Name: Rucaparib (AG-014699) phosphate
Brand: Selleck Chemicals
SKU: S1098
Rating: 5 (107 reviews)

Rucaparib (AG-014699) phosphate Chemical Structure

CAS No. 459868-92-9

Selleck's Rucaparib (AG-014699) phosphate has been cited by 107 publications

Purity & Quality Control

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PARP Signaling Pathway Map

Biological Activity

Description

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.

Features

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

Targets

PARP ^[1]
(Cell-free assay)

1.4 nM(Ki)

In vitro

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]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

BT-474	MX\GeY5kfGmxbjDBd5NigQ>?	MYCwMlEwOS93MECvNVAxOCCwTR?=			M4q4Z4lvcGmkaYTzJHBCWlBiYXP0bZZqfHliYYSgd5RienSrbnegZ49v[2W{boTyZZRqd25ib3[gOVAxKG6P	NGTncmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyPFQ2PSd-MkWxNlg1PTV:L3G+
BT474	M3XvNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4TiOVUxOCCwTR?=	NVLOWIJnOTEkgKOxOeKh\A>?		M2LKdJJm\HWlZYOgZ4VtdCCpcn;3eIghcW5idHjlJIZwfXJibHnu[ZMh[W6mIIPp[45q\mmlYX70cJk>	M17uVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUK4OFU2Lz5{NUGyPFQ2PTxxYU6=
SKBR3	M{LYcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWjyOYFLPTByIH7N	M1v6TlEx6oDVMUZCpIQ>		NY\QeJZnemWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>?	MljmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMki0OVUoRjJ3MUK4OFU2RC:jPh?=
AU565	NU\FXXdrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFPFO3M2ODBibl2=	NWntNpdtOTEkgKOxOeKh\A>?		MVXy[YR2[2W\|IHPlcIwh\3Kxd4ToJIlvKHSqZTDmc5VzKGyrbnXzJIFv\CC\|aXfubYZq[2GwdHz5	NX:0cVJvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNlg1PTVpPkK1NVI5PDV3PD;hQi=>
EFM192A	Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlfJOVAxKG6P	M1G2U\|Ex6oDVMUZCpIQ>		MlfMdoVlfWOnczDj[YxtKGe{b4f0bEBqdiC2aHWg[o92eiCuaX7ld{BidmRic3nncolncWOjboTsfS=>	NV;s[HNqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNlg1PTVpPkK1NVI5PDV3PD;hQi=>
MDA-MB-231	NUjSXG9yTnWwY4Tpc44hSXO\|YYm=	M2noXlExNzJyL{SwJO69VQ>?	NUTMZWlJOjRiaB?=		Moe5bY5kemWjc3XzJJAuSUuWIHzleoVteyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	NGWxdYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESyNFE2Oid-MkS0NlAyPTJ:L3G+
MDA-MB-231	NUHnN5BjS2WubDDWbYFjcWyrdImgRZN{[Xl?	NGTTOFUxNjFvNECg{txO	NWDRdI9rOjRiaB?=		MWPJR\|Ux6oDLPfMAjVE4Njd5wrFOwG0>	MmqzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MkCxOVIoRjJ2NEKwNVUzRC:jPh?=
MDA-MB-231	M{izT2Fxd3C2b4Ppd{BCe3OjeR?=	NX7FUpRMOTBxMkCvOFAh\|ryP	M2XPdlI1KGh?		MlvRbY5lfWOnczDhdI9xfG:\|aYOg[I9{\SCmZYDlcoRmdnSueR?=	NGr1cYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESyNFE2Oid-MkS0NlAyPTJ:L3G+
MDA-MB-231	M{j1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MXyxNE8zOC92MDFOwG0>	M{\GRVI1KGh?		MYnicI9kc3NiY3XscEBkgWOuZTDwdo9oemW\|c3nvckBqdiCJMj;NJJBp[XOn	NF3uWHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESyNFE2Oid-MkS0NlAyPTJ:L3G+
H460	MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1HM[lQxOCCwTR?=	MXiyOOKhcA>?		NU[0bXR4cW6lcnXhd4V{KGOnbHz1cIFzKHKjZHnvd4Vve2m2aY\peJk>	M12wWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEGxOlEyLz5{NESxNVYyOTxxYU6=
A549	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGKzPWQ1ODBibl2=	MkX0NlTDqGh?		Ml\RbY5kemWjc3XzJINmdGy3bHHyJJJi\Gmxc3Xud4l1cX[rdIm=	MoLiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUG2NVEoRjJ2NEGxOlEyRC:jPh?=
DT40	MmrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M4K1SGlEPTB;MkGgcm0>	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3NkixN{c,OjR\|NU[4NVM9N2F-
DU145	M4j5Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MYfJR\|UxRTF6IH7N	M3SwSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W2PFE{Lz5{NEO1OlgyOzxxYU6=
COLO704	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MX7JR\|UxRTJwNUKgxtEhOC54NzFOwG0>	M{XJSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
OVMANAb	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MYLJR\|UxRTJwNUigxtEhOC5\|ODFOwG0>	NH;VTVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
OV177	M17Zemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NGjicoJKSzVyPUKuO\|ghyrFiMD63NUDPxE1?	M4LQS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
OAW28	NVH2R5JpT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M3HzWGlEPTB;Mz62NUDDuSByLkK4JO69VQ>?	M3nP[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
OVSAHO	M1fWV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MoG1TWM2OD1\|Lk[0JOKyKDBwM{Og{txO	MmPoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
OVKATE	NX2zcFNCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NWnGNGk6UUN3ME2zMlY1KMLzIEGuO\|kh\|ryP	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OVCAR3	NHvkc2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MXzJR\|UxRTNwN{SgxtEhOC52MDFOwG0>	NUjFVYFsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
