Rucaparib (AG-014699) phosphate

For research use only. Not for use in humans.

目录号：S1098 别名： PF-01367338 中文名称：瑞卡帕布磷酸盐

Rucaparib (AG-014699) phosphate Chemical Structure

CAS No. 459868-92-9

Rucaparib (AG-014699,PF-01367338)是一种PARP抑制剂，无细胞试验中作用于PARP1的K_i为1.4 nM，对其余8个PARP位点也有结合亲和力。Phase 3。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 1091.92	现货
5mg	RMB 980.68	现货
10mg	RMB 1730.04	现货
50mg	RMB 5483.69	现货
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客户使用Selleck生产的Rucaparib (AG-014699) phosphate发表文献94篇：

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Proc Natl Acad Sci U S A, 2020, 201919445

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EMBO Mol Med, 2020, 12(12):e12391

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Nat Microbiol, 2019, 4(11):1872-1884

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Nat Commun, 2018, 9(1):2678

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J Immunol, 2018,

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Nat Cell Biol, 2017, 19(11):1371-1378

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Mol Cell, 2017, 66(4):503-516

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产品安全说明书

PARP抑制剂选择性比较

生物活性

产品描述

Rucaparib (AG-014699,PF-01367338)是一种PARP抑制剂，无细胞试验中作用于PARP1的K_i为1.4 nM，对其余8个PARP位点也有结合亲和力。Phase 3。

特性

AG-014699是第一个用于人类癌症疗法的PARP 抑制剂。

靶点

PARP ^[1]
(Cell-free assay)

1.4 nM(Ki)

