Rucaparib (AG-014699) phosphate

For research use only. Not for use in humans.

製品コードS1098 別名:PF-01367338

Rucaparib (AG-014699) phosphate化学構造

CAS No. 459868-92-9

Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki 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) 在庫  
10mM (1mL in DMSO) JPY 24200 あり
JPY 21900 あり
JPY 36800 あり
JPY 113200 あり
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バルク問合せ

文献中Selleckの製品使用例(86)

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 Ki 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 M3zsbmZ2dmO2aX;uJGF{e2G7 M2rueFAvOS9zL{WwNE8yODByIH7N M3ixdolvcGmkaYTzJHBCWlBiYXP0bZZqfHliYYSgd5RienSrbnegZ49v[2W{boTyZZRqd25ib3[gOVAxKG6P MkixQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMki0OVUoRjJ3MUK4OFU2RC:jPh?=
BT474 M3vRUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTkT4pZPTByIH7N MY[xNQKBmzF3wrDk MkX0doVlfWOnczDj[YxtKGe{b4f0bEBqdiC2aHWg[o92eiCuaX7ld{BidmRic3nncolncWOjboTsfS=> NX3r[|VVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNlg1PTVpPkK1NVI5PDV3PD;hQi=>
SKBR3 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVq0dnc6PTByIH7N NX;DSmlrOTEkgKOxOeKh\A>? MofmdoVlfWOnczDj[YxtKGe{b4f0bEBqdiC2aHWg[o92eiCuaX7ld{BidmRic3nncolncWOjboTsfS=> MnX5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMki0OVUoRjJ3MUK4OFU2RC:jPh?=
AU565 MmXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTae|JpPTByIH7N MUOxNQKBmzF3wrDk M3jBUpJm\HWlZYOgZ4VtdCCpcn;3eIghcW5idHjlJIZwfXJibHnu[ZMh[W6mIIPp[45q\mmlYX70cJk> M{\USVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUK4OFU2Lz5{NUGyPFQ2PTxxYU6=
EFM192A MkLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLUOVAxKG6P NF;DV2MyOOLCk{G1xsBl NFHG[I5z\WS3Y3XzJINmdGxiZ4Lve5RpKGmwIITo[UBnd3W{IHzpcoV{KGGwZDDzbYdvcW[rY3HueIx6 NXHCNGhWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNlg1PTVpPkK1NVI5PDV3PD;hQi=>
MDA-MB-231 MWPGeY5kfGmxbjDBd5NigQ>? MlXYNVAwOjBxNECg{txO MomwNlQhcA>? MorvbY5kemWjc3XzJJAuSUuWIHzleoVteyCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NIf2dWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESyNFE2Oid-MkS0NlAyPTJ:L3G+
MDA-MB-231 M3v3VGNmdGxiVnnhZoltcXS7IFHzd4F6 NGLnTI8xNjFvNECg{txO MnvHNlQhcA>? Mof5TWM2OOLCiU5ihKkyPy55N9Mg{txO MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR{MEG1Nkc,OjR2MkCxOVI9N2F-
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PEA2 NEn6[YNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTmVXBtUUN3ME6xOUDPxE1? NIDIUlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{eyPVQxOid-MkO3Nlk1ODJ:L3G+
SKOV3 NX7PTYx2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLVTWM2OD5zNTFOwG0> M4fqVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{K5OFAzLz5{M{eyPVQxOjxxYU6=
TOV112D NH\xU4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXicWoxNTNizszN MXLJR|UxRjF3IN88US=> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd{OUSwNkc,OjN5Mkm0NFI9N2F-
C4-2 MmT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYSwMVMh|ryP NWHpZZB4OTRiZB?= MVfEUXNQ MXjk[YNz\WG|ZYOgZ49td267IH71cYJmeiCmb4PlJIRmeGWwZHXueIx6 NGPGUI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W2OVI1PCd-MkO1OlUzPDR:L3G+
PC3 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfrXWF{OC1|IN88US=> MoS2NVQh\A>? NHfvR3hFVVOR Mknj[IVkemWjc3XzJINwdG:weTDueY1j\XJiZH;z[UBl\XCnbnTlcpRtgQ>? Ml;PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NkWyOFQoRjJ|NU[1NlQ1RC:jPh?=
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VCaP  NWnCe2hST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUSwMVMh|ryP M3XjdFE1KGR? Mn7xSG1UVw>? MYfk[YNz\WG|ZYOgZ49td267IH71cYJmeiCmb4PlJIRmeGWwZHXueIx6 M4LSU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NU[1NlQ1Lz5{M{W2OVI1PDxxYU6=
LNCaP  Ml24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HtWFAuOyEQvF2= NV73TZVMOTRiZB?= NVXnSmFsTE2VTx?= NH3ucVll\WO{ZXHz[ZMh[2:ub375JI52dWKncjDkc5NmKGSncHXu[IVvfGy7 NIH6OIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W2OVI1PCd-MkO1OlUzPDR:L3G+
MDA-MB-468 MoSwR4VtdCCYaXHibYxqfHliQYPzZZk> NIDmXVlKSzVyPUmuO{DPxE1? NXHIeY9[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2O|gyPjFpPkKyOlc5OTZzPD;hQi=>
MDA-MB-231 NHPwOoxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGi1RYdKSzVyPUGzJO69VQ>? MojSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4N{ixOlEoRjJ{Nke4NVYyRC:jPh?=
Cal-51 MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHLTSFBKSzVyPUiuOkDPxE1? MnjJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4N{ixOlEoRjJ{Nke4NVYyRC:jPh?=
LoVo NE\3[m9HfW6ldHnvckBie3OjeR?= NIC0SYg{OCCvaX7z NVv5VVhLUW6qaXLpeIlwdiCxZjDQRXJRKGmwIHj1cYFvKEyxVn:gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCyb3z5LGFFWClvcnnic5NmKHCxbInt[ZJqgmG2aX;uJIZweiB|MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBie3OjeTygSWM2OCB;IECuNFA1PjlizszNMi=> NGj6[os9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1NlcyPyd-Mk[2OVI4OTd:L3G+
