Rucaparib (AG-014699) phosphate

For research use only. Not for use in humans.

製品コードS1098 別名：PF-01367338

CAS No. 459868-92-9

Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with K_i of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.

サイズ

価格(税別)

10mM (1mL in DMSO)	JPY 24200
5mg	JPY 21900
10mg	JPY 36800
50mg	JPY 113200

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(103)

製品安全説明書

PARP阻害剤の選択性比較

生物活性

製品説明

Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with K_i of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.

特性

The first PARP inhibitor used in clinical trials combined with temozolomide.

ターゲット

PARP ^[1]
(Cell-free assay)

1.4 nM(Ki)

体外試験

Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells. Besides, Rucaparib binds detectably to eight other PARP domains, including PARP2, 3, 4, 10, 15, 16, TNKS1 and TNKS2. ^[1] ^[2] The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. ^[3] Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells. ^[4]

細胞データ

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
BT-474	MYjGeY5kfGmxbjDBd5NigQ>?	M{HpWFAvOS9zL{WwNE8yODByIH7N			NUHGd2EzcW6qaXLpeJMhWEGUUDDhZ5Rqfmm2eTDheEB{fGG{dHnu[{Bkd26lZYLueJJifGmxbjDv[kA2ODBibl2=	Ml;kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMki0OVUoRjJ3MUK4OFU2RC:jPh?=
BT474	M1;GdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYLZXodYPTByIH7N	NFq1TJgyOOLCk{G1xsBl		Mn7jdoVlfWOnczDj[YxtKGe{b4f0bEBqdiC2aHWg[o92eiCuaX7ld{BidmRic3nncolncWOjboTsfS=>	M1jWSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUK4OFU2Lz5{NUGyPFQ2PTxxYU6=
SKBR3	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2X5WlUxOCCwTR?=	M{PydlEx6oDVMUZCpIQ>		M3jtd5Jm\HWlZYOgZ4VtdCCpcn;3eIghcW5idHjlJIZwfXJibHnu[ZMh[W6mIIPp[45q\mmlYX70cJk>	NGLMfXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyPFQ2PSd-MkWxNlg1PTV:L3G+
AU565	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1XkfFUxOCCwTR?=	NY\jUWVrOTEkgKOxOeKh\A>?		M{SxWpJm\HWlZYOgZ4VtdCCpcn;3eIghcW5idHjlJIZwfXJibHnu[ZMh[W6mIIPp[45q\mmlYX70cJk>	NFmwUpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyPFQ2PSd-MkWxNlg1PTV:L3G+
EFM192A	M1fJb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkK0OVAxKG6P	M3rXSVEx6oDVMUZCpIQ>		NXHMZpJ[emWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>?	M333fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUK4OFU2Lz5{NUGyPFQ2PTxxYU6=
MDA-MB-231	NFXhU\|VHfW6ldHnvckBCe3OjeR?=	M37Dc\|ExNzJyL{SwJO69VQ>?	MVuyOEBp		NGTTdodqdmO{ZXHz[ZMheC2DS2SgcIV3\Wy\|IHnuJIEh\G:\|ZT3k[ZBmdmSnboSgcYFvdmW{	NWq3fWNvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NlAyPTJpPkK0OFIxOTV{PD;hQi=>
MDA-MB-231	Ml;nR4VtdCCYaXHibYxqfHliQYPzZZk>	M{DxZlAvOS12MDFOwG0>	NF3PemgzPCCq		NGD4fpBKSzVy4pEJQgKBkTF5Lke3xsDPxE1?	NVXSfG8yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NlAyPTJpPkK0OFIxOTV{PD;hQi=>
MDA-MB-231	MX7BdI9xfG:\|aYOgRZN{[Xl?	MlnUNVAwOjBxNECg{txO	MkDzNlQhcA>?		MnLQbY5lfWOnczDhdI9xfG:\|aYOg[I9{\SCmZYDlcoRmdnSueR?=	M3O0d\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEKwNVUzLz5{NESyNFE2OjxxYU6=
MDA-MB-231	NYTWNoE3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Ml;QNVAwOjBxNECg{txO	MlT4NlQhcA>?		Mn76Zoxw[2u\|IHPlcIwh[3mlbHWgdJJw\3Knc4Ppc44hcW5iR{KvUUBxcGG\|ZR?=	NY\OTpZ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NlAyPTJpPkK0OFIxOTV{PD;hQi=>
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COLO704	M3rMPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NXrpeWh7UUN3ME2yMlUzKMLzIECuOlch\|ryP	MojqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