体外研究

AG-014699有效抑制纯化的全长人类PARP-1，作用于LoVo和SW620细胞显示出强PARP抑制效果。AG-014699是AG14447的磷酸盐形式，且是第一个和temozolomide联用用于临床实验的PARP抑制剂。^[1] AG-014699的辐射增敏性是由于下游NF-κB激活的抑制，及SSB修复抑制。AG-014699可以作用于DNA损伤激活的NF-κB，且克服传统NF-κB抑制剂的毒性，不会损害其他重要的炎症反应。^[2]1μM AG-014699作用于D283Med细胞时抑制PARP-1活性达97.1%。^[3]在NB-1691, SH-SY-5Y, 和SKNBE(2c)细胞中AG-014699明显增强Topotecan和Temozolomide的细胞毒性。^[4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
BT-474	NGTadI1HfW6ldHnvckBCe3OjeR?=	M4PUelAvOS9zL{WwNE8yODByIH7N			MnT6bY5pcWKrdIOgVGFTWCCjY4Tpeol1gSCjdDDzeIFzfGmwZzDjc45k\XKwdILheIlwdiCxZjC1NFAhdk1?	MmrSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMki0OVUoRjJ3MUK4OFU2RC:jPh?=
BT474	MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2fpT\|UxOCCwTR?=	M3Kw[lEx6oDVMUZCpIQ>		NXzpTY9XemWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>?	Mlr4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMki0OVUoRjJ3MUK4OFU2RC:jPh?=
SKBR3	MnK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXHiSnN4PTByIH7N	MXKxNQKBmzF3wrDk		NVTWWmo3emWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>?	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF{OES1OUc,OjVzMki0OVU9N2F-
AU565	M2jJOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mn\4OVAxKG6P	M{jyblEx6oDVMUZCpIQ>		NGfyfXhz\WS3Y3XzJINmdGxiZ4Lve5RpKGmwIITo[UBnd3W{IHzpcoV{KGGwZDDzbYdvcW[rY3HueIx6	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF{OES1OUc,OjVzMki0OVU9N2F-
EFM192A	NVG0d5BUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3LoOFUxOCCwTR?=	Mm\vNVDjiJNzNdMg[C=>		Ml[1doVlfWOnczDj[YxtKGe{b4f0bEBqdiC2aHWg[o92eiCuaX7ld{BidmRic3nncolncWOjboTsfS=>	NHTpNXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGyPFQ2PSd-MkWxNlg1PTV:L3G+
MDA-MB-231	MVrGeY5kfGmxbjDBd5NigQ>?	MVexNE8zOC92MDFOwG0>	MYGyOEBp		MlrUbY5kemWjc3XzJJAuSUuWIHzleoVteyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	MmntQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MkCxOVIoRjJ2NEKwNVUzRC:jPh?=
MDA-MB-231	M2K5SGNmdGxiVnnhZoltcXS7IFHzd4F6	NYXPPHJOOC5zLUSwJO69VQ>?	MXeyOEBp		MoLqTWM2OOLCiU5ihKkyPy55N9Mg{txO	MmDRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MkCxOVIoRjJ2NEKwNVUzRC:jPh?=
MDA-MB-231	MWXBdI9xfG:\|aYOgRZN{[Xl?	NYnpflVNOTBxMkCvOFAh\|ryP	NFvzO5AzPCCq		M{flbYlv\HWlZYOgZZBweHSxc3nzJIRwe2ViZHXw[Y5l\W62bIm=	NFvHOYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESyNFE2Oid-MkS0NlAyPTJ:L3G+
MDA-MB-231	M3vWNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Ml7PNVAwOjBxNECg{txO	NGrTbpkzPCCq		NVvnfJh1[myxY3vzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25iaX6gS\|IwVSCyaHHz[S=>	NF7jc5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESyNFE2Oid-MkS0NlAyPTJ:L3G+
H460	NV30UHhZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NV3VT3NnPDByIH7N	NXfVPGpCOjUEoHi=		MVPpcoNz\WG\|ZYOgZ4VtdHWuYYKgdoFlcW:\|ZX7zbZRqfmm2eR?=	MmLEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUG2NVEoRjJ2NEGxOlEyRC:jPh?=
A549	NVnadVZGT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVG0NFAhdk1?	MlTjNlTDqGh?		M3L5OYlv[3KnYYPld{Bk\WyudXzhdkBz[WSrb4PlcpNqfGm4aYT5	NY\W[JFGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NVE3OTFpPkK0OFEyPjFzPD;hQi=>
DT40	MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MnfOTWM2OD1{MTDuUS=>	NVG4OHNWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVY5OTNpPkK0N\|U3QDF\|PD;hQi=>
DU145	NI\GOJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NGHnVm1KSzVyPUG4JI5O	NGnEb409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1OlgyOyd-MkSzOVY5OTN:L3G+
COLO704	NV;YSlZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NEDXVW1KSzVyPUKuOVIhyrFiMD62O{DPxE1?	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OVMANAb	NVG2OGRiT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NIW3TmdKSzVyPUKuOVghyrFiMD6zPEDPxE1?	NEHhNWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
OV177	M3vHfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M{W3TmlEPTB;Mj63PEDDuSByLkexJO69VQ>?	MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OAW28	MkTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NX3yTlZHUUN3ME2zMlYyKMLzIECuNlgh\|ryP	NXfUNVY{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
OVSAHO	NEjjTlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MorUTWM2OD1\|Lk[0JOKyKDBwM{Og{txO	NX7QbFF{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
OVKATE	M3T5bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NVTmbmd1UUN3ME2zMlY1KMLzIEGuO\|kh\|ryP	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
OVCAR3	MlXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M4O4cGlEPTB;Mz63OEDDuSByLkSwJO69VQ>?	NWXEPWtlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
PEO14	NEf1[5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MoDaTWM2OD1\|Lki0JOKyKDBwN{[g{txO	M4DvcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
A2780	MlewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MoP0TWM2OD1\|Lkm0JOKyKDBwMkWg{txO	NXywcVl[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
OVTOKO	MlzpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NUXLcnRJUUN3ME20MlE1KMLzIEGuOVMh\|ryP	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
KURAMOCHIb	M2DKWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MXzJR\|UxRTRwM{SgxtEhOC5{OTFOwG0>	NWnrNYZYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
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OVCA429	MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M33rVmlEPTB;OD6yPUDDuSBzLk[0JO69VQ>?	NHfaZnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
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OVCAR5	M2e4OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NFTPZnlKSzVyPUmuOVAhyrFiMj61PUDPxE1?	NF:4SpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
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CAOV3	NH7weJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MYTJR\|UxRTFyLkO3JOKyKDBwOEeg{txO	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