PEO14	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MVXJR\|UxRTNwOESgxtEhOC55NjFOwG0>	NHjUdGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
A2780	MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NELhXm9KSzVyPUOuPVQhyrFiMD6yOUDPxE1?	MmPPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
OVTOKO	NWfMRYNDT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MlrtTWM2OD12LkG0JOKyKDFwNUOg{txO	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
KURAMOCHIb	NWO3RZJnT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				Ml;XTWM2OD12LkO0JOKyKDBwMkmg{txO	NHnqNYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
TOV21G	NH;0W4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NXrXWVJxUUN3ME21MlA4KMLzIEGuN\|Ah\|ryP	NE\SZoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
OVISE	NITNV2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M3ThWGlEPTB;NT62PEDDuSByLkKzJO69VQ>?	NEfKNZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
KK	NWrWT3o4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M33tSGlEPTB;Nj6xOUDDuSBzLkSyJO69VQ>?	NXL3XmpjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
RMUGS	NX7FPXlrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NYTiZnZNUUN3ME23MlA{KMLzIEGuPFMh\|ryP	M3P0NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
PEO6	NXzQ[oY{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NWLmemtoUUN3ME23MlA3KMLzIECuO\|Qh\|ryP	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OVCA429	NEXJeoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NHu0SmpKSzVyPUiuNlkhyrFiMT62OEDPxE1?	M3;3WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
OV167	NHTOeGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MXrJR\|UxRThwM{OgxtEhOS5zODFOwG0>	MmG1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
RMG1	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MlrPTWM2OD17LkOyJOKyKDJwM{[g{txO	MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OVCAR5	MmPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MVjJR\|UxRTlwNUCgxtEhOi53OTFOwG0>	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
EFO21	NUjrRpVET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MXvJR\|UxRTlwOUKgxtEhOS56NzFOwG0>	Ml\MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
ES2	NWO5[3c5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MYLJR\|UxRTFyLkGyJOKyKDFwMkOg{txO	NUPIbod5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
Tyk-nu	MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M4DIN2lEPTB;MUCuNlAhyrFiMT6xNkDPxE1?	MofNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
CAOV3	NGHmUlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MYHJR\|UxRTFyLkO3JOKyKDBwOEeg{txO	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OV207	NYS2SW5ZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				Mo\WTWM2OD1zMj6yO{DDuSByLkOyJO69VQ>?	M164bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
HEY	MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MkjsTWM2OD1zMz6wNUDDuSByLke1JO69VQ>?	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
DOV13	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NXzCPGluUUN3ME6xOUDPxE1?	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
EFO27	M4TvdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MV\JR\|UxRjF3IN88US=>	NFrmWno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
HEY C2	NYTGeotHT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NWHJVIk2UUN3ME6xOUDPxE1?	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
KOC-7cc	M2nuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NF3ubJlKSzVyPkG1JO69VQ>?	NILrXo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
MCASb	NH74RlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NFnZbo1KSzVyPkG1JO69VQ>?	NYTsWnZyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
OAW42	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NHy1V4pKSzVyPkG1JO69VQ>?	NHjRbXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
OV2008	Ml7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MnXwTWM2OD5zNTFOwG0>	Mlm4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
OV90	M17T[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NV;mdWg2UUN3ME6xOUDPxE1?	NH;4NoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
OVCA420b	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MonXTWM2OD5zNTFOwG0>	M2PyW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
OVCA432	NInGTGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NIHRXXhKSzVyPkG1JO69VQ>?	M{\xeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
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MDA-MB-231	M17Ne2NmdGxiVnnhZoltcXS7IFHzd4F6				NUflemdZUUN3ME2xN{DPxE1?	NX;0cVZURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2O\|gyPjFpPkKyOlc5OTZzPD;hQi=>
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Rosetta2 (DE3)	M3e5ZWZ2dmO2aX;uJIF{e2G7				NX;aRXcyUW6qaXLpeIlwdiCxZjDoeY1idiCQLYTldo1qdmGuIE\4bIl{NXSjZ3fl[EBCWlSGNjCoPFc{KHSxIEGxOlEqKGW6cILld5Nm\CCrbjDFd4Np\XKrY3jpZUBkd2yrIGLvd4V1fGF{IDjESVMqKGOnbHzzJJV{cW6pIF7BSEsh[XNic4Xid5Rz[XSnIHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3MDC9JFAvODF2IN88UU4>	M4\pSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwO\|cxLz5{NEmwNFc4ODxxYU6=
Rosetta2 (DE3)	MYPGeY5kfGmxbjDhd5NigQ>?				M3rJOWlvcGmkaYTpc44hd2ZiaIXtZY4hPniqaYOteIFo\2WmIFHSWGQ2KChzMEOwJJRwKDF\|MUepJIV5eHKnc4Pl[EBqdiCHc3Po[ZJq[2irYTDjc4xqKFKxc3X0eIEzKCiGRUOpJINmdGy\|IIXzbY5oKE6DRDugZZMhe3Wkc4TyZZRmKGK7IH\seY9z\XOlZX7j[UBie3OjeTygTWM2OCB;IECuNFI2KM7:TT6=	MlHUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC3O\|AoRjJ2OUCwO\|cxRC:jPh?=
LoVo	NX3QO3F5S3m2b4TvfIlkcXS7IHHzd4F6	NV6xW5ZJOC52IIXN	NIS1cZM2KGSjeYO=		NHzIfHRRd3SnboTpZZRqd25ib3[geIVud3qxbH;tbYRmNWmwZIXj[YQh[3m2b4TvfIlkcXS7IHnuJIh2dWGwIFzvWo8h[2WubIOgZZN{\XO\|ZXSgZZMhfGWvb4rvcI9ucWSnIFfJOVAh[XRiMD60JJVOKGGodHXyJFUh\GG7czDifUBE\WyudHn0[ZIuT2yxIHHzd4F6NCCJSUWwJF0hOC5zNESg{txONg>?	M3XXOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO\|E4Lz5{Nk[1NlcyPzxxYU6=
Capan1	NIj0WFlEgXSxdH;4bYNqfHliYYPzZZk>				M1r3UGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEKUQ1GyMYRm\mmlaXXueEBpfW2jbjDDZZBidjFiY3XscJMtKEWFNUCgQUAxNjZyOTFOwG0v	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3MkexO{c,OjZ4NUK3NVc9N2F-
MDA-MB-436	MnLJRY51cWOjbnPldkBie3OjeR?=		MlrHPVYhcHK\|		MV7BcpRq[2GwY3XyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmLDRVEu\GWoaXPp[Y51KE2GQT3NRk01OzZiY3XscJMh[W[2ZYKgPVYhcHK\|IHL5JG1VXCCjc4PhfUwhS0N3MDC9JFMh\|ryPLh?=	M4[0b\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{SyPFY5Lz5{NkO0Nlg3QDxxYU6=
OVCAR3	NGm3NItCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MnPONlQhcHK\|		M3vsOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI{KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCzMlMyKM7:TT6=	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR3NkGwOkc,Ojl2NU[xNFY9N2F-
MRC5	Mlr6R5l1d3SxeHnjbZR6KGG\|c3H5				MkGwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUXJEPSClZXzsd{whTUN3MDC9JFgvPTNizszNMi=>	Mlr6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO\|E4RC:jPh?=
MCF7	M1ewVWFvfGmlYX7j[ZIh[XO\|YYm=		M3yzV\|k3KGi{cx?=		Ml\5RY51cWOjbnPldkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IF3UWEBie3OjeTygR2M2OCB;IEG5MlQ4KM7:TT6=	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN2Mki2PEc,OjZ\|NEK4Olg9N2F-
A673	MlTVdWhVWyCjc4PhfS=>				NUG0WW1IeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFG2O\|Mh[2WubIO=	NIjSU3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
A673	Ml;1dWhVWyCjc4PhfS=>				MVPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDBOlc{KGOnbHzzLS=>	M4ezd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41	M1;6W5FJXFNiYYPzZZk>				MXvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFQyKGOnbHzz	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-MC	MnHtdWhVWyCjc4PhfS=>				NWXYPWE{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	NFy4SWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
TC32	MYDxTHRUKGG\|c3H5				M2[2bpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM>	MnPOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	BRCA1 ; PAR	24085845 27960087
Growth inhibition assay	Cell viability	31119062
Immunofluorescence	53BP1 ; γH2AX ; PAR ; α-tubulin	23565244 27515310 30589644

In vivo

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]

Protocol (from reference)

Kinase Assay:^[1]	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.
Cell Research:^[4]	Cell lines: D425Med, D283Med and D384Med cells Concentrations: 0.4 μM Incubation Time: 3 or 5 days Method: 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. (Only for Reference)
Animal Research:^[4]	Animal Models: CD-1 nude mice bearing established D283Med xenografts Dosages: 1 mg/kg Administration: One or four daily by i.p. (Only for Reference)

References

+ Expand

Solubility (25°C)

In vitro	DMSO	84 mg/mL (199.35 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+2% Tween 80+ddH2O For best results, use promptly after mixing. Click to purchase: PEG300 Tween 80	10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight	421.36
Formula	C₁₉H₁₈FN₃O.H₃PO₄
CAS No.	459868-92-9
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=C3C(=CC(=C4)F)N2.OP(=O)(O)O

Download Rucaparib (AG-014699) phosphate SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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