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 NGDqdoFHfW6ldHnvckBCe3OjeR?= MWqwMlEwOS93MECvNVAxOCCwTR?= M1P6bolvcGmkaYTzJHBCWlBiYXP0bZZqfHliYYSgd5RienSrbnegZ49v[2W{boTyZZRqd25ib3[gOVAxKG6P NYXmUI9SOjVzMki0OVU>
BT474 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\X[Yo2ODBibl2= M1vNb|Ex6oDVMUZCpIQ> NWPQcoQ5emWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>? M1fqS|I2OTJ6NEW1
SKBR3 M2LhVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vCPFUxOCCwTR?= NVL4dlcxOTEkgKOxOeKh\A>? Mlm5doVlfWOnczDj[YxtKGe{b4f0bEBqdiC2aHWg[o92eiCuaX7ld{BidmRic3nncolncWOjboTsfS=> NYfVepZjOjVzMki0OVU>
AU565 NF3uRYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zBXlUxOCCwTR?= Mn;nNVDjiJNzNdMg[C=> M{PJW5Jm\HWlZYOgZ4VtdCCpcn;3eIghcW5idHjlJIZwfXJibHnu[ZMh[W6mIIPp[45q\mmlYX70cJk> M2TZRVI2OTJ6NEW1
EFM192A M2HVOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfqOVAxKG6P NWjSXYVkOTEkgKOxOeKh\A>? NH35S21z\WS3Y3XzJINmdGxiZ4Lve5RpKGmwIITo[UBnd3W{IHzpcoV{KGGwZDDzbYdvcW[rY3HueIx6 MVyyOVEzQDR3NR?=
MDA-MB-231 MoOxSpVv[3Srb36gRZN{[Xl? NYLnS5J1OTBxMkCvOFAh|ryP M2ftXVI1KGh? NHPEbXdqdmO{ZXHz[ZMheC2DS2SgcIV3\Wy|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MUOyOFQzODF3Mh?=
MDA-MB-231 NH[yRXNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYLIZmh3OC5zLUSwJO69VQ>? NY\qellvOjRiaB?= MnPLTWM2OOLCiU5ihKkyPy55N9Mg{txO MW[yOFQzODF3Mh?=
MDA-MB-231 MmHqRZBweHSxc3nzJGF{e2G7 MWqxNE8zOC92MDFOwG0> MnOwNlQhcA>? NFPVS3pqdmS3Y3XzJIFxd3C2b4Ppd{Bld3OnIHTldIVv\GWwdHz5 MVWyOFQzODF3Mh?=
MDA-MB-231 M3mxZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[xNE8zOC92MDFOwG0> MVKyOEBp NHfL[pZjdG:la4OgZ4VtdCCleXPs[UBxem:pcnXzd4lwdiCrbjDHNk9OKHCqYYPl NHruN|AzPDR{MEG1Ni=>
H460 MkjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX:0NFAhdk1? M3e0eFI1yqCq NVfGe4lMcW6lcnXhd4V{KGOnbHz1cIFzKHKjZHnvd4Vve2m2aY\peJk> MmfONlQ1OTF4MUG=
A549  M2jQfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHaOFAxKG6P NFrHOZczPMLiaB?= NWTPeoVtcW6lcnXhd4V{KGOnbHz1cIFzKHKjZHnvd4Vve2m2aY\peJk> M2H4UlI1PDFzNkGx
DT40 NUi4UYtbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTJzIH7N MUCyOFM2PjhzMx?=
DU145 Mlz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nJfmlEPTB;MUigcm0> M{TaclI1OzV4OEGz
COLO704 M1zBO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTJwNUKgxtEhOC54NzFOwG0> NVT4bWJvOjN5Mkm0NFI>
OVMANAb NHH5d2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LhbGlEPTB;Mj61PEDDuSByLkO4JO69VQ>? NVv3OGVtOjN5Mkm0NFI>
OV177 M4[zdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7ENYlKSzVyPUKuO|ghyrFiMD63NUDPxE1? MVGyN|czQTRyMh?=
OAW28 M3PkW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPLTWM2OD1|Lk[xJOKyKDBwMkig{txO NULtN3FsOjN5Mkm0NFI>
OVSAHO M3r3[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rw[mlEPTB;Mz62OEDDuSByLkOzJO69VQ>? NGn0d3MzOzd{OUSwNi=>
OVKATE NELQd2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\DTWM2OD1|Lk[0JOKyKDFwN{mg{txO MojKNlM4Ojl2MEK=
OVCAR3 MmThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVX2ZWNvUUN3ME2zMlc1KMLzIECuOFAh|ryP MUmyN|czQTRyMh?=
PEO14 NVW0dW16T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTyTWM2OD1|Lki0JOKyKDBwN{[g{txO M1jQOFI{PzJ7NECy
A2780 Ml\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\DUmlEPTB;Mz65OEDDuSByLkK1JO69VQ>? MVWyN|czQTRyMh?=