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EFO27	MmfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M1fUOmlEPTB-MUWg{txO	NWLpdlA1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
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MCASb	M4qwcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NWnEVoNEUUN3ME6xOUDPxE1?	NUSxOXY{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
OAW42	NYHYNZRoT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NYXyWWhjUUN3ME6xOUDPxE1?	NYnP[HcxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
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OV90	NE\oe\|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MUDJR\|UxRjF3IN88US=>	NXjRSHl5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3Nlk1ODJpPkKzO\|I6PDB{PD;hQi=>
OVCA420b	M3TINWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				Mlz5TWM2OD5zNTFOwG0>	Ml71QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5Mkm0NFIoRjJ\|N{K5OFAzRC:jPh?=
OVCA432	NWPEbJI1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NULqUnY3UUN3ME6xOUDPxE1?	M164XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
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SKOV3	NHfKXHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				Ml;HTWM2OD5zNTFOwG0>	M{PUdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
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C4-2	NIrFTJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWLDfXN[OC1\|IN88US=>	NVHSS\|hqOTRiZB?=	MVLEUXNQ	MoOx[IVkemWjc3XzJINwdG:weTDueY1j\XJiZH;z[UBl\XCnbnTlcpRtgQ>?	NUW3PJRRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OlUzPDRpPkKzOVY2OjR2PD;hQi=>
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LNCaP	MoiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVKwMVMh\|ryP	NULmbnVZOTRiZB?=	MlLaSG1UVw>?	NGDIRZNl\WO{ZXHz[ZMh[2:ub375JI52dWKncjDkc5NmKGSncHXu[IVvfGy7	M2\SO\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|NU[1NlQ1Lz5{M{W2OVI1PDxxYU6=
MDA-MB-468	NWXoWlRLS2WubDDWbYFjcWyrdImgRZN{[Xl?				NFi2W4RKSzVyPUmuO{DPxE1?	M{fpPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Nke4NVYyLz5{Mk[3PFE3OTxxYU6=
MDA-MB-231	M2T2d2NmdGxiVnnhZoltcXS7IFHzd4F6				MWTJR\|UxRTF\|IN88US=>	MlPrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4N{ixOlEoRjJ{Nke4NVYyRC:jPh?=
Cal-51	NILxWpdE\WyuIG\pZYJqdGm2eTDBd5NigQ>?				NGDKXGlKSzVyPUiuOkDPxE1?	M2DxZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Nke4NVYyLz5{Mk[3PFE3OTxxYU6=
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Rosetta2 (DE3)	M4PKZmZ2dmO2aX;uJIF{e2G7				NHixeYhKdmirYnn0bY9vKG:oIHj1cYFvKE5vdHXycYlv[WxiNojobZMufGGpZ3XkJGFTXER4IDi4O\|MhfG9iMUG2NUkh\XiycnXzd4VlKGmwIFXzZ4hmemmlaHnhJINwdGliUn;z[ZR1[TJiKFTFN{kh[2WubIOgeZNqdmdiTlHEL{BieyC\|dXLzeJJifGViYomg[ox2d3Knc3PlcoNmKGG\|c3H5MEBKSzVyIE2gNE4xOTRizszNMi=>	NXjXRmFJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA4PzBpPkK0PVAxPzdyPD;hQi=>
Rosetta2 (DE3)	MWXGeY5kfGmxbjDhd5NigQ>?				MX\Jcohq[mm2aX;uJI9nKGi3bXHuJFZ5cGm\|LYTh[4dm\CCDUmTEOUApOTB\|MDD0c{AyOzF5KTDlfJBz\XO\|ZXSgbY4hTXOlaHXybYNpcWFiY3;sbUBTd3OndIThNkApTEV\|KTDj[YxteyC3c3nu[{BPSURtIHHzJJN2[nO2cnH0[UBjgSCobIXvdoV{[2WwY3WgZZN{[XluIFnDOVAhRSByLkCyOUDPxE1w	M2jKdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwO\|cxLz5{NEmwNFc4ODxxYU6=
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Capan1	M33NVGN6fG:2b4jpZ4l1gSCjc4PhfS=>				MULDfZRwfG:6aXPpeJkh[WejaX7zeEBDWkODMj3k[YZq[2mnboSgbJVu[W5iQ3HwZY4yKGOnbHzzMEBGSzVyIE2gNE43ODlizszNMi=>	NV3wUIZjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
MDA-MB-436	NFjpTGlCdnSrY3HuZ4VzKGG\|c3H5		NYrE[2NoQTZiaILz		MXfBcpRq[2GwY3XyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmLDRVEu\GWoaXPp[Y51KE2GQT3NRk01OzZiY3XscJMh[W[2ZYKgPVYhcHK\|IHL5JG1VXCCjc4PhfUwhS0N3MDC9JFMh\|ryPLh?=	NWr5TpRtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zOFI5PjhpPkK2N\|QzQDZ6PD;hQi=>
OVCAR3	NV:1S4VFSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M3HRUVI1KGi{cx?=		M{nZfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI{KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCzMlMyKM7:TT6=	NXi1V5lLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OVYyODZpPkK5OFU3OTB4PD;hQi=>
MRC5	Mny3R5l1d3SxeHnjbZR6KGG\|c3H5				NFXucmxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOWkN3IHPlcIx{NCCHQ{WwJF0hQC53MzFOwG0v	NVXzcnhIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
MCF7	M1z4eGFvfGmlYX7j[ZIh[XO\|YYm=		MV65OkBpenN?		MVPBcpRq[2GwY3XyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB7NjDodpMh[nliTWTUJIF{e2G7LDDDR\|UxKD1iMUmuOFch\|ryPLh?=	MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN2Mki2PEc,OjZ\|NEK4Olg9N2F-
A673	M4XFUZFJXFNiYYPzZZk>				MlXBdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN?	NVjZUIo3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673	M3vuTpFJXFNiYYPzZZk>				NXftV5d4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl?	NV;zeIlJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41	NGPhbVhyUFSVIHHzd4F6				MlewdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog1OSClZXzsdy=>	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-MC	NGLsRYpyUFSVIHHzd4F6				MnvTdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2PQzDj[Yxtew>?	NIi0SXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
TC32	NGT6[VByUFSVIHHzd4F6				NV;HfpBUeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXEN\|MjDj[Yxtew>?	NHnhNWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
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. 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.	27960087 24085845
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	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. 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. 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. 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.	30589644 27515310 23565244

