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]|よく尋ねられる質問

文献中Selleckの製品使用例(54)

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	M{DoW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M2rUe\|I1KGh?		M4fEZmdKPTB;Mke2JI5O	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh3MkC1PEc,OjV6NUKwOVg9N2F-
Myoblast	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NI\lcJQ4OiCq		M4LZNGlEPTB;MUCzOUBvVQ>?	NH;nRmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
IMRS	NFPnd2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MkDoO\|IhcA>?		NITXZ4xKSzVyPUi3N{BvVQ>?	NIH3[Is9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
SKNAS	M{PEWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NU\yb4pnPzJiaB?=		Mn\FTWM2OO,:nkGwNFAxKG6P	M1jvNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEGwN\|c2Lz5{NUixNFM4PTxxYU6=
Rh28	MlPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MlHMO\|IhcA>?		NEWw[IJKSzVyPUi0OUBvVQ>?	NX\rOG9SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
Rh41	NHTpcWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MnfRO\|IhcA>?		Mn7LTWM2OD15MUi3JI5O	NGXrS5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
CW9019	NWrG[\|RjT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MVy3NkBp		MmjrTWM2OD17OUGyJI5O	NE\NVoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUixNFM4PSd-MkW4NVA{PzV:L3G+
Rh5	MkjjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MoH4O\|IhcA>?		NUHaSXROUUN3MP-8olExODByIH7N	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPThzMEO3OUc,OjV6MUCzO\|U9N2F-
Rh30	NHjzUGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MYe3NkBp		NWTBeXdmUUN3MP-8olExODByIH7N	NWLpO3poRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NVA{PzVpPkK1PFExOzd3PD;hQi=>
778	M2Hlbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NYL6OXF3PzJiaB?=		MVPpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5	Mn3CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMki0OlkoRjJ3MEK4OFY6RC:jPh?=
449	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M4jZXlczKGh?		NWLOU\|dGcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>?	NGXpOVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyPFQ3QSd-MkWwNlg1Pjl:L3G+
LP3	MoHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NHzBXWE4OiCq		NW\wcGpjcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>?	NF7LOnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyPFQ3QSd-MkWwNlg1Pjl:L3G+
LP6	MoXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NVfEdZlbPzJiaB?=		NEDaNFJqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6	NU\oNlFGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
LP8	MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MkXZO\|IhcA>?		NFn1SIdqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6	M{S2dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
LPS141	NHfDdIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NU\WcnNHPzJiaB?=		NGrLRlVqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6	NWfRd5NxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
778	NFrCU\|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnT0N{4{OyEQvF2=	NYXrPYVEOjRiaB?=		M{Wwb4Rm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl	Mm\5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMki0OlkoRjJ3MEK4OFY6RC:jPh?=
449	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmjBN{4{OyEQvF2=	NFfnR3ozPCCq		M17BT4Rm[3KnYYPld{B1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBUKHCqYYPl	NVzwcGZpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwNlg1PjlpPkK1NFI5PDZ7PD;hQi=>
LP3	MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MW[zMlM{KM7:TR?=	Mor4NlQhcA>?		NVuz[GZv\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U>	M4TaPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEK4OFY6Lz5{NUCyPFQ3QTxxYU6=
LP6	M{[yNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Ml3QN{4{OyEQvF2=	NHHyPWMzPCCq		NYTh[\|hI\GWlcnXhd4V{KHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKFNicHjhd4U>	NEf6N5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyPFQ3QSd-MkWwNlg1Pjl:L3G+
LP8	MoXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXf2Z2R1Oy5\|MzFOwG0>	NGDVXWUzPCCq		MmLX[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy\|IHnuJHMheGijc3W=	NH\ZNnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUCyPFQ3QSd-MkWwNlg1Pjl:L3G+
LPS141	NYrnSGdnT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYOzMlM{KM7:TR?=	MWCyOEBp		Ml3w[IVkemWjc3XzJJRp\SCycn;wc5J1cW:wIH;mJINmdGy\|IHnuJHMheGijc3W=	Mn3JQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyMki0OlkoRjJ3MEK4OFY6RC:jPh?=
IMR5	NVrC[WNKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MkLRNlQhcA>?	NVPPcnZJTE2VTx?=	MV\JR\|UxRTF{NjDuUS=>	Mor1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNEWxO\|koRjJ2MES1NVc6RC:jPh?=
BE2C	MmOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NFnj[4EzPCCq	MVTEUXNQ	NGj5TYpKSzVyPUGzOEBvVQ>?	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO\|k9N2F-
1643	MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NWf2TlBKOjRiaB?=	NIjjfo1FVVOR	NGPDcZRKSzVyPUG0O{BvVQ>?	NV3OeFVzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
SKNSH	NGTGU3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M2TYSFI1KGh?	NGPBfnhFVVOR	NUDrU4M1UUN3ME2xOFghdk1?	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO\|k9N2F-
SY5Y	MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M{nET\|I1KGh?	MoTRSG1UVw>?	NFLRfGtKSzVyPUG1OEBvVQ>?	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO\|k9N2F-
NGP	NVP5bIFST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NFe2fnEzPCCq	M1LGUWROW09?	NVfXSGNiUUN3ME2xO\|Uhdk1?	MoHHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNEWxO\|koRjJ2MES1NVc6RC:jPh?=
KELLY	NHXuV2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M{G5S\|I1KGh?	M3\PPWROW09?	MYfJR\|UxRTJ{MDDuUS=>	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO\|k9N2F-
CHP134	NG\RVYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NEDRUFYzPCCq	NGK5NnVFVVOR	MYfJR\|UxRTJ5MzDuUS=>	M3qxTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
NLF	NF:2U5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Mny3NlQhcA>?	NVHrTlJbTE2VTx?=	M1[1OWlEPTB;M{K4JI5O	NEjVOJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
LAN5	Mom3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M4W4T\|I1KGh?	Mln5SG1UVw>?	NV;QZ4RNUUN3ME20Nlkhdk1?	M13wOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
NB69	NETPfWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MWWyOEBp	MX;EUXNQ	NEPPNmdKSzVyPUezPEBvVQ>?	NFTLUVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC0OVE4QSd-MkSwOFUyPzl:L3G+
SKNDZ	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NFy2TmYzPCCq	MkPBSG1UVw>?	NYrYZVRUUUN3ME24NFEhdk1?	NXqxSW9YRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
NBSD	NFPXR2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NWfTPGFLOjRiaB?=	NHu3OWNFVVOR	NWXSWnN7UUN3ME2xPVAxKG6P	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO\|k9N2F-
SKNF1	M{PYZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M1u2TFI1KGh?	M1rJ[GROW09?	NIPSW21KSzVyPUO1NFAhdk1?	NXnZU3hlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
EBC1	MkPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MlnvNlQhcA>?	MmHWSG1UVw>?	MU\JR\|UxRTZ2MECgcm0>	MnXXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNEWxO\|koRjJ2MES1NVc6RC:jPh?=
SKNAS	NIrQOmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NIXqUlEzPCCq	MmPJSG1UVw>?	MXHJR\|Ux97zgMUCwNFAhdk1?	M4fFWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MES1NVc6Lz5{NEC0OVE4QTxxYU6=
NB16	NW\6[I1jT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NXzNPVdPOjRiaB?=	Ml7OSG1UVw>?	NIPhTGdKSzVy78{eNVAxODBibl2=	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2NUG3PUc,OjRyNEWxO\|k9N2F-
RPE1	MlnIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MX2yOEBp	NIi0TYdFVVOR	NGDMboxKSzVy78{eNVAxODBibl2=	NUm2V2FxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOFUyPzlpPkK0NFQ2OTd7PD;hQi=>
Sf21	MkLSSpVv[3Srb36gZZN{[Xl?		NVfNSYdwOTBibXnudy=>		M{P3eGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iZoXscEBt\W6pdHigUk11\XKvaX7hcEBIW1RvdHHn[4VlKEOGS{SvR5lkdGmwLVSzJINwNWW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EB{\jJzIHPlcIx{KHW\|aX7nJHJjKHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBc\2GvbXGzN3BeSVSSIHHmeIVzKDFyIH3pcpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{Bu\XSqb3SsJGlEPTBiPTCwMlAyOyEQvF2u	NYPEZWVCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
Sf21	MULGeY5kfGmxbjDhd5NigQ>?		MnHRNVAhdWmwcx?=		MUDJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKG[3bHygcIVv\3SqIFOteIVzdWmwYXygOmhqey22YXfn[YQhS0SNOT;DfYNtcW5vVEGgZ48u\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJJNnOjFiY3XscJMhfXOrbnegVGRMfGmmZTDzeYJ{fHKjdHWgbY4heHKnc3XuZ4Uhd2ZiW3fhcY1iOzOSXVHUVEBi\nSncjCxNEBucW6\|IHL5JJNkcW62aXzsZZRqd25iY3;1cpRqdmdibXX0bI9lNCCLQ{WwJF0hOC5zOUeg{txONg>?	NYrKclBRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
HepG2	MkLhRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NFLxWHI4OiCqcoO=		MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy\|IHHmeIVzKDd{IHjyd{BjgSCFZXzUbZRmei2JbH:gZZN{[XluIFXDOVAhRSByLkK4OlIh\|ryPLh?=	NU\1V45VRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzVpPkK5OFA4QTd3PD;hQi=>
SEM	NECye4RCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MXu3NkBpenN?		NH2yWVlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPFUUBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XsWIl1\XJvR3zvJIF{e2G7LDDFR\|UxKD1iMD60OlA2KM7:TT6=	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTRyN{m3OUc,Ojl2MEe5O\|U9N2F-
KOPN8	M4q5PWFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NITIXm84OiCqcoO=		M2H0NWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1;QUlgh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcHRqfGW{LVfsc{Bie3OjeTygSWM2OCB;IECuOVAxQCEQvF2u	NX;SbnoyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzVpPkK5OFA4QTd3PD;hQi=>
NCI-H1299	NH75eY9EgXSxdH;4bYNqfHliYYPzZZk>		MXG3NkBpenN?		NILUXmZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSEGyPVkh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBES0t6IHHzd4F6NCCLQ{WwJF0hPS52NjFOwG0v	M3;kNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N\|EzLz5{OUWxPFMyOjxxYU6=
T47D	NYe2ZoV3T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NEHz[ZQ4OiCqcoO=		NWO3U4lWT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hXDR5RDDj[YxteyCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBES0t6IHHzd4F6NCCLQ{WwJF0hPi5{Mkeg{txONg>?	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ3MUm3PUc,Ojh4NUG5O\|k9N2F-
T47D	Mnz4R5l1d3SxeHnjbZR6KGG\|c3H5		NFnPNng4OiCqcoO=		M1;HcGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHQ1P0RiY3XscJMh[XO\|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCFQ1u4JIF{e2G7LDDJR\|UxKD1iNj6yN{DPxE1w	NEfRU\|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
H1299	MmnnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M1LQZVczKGi{cx?=		M2HyRWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGgyOjl7IHPlcIx{KGmwY4XiZZRm\CCob4KgO\|IhcHK\|IHL5JGNEUzhiYYPzZZktKEmFNUCgQUA4NjZ\|NzFOwG0v	NYfVPIVrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2OVE6PzlpPkK4OlUyQTd7PD;hQi=>
KOPN8	MkHTRZBweHSxc3nzJIF{e2G7	NUW4eFZGOC53IIXN	NFfwdnA{KGi{cx?=		Ml7vTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCNT2DOPEBk\WyuczDhd5Nme3OnZDDhd{B2eHKnZ4XsZZRqd25ib3[gZ4xm[X[nZDDQRXJRKGyndnXsJIF1KDBwNTD1UUBi\nSncjCzJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM>	M1y0N\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEC3PVc2Lz5{OUSwO\|k4PTxxYU6=
KOPN8	M3u5UGFxd3C2b4Ppd{Bie3OjeR?=	NIjic3QxNjVidV2=	NWjHZZo3OjRiaILz		MkDwTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCNT2DOPEBk\WyuczDhd5Nme3OnZDDhd{B2eHKnZ4XsZZRqd25ib3[gZ4xm[X[nZDDQRXJRKGyndnXsJIF1KDBwNTD1UUBxemVvdILlZZRm\CC5aYToJG5CSyCob4KgNUBpeiCjbnSgcYVie3W{ZXSgZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=>	NUfR[4tpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0NFc6PzVpPkK5OFA4QTd3PD;hQi=>
