Rucaparib (AG-014699,PF-01367338) 化学構造
分子量: 421.36

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製品説明

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製品の説明

生物活性

製品説明 Rucaparib (AG-014699,PF-01367338)はPARPを抑制、Ki値が1.4 nMです。
ターゲット PARP
IC50 1.4 nM (Ki) [1]
In vitro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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
BT-474 Mm\KSpVv[3Srb36gRZN{[Xl? M1f1elAvOS9zL{WwNE8yODByIH7N MUPpcohq[mm2czDQRXJRKGGldHn2bZR6KGG2IIP0ZZJ1cW6pIHPvcoNmem62cnH0bY9vKG:oIEWwNEBvVQ>? NWnoTZFyOjVzMki0OVU>
BT474 M4TNTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXsOVAxKG6P NF3iPJQyOOLCk{G1xsBl NIPDdZNz\WS3Y3XzJINmdGxiZ4Lve5RpKGmwIITo[UBnd3W{IHzpcoV{KGGwZDDzbYdvcW[rY3HueIx6 MlzNNlUyOjh2NUW=
SKBR3 M2TyXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPTU482ODBibl2= MV:xNQKBmzF3wrDk Ml3NdoVlfWOnczDj[YxtKGe{b4f0bEBqdiC2aHWg[o92eiCuaX7ld{BidmRic3nncolncWOjboTsfS=> NHvvS|MzPTF{OES1OS=>
AU565 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1q3TlUxOCCwTR?= M1ztNlEx6oDVMUZCpIQ> NFvDWG5z\WS3Y3XzJINmdGxiZ4Lve5RpKGmwIITo[UBnd3W{IHzpcoV{KGGwZDDzbYdvcW[rY3HueIx6 NEHDcY4zPTF{OES1OS=>
EFM192A NGX4[WhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWC1NFAhdk1? MUexNQKBmzF3wrDk NI\DdINz\WS3Y3XzJINmdGxiZ4Lve5RpKGmwIITo[UBnd3W{IHzpcoV{KGGwZDDzbYdvcW[rY3HueIx6 M1PDOFI2OTJ6NEW1
MDA-MB-231 MULGeY5kfGmxbjDBd5NigQ>? MlrKNVAwOjBxNECg{txO NHr5R4szPCCq M2\sV4lv[3KnYYPld{BxNUGNVDDs[ZZmdHNiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHezOG8zPDR{MEG1Ni=>
MDA-MB-231 MYXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3mx[FAvOS12MDFOwG0> MV6yOEBp M2W3U2lEPTEkgJm95qCKOTdwN{hCpO69VQ>? NX23[ZFCOjR2MkCxOVI>
MDA-MB-231 MmCzRZBweHSxc3nzJGF{e2G7 Mlu1NVAwOjBxNECg{txO MX[yOEBp MoDEbY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= MmHYNlQ1OjBzNUK=
MDA-MB-231 NHHNeVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWi0Nm1tOTBxMkCvOFAh|ryP MkTpNlQhcA>? NWLFWoVl[myxY3vzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25iaX6gS|IwVSCyaHHz[S=> M{PLUVI1PDJyMUWy
H460 M{i5emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV:3d5Z4PDByIH7N M1j0d|I1yqCq NV7CeHdScW6lcnXhd4V{KGOnbHz1cIFzKHKjZHnvd4Vve2m2aY\peJk> MVKyOFQyOTZzMR?=
A549  M1;DNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYO0NFAhdk1? NVv3UHA4OjUEoHi= MnOybY5kemWjc3XzJINmdGy3bHHyJJJi\Gmxc3Xud4l1cX[rdIm= M33EZVI1PDFzNkGx
DT40 NYq5[nlTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PrbWlEPTB;MkGgcm0> NU\5XIxlOjR|NU[4NVM>
DU145 NVHES5VOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTF6IH7N M4rlNVI1OzV4OEGz
COLO704 NGfMSpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfNVoJKSzVyPUKuOVIhyrFiMD62O{DPxE1? NFjpOJozOzd{OUSwNi=>
OVMANAb M4HISGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrNcpFqUUN3ME2yMlU5KMLzIECuN|gh|ryP MUCyN|czQTRyMh?=
OV177 NYfURlRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{m5ZmlEPTB;Mj63PEDDuSByLkexJO69VQ>? MmC0NlM4Ojl2MEK=
OAW28 NVXCfWdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTNwNkGgxtEhOC5{ODFOwG0> M4G2O|I{PzJ7NECy
OVSAHO NHfDPYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzrSFVKSzVyPUOuOlQhyrFiMD6zN{DPxE1? M3jMO|I{PzJ7NECy