OVMANAb	NVLnUmhVT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NH3aPY1KSzVyPUKuOVghyrFiMD6zPEDPxE1?	MorXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
OV177	NEnHfmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NF;PNHFKSzVyPUKuO\|ghyrFiMD63NUDPxE1?	M3;3O\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
OAW28	Ml7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MnLITWM2OD1\|Lk[xJOKyKDBwMkig{txO	M1jxUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
OVSAHO	Mlz6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NH3hTGpKSzVyPUOuOlQhyrFiMD6zN{DPxE1?	MmHFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
OVKATE	NVnlZldoT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MUPJR\|UxRTNwNkSgxtEhOS55OTFOwG0>	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OVCAR3	MnHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MWLJR\|UxRTNwN{SgxtEhOC52MDFOwG0>	NYP4W2lJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
PEO14	NW\sbFc{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MmTsTWM2OD1\|Lki0JOKyKDBwN{[g{txO	M3jjW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
A2780	Mo\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MVjJR\|UxRTNwOUSgxtEhOC5{NTFOwG0>	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OVTOKO	NW\NOlZmT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NVrHeXFTUUN3ME20MlE1KMLzIEGuOVMh\|ryP	MmniQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
KURAMOCHIb	NHzBZXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NI\s[VdKSzVyPUSuN\|QhyrFiMD6yPUDPxE1?	NGDCbIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
TOV21G	Ml3lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MWHJR\|UxRTVwMEegxtEhOS5\|MDFOwG0>	NIDtN3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
OVISE	NXzVW3JkT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MWPJR\|UxRTVwNkigxtEhOC5{MzFOwG0>	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
KK	M3Xi[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MWXJR\|UxRTZwMUWgxtEhOS52MjFOwG0>	NUTWbIFHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
RMUGS	NEWy[mNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NIjGN2pKSzVyPUeuNFMhyrFiMT64N{DPxE1?	MoLuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
PEO6	NGrC[5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M2nRdmlEPTB;Nz6wOkDDuSByLke0JO69VQ>?	NXnWZYJ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
OVCA429	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NEnK[2RKSzVyPUiuNlkhyrFiMT62OEDPxE1?	NIftUm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
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RMG1	MnnIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NVrVN2dMUUN3ME25MlMzKMLzIEKuN\|Yh\|ryP	M1jhbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
OVCAR5	NWrqfVRyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MV\JR\|UxRTlwNUCgxtEhOi53OTFOwG0>	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
EFO21	NWO4XoVFT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M3W0e2lEPTB;OT65NkDDuSBzLki3JO69VQ>?	MkDlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
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DOV13	MmDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NHywOmJKSzVyPkG1JO69VQ>?	NGLldpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
EFO27	Mmr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MUTJR\|UxRjF3IN88US=>	M{fpRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
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VCaP	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2jzT\|AuOyEQvF2=	MWqxOEBl	MWLEUXNQ	NFjsZoxl\WO{ZXHz[ZMh[2:ub375JI52dWKncjDkc5NmKGSncHXu[IVvfGy7	MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV4NUK0OEc,OjN3NkWyOFQ9N2F-
LNCaP	NILhZZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXTxWWt4OC1\|IN88US=>	MmnnNVQh\A>?	NWn5ZlB[TE2VTx?=	NGLGdZRl\WO{ZXHz[ZMh[2:ub375JI52dWKncjDkc5NmKGSncHXu[IVvfGy7	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV4NUK0OEc,OjN3NkWyOFQ9N2F-
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MDA-MB-231	M4PXOGNmdGxiVnnhZoltcXS7IFHzd4F6				M4rFbWlEPTB;MUOg{txO	NH\SXJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[3PFE3OSd-MkK2O\|gyPjF:L3G+
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LoVo	MUTGeY5kfGmxbjDhd5NigQ>?		NF7UfIM{OCCvaX7z		MWjJcohq[mm2aX;uJI9nKFCDUmCgbY4hcHWvYX6gUI9XdyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJBwdHlqQVTQLU1zcWKxc3WgdI9tgW2ncnn6ZZRqd25iZn;yJFMxKG2rboOgZpkh\my3b4Lld4NmdmOnIHHzd4F6NCCHQ{WwJF0hOC5yMES2PUDPxE1w	Mln0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO\|E4RC:jPh?=
MX1	NYroXYVIS3m2b4TvfIlkcXS7IHHzd4F6				M{D5PGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEKUQ1GxMYRm\mmlaXXueEBpfW2jbjDNXFEh[2WubIOsJGVEPTBiPTCwMlAxPTNizszNMi=>	M3;LW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO\|E4Lz5{Nk[1NlcyPzxxYU6=
Rosetta2 (DE3)	NUfnc\|hrTnWwY4Tpc44h[XO\|YYm=				Mme5TY5pcWKrdHnvckBw\iCqdX3hckBPNXSncn3pcoFtKD[6aHnzMZRi\2enZDDBVnRFPiBqOEezJJRwKDFzNkGpJIV5eHKnc4Pl[EBqdiCHc3Po[ZJq[2irYTDjc4xqKFKxc3X0eIEzKCiGRUOpJINmdGy\|IIXzbY5oKE6DRDugZZMhe3Wkc4TyZZRmKGK7IH\seY9z\XOlZX7j[UBie3OjeTygTWM2OCB;IECuNFE1KM7:TT6=	M3j5dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwO\|cxLz5{NEmwNFc4ODxxYU6=
Rosetta2 (DE3)	MXfGeY5kfGmxbjDhd5NigQ>?				MVfJcohq[mm2aX;uJI9nKGi3bXHuJFZ5cGm\|LYTh[4dm\CCDUmTEOUApOTB\|MDD0c{AyOzF5KTDlfJBz\XO\|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBTd3OndIThNkApTEV\|KTDj[YxteyC3c3nu[{BPSURtIHHzJJN2[nO2cnH0[UBjgSCobIXvdoV{[2WwY3WgZZN{[XluIFnDOVAhRSByLkCyOUDPxE1w	M3jDO\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwO\|cxLz5{NEmwNFc4ODxxYU6=
LoVo	M3fZXGN6fG:2b4jpZ4l1gSCjc4PhfS=>	MnLrNE41KHWP	NGPZWoY2KGSjeYO=		M2f5XXBwfGWwdHnheIlwdiCxZjD0[Y1wgm:ub33p[IUucW6mdXPl[EBkgXSxdH;4bYNqfHliaX6gbJVu[W5iTH;Wc{Bk\WyuczDhd5Nme3OnZDDhd{B1\W2xen;sc41q\GViR1m1NEBifCByLkSgeW0h[W[2ZYKgOUBl[Xm\|IHL5JGNmdGy2aYTldk1IdG9iYYPzZZktKEeLNUCgQUAxNjF2NDFOwG0v	NHKxbJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
Capan1	MoXZR5l1d3SxeHnjbZR6KGG\|c3H5				M1vjSGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEKUQ1GyMYRm\mmlaXXueEBpfW2jbjDDZZBidjFiY3XscJMtKEWFNUCgQUAxNjZyOTFOwG0v	MmnZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO\|E4RC:jPh?=
MDA-MB-436	Mn;sRY51cWOjbnPldkBie3OjeR?=		MXG5OkBpenN?		M{XVVWFvfGmlYX7j[ZIh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCVmNCOS2mZX\pZ4lmdnRiTVTBMW1DNTR\|NjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6NCCFQ{WwJF0hOyEQvF2u	NF;jPXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO0Nlg3QCd-Mk[zOFI5Pjh:L3G+
OVCAR3	M3OxOmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MoCxNlQhcHK\|		Mn31RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCRVlPBVlMh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEOuN\|Eh\|ryPLh?=	Ml;PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NU[xNFYoRjJ7NEW2NVA3RC:jPh?=
MRC5	NV7Pb5NoS3m2b4TvfIlkcXS7IHHzd4F6				NHzCRpdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOWkN3IHPlcIx{NCCHQ{WwJF0hQC53MzFOwG0v	NFLKfYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
MCF7	NUXKVWNUSW62aXPhcoNmeiCjc4PhfS=>		MXm5OkBpenN?		MWPBcpRq[2GwY3XyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB7NjDodpMh[nliTWTUJIF{e2G7LDDDR\|UxKD1iMUmuOFch\|ryPLh?=	NV7Bb4lNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOFI5PjhpPkK2N\|QzQDZ6PD;hQi=>
