈剤
初めの濃度：
稀釈倍数：

計算結果

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):

分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください：

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

臨床試験 (data from https://clinicaltrials.gov, updated on 2021-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04657679	Not yet 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)	December 2020	--
NCT04315233	Recruiting	Drug: Ribociclib\|Drug: Belinostat	Metastatic Breast Cancer\|Recurrent Ovarian Carcinoma	University of Utah\|Novartis\|Acrotech Biopharma	October 29 2020	Phase 1
NCT04417621	Recruiting	Drug: LXH254\|Drug: LTT462\|Drug: Trametinib\|Drug: Ribociclib	Melanoma	Novartis Pharmaceuticals\|Novartis	October 16 2020	Phase 2
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

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CDKシグナル伝達経路

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研究分野別

製品類型

Ribociclib (LEE011)

文献中Selleckの製品使用例(49)

製品安全説明書

CDK阻害剤の選択性比較

生物活性

お薦めの試験操作（参考用のみ）

参考

溶解度 (25°C)

化学情報 Ribociclib (LEE011) SDFをダウンロードする

投与溶媒組成計算器(クリア溶液)

便利ツール

モル濃度計算器

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

希釈計算器

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

連続希釈計算器方程式

連続希釈剤

計算結果

分子量计算器

総分子量：g/mol

モル濃度計算器

臨床試験 (data from https://clinicaltrials.gov, updated on 2021-01-06)

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CDKシグナル伝達経路

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