OVKATE Mk\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfLS2pKSzVyPUOuOlQhyrFiMT63PUDPxE1? NWS3e416OjN5Mkm0NFI>
OVCAR3 NVXiXphyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2r2bGlEPTB;Mz63OEDDuSByLkSwJO69VQ>? NEfrTowzOzd{OUSwNi=>
PEO14 NGHzSYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1j2dmlEPTB;Mz64OEDDuSByLke2JO69VQ>? MUCyN|czQTRyMh?=
A2780 NI\qe2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XwT2lEPTB;Mz65OEDDuSByLkK1JO69VQ>? NFn5PXkzOzd{OUSwNi=>
OVTOKO MnHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTRwMUSgxtEhOS53MzFOwG0> Ml2wNlM4Ojl2MEK=
KURAMOCHIb NV;vV5pQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTRwM{SgxtEhOC5{OTFOwG0> M2jSPVI{PzJ7NECy
TOV21G NFXSbHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXIfmZKSzVyPUWuNFchyrFiMT6zNEDPxE1? MknlNlM4Ojl2MEK=
OVISE NULOdlRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{f2fWlEPTB;NT62PEDDuSByLkKzJO69VQ>? NVL0cZNZOjN5Mkm0NFI>
KK NITpN4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfsSZFKSzVyPU[uNVUhyrFiMT60NkDPxE1? MXOyN|czQTRyMh?=
RMUGS MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTdwMEOgxtEhOS56MzFOwG0> MXiyN|czQTRyMh?=
PEO6 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjFTWM2OD15LkC2JOKyKDBwN{Sg{txO M3nmVFI{PzJ7NECy
OVCA429 NHLEW|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HhS2lEPTB;OD6yPUDDuSBzLk[0JO69VQ>? MnzoNlM4Ojl2MEK=
OV167 NVvhXopkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrmWY5uUUN3ME24MlM{KMLzIEGuNVgh|ryP MYeyN|czQTRyMh?=
RMG1 M2[wN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3H3dmlEPTB;OT6zNkDDuSB{LkO2JO69VQ>? NXnpcnF4OjN5Mkm0NFI>
OVCAR5 M{fHNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorwTWM2OD17LkWwJOKyKDJwNUmg{txO MoX5NlM4Ojl2MEK=
EFO21 Ml7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\2dWN3UUN3ME25MlkzKMLzIEGuPFch|ryP M1fOZVI{PzJ7NECy
ES2 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PhR2lEPTB;MUCuNVIhyrFiMT6yN{DPxE1? MYGyN|czQTRyMh?=
Tyk-nu MlnuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LRdWlEPTB;MUCuNlAhyrFiMT6xNkDPxE1? MXuyN|czQTRyMh?=
CAOV3 M2qzfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjOPGVKUUN3ME2xNE4{PyEEsTCwMlg4KM7:TR?= NULKdmtUOjN5Mkm0NFI>
OV207 NFq3TpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGf3NnlKSzVyPUGyMlI4KMLzIECuN|Ih|ryP MmLLNlM4Ojl2MEK=
HEY NYnQXZF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnL1TWM2OD1zMz6wNUDDuSByLke1JO69VQ>? NIjGSWozOzd{OUSwNi=>
DOV13 NIG3[FhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH[4cXdKSzVyPkG1JO69VQ>? MVGyN|czQTRyMh?=
EFO27 M{ewbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRjF3IN88US=> MlHUNlM4Ojl2MEK=
HEY C2 MmXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGW5bXJKSzVyPkG1JO69VQ>? Mn:xNlM4Ojl2MEK=
KOC-7cc M3HNV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPXS2lKSzVyPkG1JO69VQ>? MlzaNlM4Ojl2MEK=
MCASb NFfvWXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjkepRNUUN3ME6xOUDPxE1? NXPQeFhnOjN5Mkm0NFI>
OAW42 MlnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHj6[m1KSzVyPkG1JO69VQ>? MmnkNlM4Ojl2MEK=
OV2008 NWHEVIs{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTRUpFLUUN3ME6xOUDPxE1? M3noOlI{PzJ7NECy
OV90 NUfQTZVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX35OnprUUN3ME6xOUDPxE1? M3fyXVI{PzJ7NECy
OVCA420b MlfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRjF3IN88US=> NVjjdI5FOjN5Mkm0NFI>
OVCA432 MnPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rhZmlEPTB-MUWg{txO MnLCNlM4Ojl2MEK=
PEA2 NGDPb5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjldHFKSzVyPkG1JO69VQ>? MkXCNlM4Ojl2MEK=
SKOV3 NYLD[Vh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRjF3IN88US=> MXSyN|czQTRyMh?=
TOV112D MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PHelAuOyEQvF2= NUmxTpo6UUN3ME6xOUDPxE1? MoPTNlM4Ojl2MEK=
C4-2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33BNFAuOyEQvF2= Mo\qNVQh\A>? NEHLNIdFVVOR NVjubFRD\GWlcnXhd4V{KGOxbH;ufUBvfW2kZYKg[I9{\SCmZYDlcoRmdnSueR?= NWjWWIl1OjN3NkWyOFQ>
PC3 NXHtRXFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjqTlQxNTNizszN NUn4S2xOOTRiZB?= MkC0SG1UVw>? Ml20[IVkemWjc3XzJINwdG:weTDueY1j\XJiZH;z[UBl\XCnbnTlcpRtgQ>? MmLSNlM2PjV{NES=
DU145 NIjZOI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELkV4MxNTNizszN MUCxOEBl NIfMbZFFVVOR NV\oTGdu\GWlcnXhd4V{KGOxbH;ufUBvfW2kZYKg[I9{\SCmZYDlcoRmdnSueR?= MmW1NlM2PjV{NES=
VCaP  MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfwS|cxNTNizszN MoX0NVQh\A>? MmPOSG1UVw>? MnvV[IVkemWjc3XzJINwdG:weTDueY1j\XJiZH;z[UBl\XCnbnTlcpRtgQ>? NXfCfXlTOjN3NkWyOFQ>
LNCaP  MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDrepcxNTNizszN NW\6cWNsOTRiZB?= NH;w[XVFVVOR MYnk[YNz\WG|ZYOgZ49td267IH71cYJmeiCmb4PlJIRmeGWwZHXueIx6 MXOyN|U3PTJ2NB?=
MDA-MB-468 NXv2ZY1GS2WubDDWbYFjcWyrdImgRZN{[Xl? MYTJR|UxRTlwNzFOwG0> MWCyNlY4QDF4MR?=
MDA-MB-231 NIHifpNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXzJR|UxRTF|IN88US=> NI\vVoMzOjZ5OEG2NS=>
Cal-51 NFvnWVZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFHrd4NKSzVyPUiuOkDPxE1? MmHtNlI3PzhzNkG=

... Click to View More Cell Line Experimental Data

In vivo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]
臨床試験 Rucaparib is currently in Phase II clinical trials for locally advanced/metastatic breast or advanced ovarian cancer.
特集 The first PARP inhibitor used in clinical trials combined with temozolomide.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.
Inhibition of PARP activity Inhibition of PARP activity in 5 × 103 D283Med cells is measured using various concentrations of Rucaparib (0-1 μM), compared with DMSO-only. Maximally stimulated PARP activity is measured in samples of permeabilised cells by immunologica

細胞アッセイ: [4]

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.

動物実験: [4]

動物モデル CD-1 nude mice bearing established D283Med xenografts
製剤 Normal saline
投薬量 1 mg/kg
投与方法 One or four daily by i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Rucaparib (AG-014699,PF-01367338) SDF
分子量 421.36
化学式

C19H18FN3O.H3PO4

CAS No. 459868-92-9
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 84 mg/mL (199.35 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 8-fluoro-5-(4-((methylamino)methyl)phenyl)-3,4-dihydro-2H-azepino[5,4,3-cd]indol-1(6H)-one phosphoric acid

文献中の引用 (14)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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