A673	M2G2VJFJXFNiYYPzZZk>				M2S5SJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy\|	NXS5WXhKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673	NFrHfZZyUFSVIHHzd4F6				MmjldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRVY4OyClZXzsd{k>	NGHjc5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Rh41	MlnCdWhVWyCjc4PhfS=>				MkXUdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog1OSClZXzsdy=>	NFLNVVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
SK-N-MC	NWn2NVdTeUiWUzDhd5NigQ>?				NWHUR256eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	NVL1bJpGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32	NYjjbJN1eUiWUzDhd5NigQ>?				NXLTflRIeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXEN\|MjDj[Yxtew>?	NHPMO3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl: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	BRCA1; PubMed: 24085845 Proc Natl Acad Sci U S A MCF7 cells, MDA-MB-436 parental cells and resistant clones RR-1, RR-5, and RR-6 were treated with DMSO (−) or 1 µM rucaparib (+) for 24 h, and BRCA1 protein levels were assessed by using BRCA1 N- or C-terminal-specific antibodies by Western blot. PAR; PubMed: 27960087 Cancer Cell MCF-7 cells were pretreated ± Rucaparib (15 µM, 2 hr), then ± Rucaparib (15 µM) or two different doses of β-lap (2.0 or 5.0 µM) for 2 hr. Levels of PAR (PARP hyperactivation) formation were assessed with α-tubulin as loading controls.	24085845 27960087
Growth inhibition assay	Cell viability; PubMed: 31119062 Adv Wound Care (New Rochelle) The effect of rucaparib on proliferation of keloid fibroblasts. (A) Keloid cell growth following treatment with rucaparib at various concentration (0, 2, 10, 20 μM) was evaluated by MTT assays. Data are expression as mean standard deviation of percent changes of triplicate optical densities. (B) Rucaparib (20 μM) significantly decreased proliferation of keloid fibroblasts. The combination of rucaparib (20 μM) and triamcinolone (50 μM) showed additive suppressive effect on keloid fibroblasts as compared with rucaparib single therapy. Data are expression as mean standard deviation of percent changes of triplicate optical densities. MTT, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide.	31119062
Immunofluorescence	53BP1; PubMed: 23565244 PLoS One 53BP1 foci was determined by immunofluoresecence microscopy at 24 h following combined treatment with radiation and rucaparib in PC3 and LNCaP cells. γH2AX; PubMed: 23565244 PLoS One γH2AX foci was determined by immunofluoresecence microscopy at 24 h following combined treatment with radiation and rucaparib in PC3 and LNCaP cells. PAR; PubMed: 27515310 BMC Cancer Cells were treated with 20 mM hydrogen peroxide (H2O2) in order to stimulate PARP-1 activity in the presence or absence of the PARP-1 inhibitors rucaparib and olaparib. Poly(ADP-ribose) (PAR) chain synthesis was detected using an anti-PAR monoclonal Alexa Fluor 488-conjugated antibody (green). The nucleus was visualised using the nuclear counterstain DAPI (blue). Representative images obtained from the analysis of anti-PAR staining of SK-N-BE(2c) cells are shown. α-tubulin; PubMed: 30589644 J Clin Invest Representative immunofluorescence images of DMSO-, rucaparib- (Ruca-), and Ola-exposed A549-ERCC1(WT/WT) and A549-ERCC1(–/–) cells. Cells were exposed to 15 μM Ruca or 40 μM Ola during 72 hours. White arrows, CCFs; yellow arrows, micronuclei. Scale bar: 20 μm.	23565244 27515310 30589644

体内試験

Rucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy. ^[4] Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts. ^[5]

お薦めの試験操作（参考用のみ）

キナーゼ試験：^[1]	- 合併 K_i Determination: Inhibition of human full-length recombinant PARP-1 by [³²P]NAD⁺ incorporation is measured. The [³²P]ADP-ribose incorporated into acid insoluble material is quantified using a PhosphorImager. K_i is calculated by nonlinear regression analysis.
細胞試験： ^[4]	- 合併細胞株： D425Med, D283Med and D384Med cells 濃度： 0.4 μM 反応時間： 3 or 5 days 実験の流れ： Medulloblastoma cell lines are seeded in 96-well plates at a density of 1 × 10³, 3 × 10³ and 3 × 10³, respectively. At 24 hours (D384Med) or 48 hours (D283Med and D425Med) after seeding, the cells are exposed to various concentrations of temozolomide in the presence or absence of 0.4 μM Rucaparib. After 3 days (D425Med and D384Med) or 5 days (D283Med) of culture, cell viability is evaluated by a XTT cell proliferation kit assay. Cell growth is expressed as a percentage in relation to DMSO or 0.4 μM Rucaparib-alone controls. The concentration of temozolomide, alone or in combination with Rucaparib that inhibited growth by 50% (GI50) is calculated. The potentiation factor 50 (PF50) is defined as the ratio of the GI50 of temozolomide in the presence of Rucaparib to the GI50 of temozolomide alone. (参考用のみ)
動物試験：^[4]	- 合併動物モデル： CD-1 nude mice bearing established D283Med xenografts 投薬量： 1 mg/kg 投与方法： One or four daily by i.p. (参考用のみ)

参考

- 合併

溶解度 (25°C)

体外	DMSO	84 mg/mL (199.35 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	左から（NMPから）右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ): 2% DMSO+30% PEG 300+2% Tween 80+ddH2O 混合させたのち直ちに使用することを推奨します。	10mg/mL

* 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 Rucaparib (AG-014699) phosphate SDFをダウンロードする

分子量	421.36
化学式	C₁₉H₁₈FN₃O.H₃PO₄
CAS No.	459868-92-9
Storage	3 years-20°C powder 2 years-80°C in solvent
別名	PF-01367338
Smiles	CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=C3C(=CC(=C4)F)N2.OP(=O)(O)O

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SDS/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SDS/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 2021-09-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04539327	Recruiting	Drug: Rucaparib	Epithelial Ovarian Cancer\|Fallopian Tube Cancer\|Primary Peritoneal Cancer	Grupo Español de Investigación en Cáncer de Ovario\|Clovis Oncology Inc.	July 29 2020	--
NCT04179396	Active not recruiting	Drug: Rucaparib\|Drug: Enzalutamide\|Drug: Abiraterone	Metastatic Castration Resistant Prostate Cancer	Clovis Oncology Inc.	December 5 2019	Phase 1
NCT04171700	Recruiting	Drug: Rucaparib	Solid Tumor	Clovis Oncology Inc.	November 21 2019	Phase 2
NCT03824704	Terminated	Drug: Rucaparib\|Drug: Nivolumab	Epithelial Ovarian Cancer\|Fallopian Tube Cancer\|Primary Peritoneal Carcinoma\|High Grade Serous Carcinoma\|Endometrioid Adenocarcinoma	Clovis Oncology Inc.\|Bristol-Myers Squibb\|Foundation Medicine	August 23 2019	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:

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Most Potent PARP Inhibitor

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PARP Inhibitor in Clinical Trial

Iniparib (BSI-201) : Phase III for solid tumors.

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研究分野別

製品類型

Rucaparib (AG-014699) phosphate

文献中Selleckの製品使用例(103)

製品安全説明書

PARP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 Rucaparib (AG-014699) phosphate 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 2021-09-06)

技術サポート

PARPシグナル伝達経路

PARP Inhibitors with Unique Features

相関PARP製品