体内研究

AG-014699无毒，明显增强D384Med移植瘤DNA修复功能蛋白中temozolomide诱导的TGD。药物动力学研究显示在脑组织中也检测到AG-014699，说明AG-014699用于治疗颅内恶性肿瘤具有潜在可能。^[3]活体模型(NB1691和SHSY5Y移植瘤)研究显示AG-014699增强temozolomide的抗癌活性，产生彻底且持久的肿瘤衰退现象。^[4]

激酶实验：^[3]	- 合并激酶实验: 不同浓度(0到1μ)AG-014699作用于5×10³D283Med 细胞，与只用DMSO处理5×10³D283Med细胞相比，来测定PARP活性抑制率。参考GCLP验证试验的PAR标准曲线，在和NAD⁺及寡核苷酸(底物和激活剂)温育的6分钟期间，使用10H PAR抗体，通过PAR形成量的免疫检测，在细胞样本中测量最大程度刺激的PARP活性。
细胞实验： ^[3]	- 合并 Cell lines: D425Med, D283Med和D384Med细胞 Concentrations: 0.4 μM Incubation Time: 3或5天 Method: 髓母细胞瘤细胞系包含D425Med, D283Med，和D384Med细胞，分别按1×10³, 3×10³，和3×10³密度接种在96孔板上。接种24小时(D384Med细胞)或48小时(D283Med和D425Med细胞)后，细胞用不同浓度temozolomide处理。培养3天(D425Med和D384Med细胞)或5天(D283Med细胞)后，通过XTT细胞增殖检测试剂盒检测细胞活力。用DMSO处理的对照组和0.4μ AG-014699处理的实验组的百分比表示细胞生长。计算temozolomide单独使用或者和AG-014699联用时的GI50值。Temozolomide单独使用时的GI50值和与AG-014699联用时的GI50值之比就是趋化因子50（PF50）值。 (Only for Reference)
动物实验：^[3]	- 合并 Animal Models: 携带D283Med移植瘤的CD-1裸鼠 Dosages: 1 mg/kg Administration: 腹腔注射，每天1次或4次 (Only for Reference)

参考文献

- 合并

溶解度 (25°C)

体外	DMSO	84 mg/mL (199.35 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 2% DMSO+30% PEG 300+2% Tween 80+ddH2O	10mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Rucaparib (AG-014699) phosphate SDF

分子量	421.36
化学式	C₁₉H₁₈FN₃O.H₃PO₄
CAS号	459868-92-9
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	PF-01367338

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

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):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-05-17)

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
NCT03954366	Active not recruiting	Drug: Rucaparib\|Drug: Rosuvastatin\|Drug: Oral Contraceptives	Neoplasms	Clovis Oncology Inc.	May 8 2019	Phase 1
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	May 15 2019	Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

选择性强的PARP抑制剂

AG-14361 : PARP1-selective, K_i<5 nM.
选择性强的PARP抑制剂

UPF 1069 : PARP2-selective, IC50=0.3 μM.
活性最高的PARP抑制剂

MK-4827 (Niraparib) : PARP1, IC50=3.8 nM; PARP2, IC50=2.1 nM.
用于临床的PARP抑制剂

Iniparib (BSI-201) : Phase III for solid tumors.
最新的PARP抑制剂

PJ34 HCl ^New : PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

研究领域

产品类型

定制您的化合物库

Rucaparib (AG-014699) phosphate

客户使用Selleck生产的Rucaparib (AG-014699) phosphate发表文献94篇：

产品安全说明书

PARP抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Rucaparib (AG-014699) phosphate SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-05-17)

技术支持

PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

相关PARP产品