Hep3B	M2nlfmNmdGxiY4njcIUh[XO\|YYm=		MWiyOEBpenN?		NVvSOFNPS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hUGWyM1KgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFewM2cyKHCqYYPlJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pIHLhd4VlKG[ub4egZ5l1d22ndIL5	NFXHN3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWxPFMyOid-Mkm1NVg{OTJ:L3G+
HepG2	MX7D[YxtKGO7Y3zlJIF{e2G7		MmfCNlQhcHK\|		M4[0V2NmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG\|c3Xzd4VlKGG\|IHHjZ5VufWyjdHnvckBifCCJMD;HNUBxcGG\|ZTDh[pRmeiB{NDDodpMh[nlicILvdIllcXWvIHnv[Ill\SC\|dHHpcolv\yCkYYPl[EBndG:5IHP5eI9u\XS{eR?=	NXL4SmhPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
A549	M122[2NmdGxiY4njcIUh[XO\|YYm=		MkLENlQhcHK\|		M2\XcmNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGE2PDliY3XscJMh[XO\|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdyL1exJJBp[XOnIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oKGKjc3XkJIZtd3diY4n0c41mfHK7	M{HIV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N\|EzLz5{OUWxPFMyOjxxYU6=
NCI-H460	MlTzR4VtdCCleXPs[UBie3OjeR?=		MlPGNlQhcHK\|		MU\D[YxtKGO7Y3zlJIFzemW\|dDDpckBpfW2jbjDOR2kuUDR4MDDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{CvS\|EheGijc3WgZYZ1\XJiMkSgbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdiYnHz[YQh\myxdzDjfZRwdWW2com=	NU\vUZVRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
T47D	MWDD[YxtKGO7Y3zlJIF{e2G7		Ml\XNlQhcHK\|		MlLUR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gWFQ4TCClZXzsd{Bie3Onc4Pl[EBieyCjY3P1cZVt[XSrb36gZZQhTzBxR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcoch[mG\|ZXSg[oxwfyCleYTvcYV1enl?	M4rj[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUG4N\|EzLz5{OUWxPFMyOjxxYU6=
MDA-MB-231	MXfD[YxtKGO7Y3zlJIF{e2G7		MlPBNlQhcHK\|		M3TR[2NmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJG1FSS2PQj2yN\|Eh[2WubIOgZZN{\XO\|ZXSgZZMh[WOldX31cIF1cW:wIHH0JGcxN0dzIIDoZZNmKGGodHXyJFI1KGi{czDifUBxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nJIJie2WmIH\sc5ch[3m2b33leJJ6	NUfVO3U{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
Fluc-labeled 4T1	NGTLcZFCdnSrdIXtc5Ih[XO\|YYm=	Mn\INVMxKG2pL3vn	Mmq3NVgh\GG7cx?=		NXzmbINySW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhdW:3c3WgSox2[y2uYXLlcIVlKDSWMTDj[YxteyCrbYDsZY51\WRiaX6gRoFt[i:lIH3veZNmKGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckB1fW2xcjD3[YlocHRiYYSgNVMxKG2pL3vnMEBqeCCjZH3pcol{fGW{ZXSg[IFqdHliZn;yJFE5KGSjeYOgcYVie3W{ZXSgZYZ1\XJiODD0c{AzPSCmYYnz	NV3MTY4xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NVg{OTJpPkK5OVE5OzF{PD;hQi=>
T47D	M1PRW2NmdGxiY4njcIUh[XO\|YYm=		NIe0S20zPCCqcoO=		MkDRTY5lfWO2aX;uJI9nKGOnbHygZ5lkdGViYYLy[ZN1KGmwIHj1cYFvKFR2N1SgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hTzBxR{GgdIhie2ViYXPjeY12dGG2aX;uJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IH\sc5ch[3m2b33leJJ6	NFi2fmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[1NVk4QSd-Mki2OVE6Pzl:L3G+

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 2021-05-17)

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

他に質問がある場合は、お気軽にお問い合わせください。

* 必須
*大学・企業名:
*名前:
*電子メール:
*電話番号:
*内容:

CDKシグナル伝達経路

相関CDK製品

SU9516

SU 9516 is a 3-substituted indolinone CDK inhibitor with IC50 of 22 nM, 40 nM, and 200 nM for CDK2, CDK1, and CDK4, respectively.
Ro-3306

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.
Purvalanol A

Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy.
Palbociclib (PD-0332991) HCl

Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

Features:Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).
Palbociclib (PD0332991) Isethionate

Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

Features:The 1st specific inhibitor for CDK4/6 to show promise in multiple cancers.
Dinaciclib (SCH727965)

Dinaciclib (SCH727965, PS-095760) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3.
Flavopiridol (L86-8275) HCl

Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.

研究分野別

製品類型

Ribociclib (LEE011)

文献中Selleckの製品使用例(54)

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 2021-05-17)

技術サポート

CDKシグナル伝達経路

相関CDK製品