MX1 NHS3cI9EgXSxdH;4bYNqfHliYYPzZZk> M1HrS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KEKUQ1GxMYRm\mmlaXXueEBpfW2jbjDNXFEh[2WubIOsJGVEPTBiPTCwMlAxPTNizszNMi=> M1TCc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
Rosetta2 (DE3) MnXpSpVv[3Srb36gZZN{[Xl? M2mz[GlvcGmkaYTpc44hd2ZiaIXtZY4hVi22ZYLtbY5idCB4eHjpd{11[WepZXSgRXJVTDZiKEi3N{B1dyBzMU[xLUBmgHC{ZYPz[YQhcW5iRYPjbIVzcWOqaXGgZ49tcSCUb4PleJRiOiBqRFWzLUBk\WyuczD1d4lv\yCQQVSrJIF{KHO3YoP0doF1\SCkeTDmcJVwemW|Y3XuZ4Uh[XO|YYmsJGlEPTBiPTCwMlAyPCEQvF2u MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEe3NEc,OjR7MEC3O|A9N2F-
Rosetta2 (DE3) MVvGeY5kfGmxbjDhd5NigQ>? MmL2TY5pcWKrdHnvckBw\iCqdX3hckA3gGircz30ZYdo\WRiQWLUSFUhMDFyM{CgeI8hOTNzNzmg[ZhxemW|c3XkJIlvKEW|Y3jldolkcGmjIHPvcIkhWm:|ZYT0ZVIhMESHMzmgZ4VtdHNidYPpcochVkGGKzDhd{B{fWK|dILheIUh[nliZnz1c5Jme2OnbnPlJIF{e2G7LDDJR|UxKD1iMD6wNlUh|ryPLh?= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEe3NEc,OjR7MEC3O|A9N2F-
LoVo NXj4V5ZpS3m2b4TvfIlkcXS7IHHzd4F6 NIrJeW8xNjRidV2= M2DsOVUh\GG7cx?= M4PqUXBwfGWwdHnheIlwdiCxZjD0[Y1wgm:ub33p[IUucW6mdXPl[EBkgXSxdH;4bYNqfHliaX6gbJVu[W5iTH;Wc{Bk\WyuczDhd5Nme3OnZDDhd{B1\W2xen;sc41q\GViR1m1NEBifCByLkSgeW0h[W[2ZYKgOUBl[Xm|IHL5JGNmdGy2aYTldk1IdG9iYYPzZZktKEeLNUCgQUAxNjF2NDFOwG0v Mk\GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
Capan1 NHS2NmlEgXSxdH;4bYNqfHliYYPzZZk> NGT0TlBEgXSxdH;4bYNqfHliYXfhbY5{fCCEUlPBNk1l\W[rY3nlcpQhcHWvYX6gR4Fx[W5zIHPlcIx{NCCHQ{WwJF0hOC54MEmg{txONg>? MmT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?=
MDA-MB-436 M3e1WmFvfGmlYX7j[ZIh[XO|YYm= Mni3PVYhcHK| MXTBcpRq[2GwY3XyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmLDRVEu\GWoaXPp[Y51KE2GQT3NRk01OzZiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JG1VXCCjc4PhfUwhS0N3MDC9JFMh|ryPLh?= M{\LeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{SyPFY5Lz5{NkO0Nlg3QDxxYU6=
OVCAR3 NWTQTFdjSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M4fsT|I1KGi{cx?= MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSN{Bk\WyuczDh[pRmeiB{NDDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMz6zNUDPxE1w NX7vd3hIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OVYyODZpPkK5OFU3OTB4PD;hQi=>
MRC5 NFLvXFBEgXSxdH;4bYNqfHliYYPzZZk> M4LyXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1TSzViY3XscJMtKEWFNUCgQUA5NjV|IN88UU4> M4exV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyO|E4Lz5{Nk[1NlcyPzxxYU6=
MCF7 NV7HSI9YSW62aXPhcoNmeiCjc4PhfS=> MlTFPVYhcHK| MV;BcpRq[2GwY3XyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB7NjDodpMh[nliTWTUJIF{e2G7LDDDR|UxKD1iMUmuOFch|ryPLh?= NFzm[mQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO0Nlg3QCd-Mk[zOFI5Pjh:L3G+
A673 NWfxPZd1eUiWUzDhd5NigQ>? MUDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NX:5dIFoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 NHS1NXpyUFSVIHHzd4F6 NWPmZnlkeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh41 NEL5RXVyUFSVIHHzd4F6 M{HWZ5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpPDFiY3XscJM> MljNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC NWH1WnY6eUiWUzDhd5NigQ>? NWfRW2ZreUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
TC32 MorsdWhVWyCjc4PhfS=> MVjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz M{XvTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

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
PAR; 

PubMed: 27960087     


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     


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     


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     


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     


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     


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     


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

Ki 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. Ki 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)

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

分子量 421.36
化学式

C19H18FN3O.H3PO4

CAS No. 459868-92-9
Storage powder
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 g 投与体積(動物毎) ul 動物数
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

便利ツール

モル濃度計算器

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

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

  • 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:

総分子量:g/mol

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

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 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

PARPシグナル伝達経路

PARP Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID