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Ribociclib (LEE011)

製品コード：S7440

For research use only.

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

CAS No. 1211441-98-3

サイズ	価格(税別)
10mM (1mL in DMSO)	JPY 44700
5mg	JPY 34700
10mg	JPY 51300
25mg	JPY 86960

代表番号: 03-5615-9297\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（64）

製品安全説明書

CDK阻害剤の選択性比較

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Palbociclib (PD0332991) Isethionate

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CDK Signaling Pathway Map

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	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M1LVV\|I1KGh?		MlLJS2k2OD1{N{[gcm0>	NHnUXZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUi1NlA2QCd-MkW4OVIxPTh:L3G+
Myoblast	M2\peGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NUHtRoQ2PzJiaB?=		Mo\JTWM2OD1zMEO1JI5O	NYjHS\|dERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
IMRS	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MlL3O\|IhcA>?		MXPJR\|UxRTh5MzDuUS=>	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMEO3OUc,OjV6MUCzO\|U9N2F-
SKNAS	MlXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NGnQTpA4OiCq		NIPJNYFKSzVy78{eNVAxODBibl2=	NEfBVXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
Rh28	MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MXO3NkBp		M3zaTWlEPTB;OES1JI5O	NXf3WGtpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
Rh41	NYD6NXpMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MkGxO\|IhcA>?		MYjJR\|UxRTdzOEegcm0>	NYDjcVNIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
CW9019	NXTU[Zc1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M{HMZVczKGh?		NY\M[Iw{UUN3ME25PVEzKG6P	NV3ISVNyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
Rh5	NYWySnI1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MkjSO\|IhcA>?		MYTJR\|Ux97zgMUCwNFAhdk1?	MojkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MUCzO\|UoRjJ3OEGwN\|c2RC:jPh?=
Rh30	NUD2fVFRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MXu3NkBp		MUjJR\|Ux97zgMUCwNFAhdk1?	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMEO3OUc,OjV6MUCzO\|U9N2F-
778	NWjsbpJQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M1;xXlczKGh?		NVfhe2hIcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>?	NXPBeIw5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
449	M1mxeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MUS3NkBp		MWLpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5	M2faSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
LP3	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NGraRlg4OiCq		NH\XWpVqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6	NXfQfoFbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
LP6	NITuPGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NXWwVJV4PzJiaB?=		Mlm3bY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:\|ZTDk[ZBmdmSnboTsfS=>	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB{OES2PUc,OjVyMki0Olk9N2F-
LP8	NFq1NopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NI\yUFY4OiCq		MVzpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB{OES2PUc,OjVyMki0Olk9N2F-
LPS141	NE\YU3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NWTmbFVRPzJiaB?=		NES4V5pqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6	Mn\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMki0OlkoRjJ3MEK4OFY6RC:jPh?=
778	Mmr3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2XicVMvOzNizszN	NIPCW2EzPCCq		NGThPIll\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=>	NF;ENoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyPFQ3QSd-MkWwNlg1Pjl:L3G+
449	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFHsc5Y{NjN\|IN88US=>	MVKyOEBp		M4TrbIRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB{OES2PUc,OjVyMki0Olk9N2F-
LP3	M{i4[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmjvN{4{OyEQvF2=	M{HhR\|I1KGh?		NFj3Xnhl\WO{ZXHz[ZMhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hWyCyaHHz[S=>	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB{OES2PUc,OjVyMki0Olk9N2F-
LP6	NHvHbZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYLz[HpUOy5\|MzFOwG0>	NG[wVoMzPCCq		M4qx[IRm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl	M17ISlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
LP8	M{e1[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NFKxT3g{NjN\|IN88US=>	MnSxNlQhcA>?		NX3wXmlC\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U>	M1zZeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
LPS141	NGKybG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYWzMlM{KM7:TR?=	MkHENlQhcA>?		MV;k[YNz\WG\|ZYOgeIhmKHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6gV{BxcGG\|ZR?=	NYXRT5lSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
IMR5	NEXtWpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NFe4eIwzPCCq	M4LOdGROW09?	MVvJR\|UxRTF{NjDuUS=>	NWLiW25[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
BE2C	M4OxcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NFTHfZQzPCCq	M3HQc2ROW09?	NIrLNlNKSzVyPUGzOEBvVQ>?	NGK2dGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
1643	MnvWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MVeyOEBp	NWHZSZk5TE2VTx?=	NEXFSolKSzVyPUG0O{BvVQ>?	NVi3WIFSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
SKNSH	NHvTT4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MoLLNlQhcA>?	NXfP[\|JrTE2VTx?=	MnXWTWM2OD1zNEigcm0>	NIn5c5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
SY5Y	M4PtfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MlHDNlQhcA>?	Mnv1SG1UVw>?	Mo\tTWM2OD1zNUSgcm0>	NH7ZemQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
NGP	M3;NR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NI\zboMzPCCq	M3qwWWROW09?	NVXRTox7UUN3ME2xO\|Uhdk1?	MoPlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNEWxO\|koRjJ2MES1NVc6RC:jPh?=
KELLY	NUnuSpRKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MUCyOEBp	M2\GdmROW09?	M4W0WmlEPTB;MkKwJI5O	NFrLfIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
CHP134	NEXaeW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NXm0dol1OjRiaB?=	NUfnZYV{TE2VTx?=	M2f3TWlEPTB;MkezJI5O	M{PhVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
NLF	MlXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MYqyOEBp	MmXsSG1UVw>?	MUfJR\|UxRTN{ODDuUS=>	NVjxdJh[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
LAN5	NX3GdZZFT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		Mm\jNlQhcA>?	MUDEUXNQ	NIL1O3JKSzVyPUSyPUBvVQ>?	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO\|k9N2F-
NB69	MmXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NIG5[IszPCCq	NHnXfnJFVVOR	NFPDdlVKSzVyPUezPEBvVQ>?	NXLzOY86RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
SKNDZ	NHu1bHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NEj3clQzPCCq	NXq0RVRZTE2VTx?=	NYn1fXZZUUN3ME24NFEhdk1?	MmrQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNEWxO\|koRjJ2MES1NVc6RC:jPh?=
NBSD	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NYXYZ5JIOjRiaB?=	MUnEUXNQ	NW\lZZVUUUN3ME2xPVAxKG6P	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO\|k9N2F-
SKNF1	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M3;4S\|I1KGh?	NEDBNYZFVVOR	NEnJWG1KSzVyPUO1NFAhdk1?	M4PFRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
EBC1	NVPXdYttT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MX6yOEBp	NV;NXXVlTE2VTx?=	MlPxTWM2OD14NECwJI5O	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO\|k9N2F-
SKNAS	M2DjUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NHrr[WYzPCCq	NUPhempHTE2VTx?=	MX;JR\|Ux97zgMUCwNFAhdk1?	NIDEZ4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
NB16	NULDT5A3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M13FV\|I1KGh?	M{LZRWROW09?	NE\yW4JKSzVy78{eNVAxODBibl2=	NVv3TnRFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
RPE1	M33rTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NXf5bZlQOjRiaB?=	NELUTWZFVVOR	Mmr4TWM2OO,:nkGwNFAxKG6P	NFzHZm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
Sf21	Mn3ZSpVv[3Srb36gZZN{[Xl?		MX:xNEBucW6\|		MVzJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKG[3bHygcIVv\3SqIF6teIVzdWmwYXygS3NVNXSjZ3fl[EBETEt2L1P5Z4xqdi2GMzDjc{1mgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgd4YzOSClZXzsd{B2e2mwZzDSZkB{fWK\|dILheIUhcW5icILld4Vv[2Vib3[gX4didW2jM{PQYWFVWCCjZoTldkAyOCCvaX7zJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnegcYV1cG:mLDDJR\|UxKD1iMD6wNVMh\|ryPLh?=	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVzOEOxNkc,Ojl3MUizNVI9N2F-
Sf21	M37pRWZ2dmO2aX;uJIF{e2G7		NYPwXJJpOTBibXnudy=>		M{HTZ2lvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iZoXscEBt\W6pdHigR{11\XKvaX7hcEA3UGm\|LYTh[4dm\CCFRFu5M2N6[2yrbj3UNUBkdy2neIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhe2Z{MTDj[YxteyC3c3nu[{BRTEu2aXTlJJN2[nO2cnH0[UBqdiCycnXz[Y5k\SCxZjDb[4FudWF\|M2DdRXRRKGGodHXyJFExKG2rboOgZpkhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDt[ZRpd2RuIFnDOVAhRSByLkG5O{DPxE1w	M3rDT\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N\|EzLz5{OUWxPFMyOjxxYU6=
HepG2	NHfDfZJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NEDFUZo4OiCqcoO=		NIHNSpNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxVcXSncj3HcI8h[XO\|YYmsJGVEPTBiPTCwMlI5PjJizszNMi=>	MkH4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2MEe5O\|UoRjJ7NEC3PVc2RC:jPh?=
SEM	MV3BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NETXPY84OiCqcoO=		MornRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCVRV2gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbGTpeIVzNUeubzDhd5NigSxiRVO1NEA:KDBwNE[wOUDPxE1w	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O\|U9N2F-
KOPN8	Mn34RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		M1fIOlczKGi{cx?=		Mk\qRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCNT2DOPEBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XsWIl1\XJvR3zvJIF{e2G7LDDFR\|UxKD1iMD61NFA5KM7:TT6=	NUTZd3g4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzVpPkK5OFA4QTd3PD;hQi=>
NCI-H1299	M{KxemN6fG:2b4jpZ4l1gSCjc4PhfS=>		MYO3NkBpenN?		MmjLR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUhzMkm5JINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgR2NMQCCjc4PhfUwhUUN3MDC9JFUvPDZizszNMi=>	NG\sNms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
T47D	M4PWc2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NVHjRWhnPzJiaILz		NHzVU3NIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBVPDeGIHPlcIx{KGmwY4XiZZRm\CCob4KgO\|IhcHK\|IHL5JGNEUzhiYYPzZZktKEmFNUCgQUA3NjJ{NzFOwG0v	MofNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4NUG5O\|koRjJ6NkWxPVc6RC:jPh?=
T47D	NGTLO4NEgXSxdH;4bYNqfHliYYPzZZk>		MWK3NkBpenN?		NEPoc\|JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVPDeGIHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB5MjDodpMh[nliQ1PLPEBie3OjeTygTWM2OCB;IE[uNlMh\|ryPLh?=	M1uwOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N\|EzLz5{OUWxPFMyOjxxYU6=
H1299	MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MmHlO\|IhcHK\|		NWf0[5NwT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUDF{OUmgZ4VtdHNiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhS0ONODDhd5NigSxiSVO1NEA:KDdwNkO3JO69VS5?	NHL3T4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[1NVk4QSd-Mki2OVE6Pzl:L3G+
KOPN8	MY\BdI9xfG:\|aYOgZZN{[Xl?	MoLiNE42KHWP	NXjUd2hzOyCqcoO=		M1TDZ2lv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iS1;QUlgh[2WubIOgZZN{\XO\|ZXSgZZMhfXC{ZXf1cIF1cW:wIH;mJINt\WG4ZXSgVGFTWCCuZY\lcEBifCByLkWgeW0h[W[2ZYKgN{BpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O\|U9N2F-
KOPN8	NX;SOlhGSXCxcITvd4l{KGG\|c3H5	MVWwMlUhfU1?	M2jIZ\|I1KGi{cx?=		MX;JcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEuRUF64JINmdGy\|IHHzd4V{e2WmIHHzJJVxemWpdXzheIlwdiCxZjDjcIVifmWmIGDBVnAhdGW4ZXygZZQhOC53IIXNJJBz\S22cnXheIVlKHerdHigUmFEKG[xcjCxJIhzKGGwZDDt[YF{fXKnZDDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O\|U9N2F-
Hep3B	NX63boExS2WubDDjfYNt\SCjc4PhfS=>		NXvEZYVXOjRiaILz		MY\D[YxtKGO7Y3zlJIFzemW\|dDDpckBpfW2jbjDI[ZA{SiClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzBxR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcoch[mG\|ZXSg[oxwfyCleYTvcYV1enl?	NXryc5RHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
HepG2	NIDQbGRE\WyuIHP5Z4xmKGG\|c3H5		Mm\3NlQhcHK\|		NXyzNGxUS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFewM2cyKHCqYYPlJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pIHLhd4VlKG[ub4egZ5l1d22ndIL5	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVzOEOxNkc,Ojl3MUizNVI9N2F-
A549	Mlr4R4VtdCCleXPs[UBie3OjeR?=		MonRNlQhcHK\|		MY\D[YxtKGO7Y3zlJIFzemW\|dDDpckBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W\|c3XkJIF{KGGlY4XteYxifGmxbjDheEBIOC:JMTDwbIF{\SCjZoTldkAzPCCqcoOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{Bj[XOnZDDmcI94KGO7dH;t[ZRzgQ>?	NFjhblI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
NCI-H460	NXPHPIU{S2WubDDjfYNt\SCjc4PhfS=>		NFrIbZgzPCCqcoO=		MmG5R4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gUmNKNUh2NkCgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFewM2cyKHCqYYPlJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pIHLhd4VlKG[ub4egZ5l1d22ndIL5	NWDxeYRURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
T47D	MV7D[YxtKGO7Y3zlJIF{e2G7		M2jUNFI1KGi{cx?=		MWHD[YxtKGO7Y3zlJIFzemW\|dDDpckBpfW2jbjDUOFdFKGOnbHzzJIF{e2W\|c3XkJIF{KGGlY4XteYxifGmxbjDheEBIOC:JMTDwbIF{\SCjZoTldkAzPCCqcoOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{Bj[XOnZDDmcI94KGO7dH;t[ZRzgQ>?	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVzOEOxNkc,Ojl3MUizNVI9N2F-
MDA-MB-231	MluxR4VtdCCleXPs[UBie3OjeR?=		NImyTVYzPCCqcoO=		M3LLfmNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJG1FSS2PQj2yN\|Eh[2WubIOgZZN{\XO\|ZXSgZZMh[WOldX31cIF1cW:wIHH0JGcxN0dzIIDoZZNmKGGodHXyJFI1KGi{czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nJIJie2WmIH\sc5ch[3m2b33leJJ6	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTVzOEOxNkc,Ojl3MUizNVI9N2F-
Fluc-labeled 4T1	MkjRRY51cXS3bX;yJIF{e2G7	MUKxN\|AhdWdxa3e=	M4DoSFE5KGSjeYO=		NHTVUHZCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBud3W\|ZTDGcJVkNWyjYnXs[YQhPFRzIHPlcIx{KGmvcHzhcpRm\CCrbjDCZYxjN2NibX;1d4Uh[XO\|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJJR2dW:{IIflbYdpfCCjdDCxN\|AhdWdxa3esJIlxKGGmbXnubZN1\XKnZDDkZYltgSCob4KgNVgh\GG7czDt[YF{fXKnZDDh[pRmeiB6IITvJFI2KGSjeYO=	MnzZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MUizNVIoRjJ7NUG4N\|EzRC:jPh?=
T47D	MXXD[YxtKGO7Y3zlJIF{e2G7		MV2yOEBpenN?		Ml7HTY5lfWO2aX;uJI9nKGOnbHygZ5lkdGViYYLy[ZN1KGmwIHj1cYFvKFR2N1SgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hTzBxR{GgdIhie2ViYXPjeY12dGG2aX;uJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IH\sc5ch[3m2b33leJJ6	NWHuXowzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2OVE6PzlpPkK4OlUyQTd7PD;hQi=>

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	29789630
Growth inhibition assay	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]	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.
動物試験： ^[1]	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.

細胞試験：

^[1]

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.

動物試験：

^[1]

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	[1] Rader J, et al. Clin Cancer Res. 2013, 19(22), 6173-6182. [2] Antonio Marra, Giuseppe Curigliano. NPJ Breast Cancer. 2019 Aug 29;5:27.

溶解度 (25°C)

体外

化学情報

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

Ribociclib (LEE011) SDFをダウンロードする

投与溶液組成計算機(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 g 投与体積（動物毎）μL 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

%DMSO+ %

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：Take 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。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

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

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

臨床試験

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)

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

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電話番号

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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):