OVTOKO MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTRwMUSgxtEhOS53MzFOwG0> MYWyN|czQTRyMh?=
KURAMOCHIb MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTweVNRUUN3ME20MlM1KMLzIECuNlkh|ryP MoLQNlM4Ojl2MEK=
TOV21G NV;kW2tvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELPbJlKSzVyPUWuNFchyrFiMT6zNEDPxE1? NEX5[YUzOzd{OUSwNi=>
OVISE NIKyfolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFr3[opKSzVyPUWuOlghyrFiMD6yN{DPxE1? Ml7uNlM4Ojl2MEK=
KK M{D0[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTZwMUWgxtEhOS52MjFOwG0> M4LUN|I{PzJ7NECy
RMUGS Mle5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXzTWM2OD15LkCzJOKyKDFwOEOg{txO NHnqWYUzOzd{OUSwNi=>
PEO6 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTdwME[gxtEhOC55NDFOwG0> MoXGNlM4Ojl2MEK=
OVCA429 MmPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfZTWM2OD16LkK5JOKyKDFwNkSg{txO NGfX[JMzOzd{OUSwNi=>
OV167 NWfRZXVDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRThwM{OgxtEhOS5zODFOwG0> MmG0NlM4Ojl2MEK=
RMG1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkThTWM2OD17LkOyJOKyKDJwM{[g{txO NX61PGd5OjN5Mkm0NFI>
OVCAR5 NIDo[|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTsU4lKSzVyPUmuOVAhyrFiMj61PUDPxE1? Mnf6NlM4Ojl2MEK=
EFO21 M363dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml:4TWM2OD17LkmyJOKyKDFwOEeg{txO Mme5NlM4Ojl2MEK=
ES2 M3m3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHkTWM2OD1zMD6xNkDDuSBzLkKzJO69VQ>? Mmj5NlM4Ojl2MEK=
Tyk-nu M2C4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFyLkKwJOKyKDFwMUKg{txO MXuyN|czQTRyMh?=
CAOV3 NHjJZ4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnF[mVxUUN3ME2xNE4{PyEEsTCwMlg4KM7:TR?= Mk\ONlM4Ojl2MEK=
OV207 NG\NU45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{n5U2lEPTB;MUKuNlchyrFiMD6zNkDPxE1? M3vocFI{PzJ7NECy
HEY MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTF|LkCxJOKyKDBwN{Wg{txO NGPtV3UzOzd{OUSwNi=>
DOV13 NUjHOFh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXmTWM2OD5zNTFOwG0> MYmyN|czQTRyMh?=
EFO27 NIjwbnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;OSIpKSzVyPkG1JO69VQ>? NGPZRpEzOzd{OUSwNi=>
HEY C2 M1TMUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWm4OIJLUUN3ME6xOUDPxE1? M17JXFI{PzJ7NECy
KOC-7cc NH;nem1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe2e2tKSzVyPkG1JO69VQ>? NV7tSZNxOjN5Mkm0NFI>
MCASb MmfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRjF3IN88US=> MnXBNlM4Ojl2MEK=
OAW42 NXnTN4h4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmX1TWM2OD5zNTFOwG0> NFO0WJgzOzd{OUSwNi=>
OV2008 NYS5cWlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTjTWM2OD5zNTFOwG0> MX[yN|czQTRyMh?=
OV90 NGTHTYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33qPGlEPTB-MUWg{txO NH\WdlEzOzd{OUSwNi=>
OVCA420b MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjXTlhNUUN3ME6xOUDPxE1? MVOyN|czQTRyMh?=
OVCA432 MmjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fG[GlEPTB-MUWg{txO NVzoVo9lOjN5Mkm0NFI>
PEA2 NEjCZldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HlOWlEPTB-MUWg{txO NVK5c5l3OjN5Mkm0NFI>
SKOV3 MknFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLwTWM2OD5zNTFOwG0> NXzlT40{OjN5Mkm0NFI>
TOV112D Mn6xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYewMVMh|ryP NFzWXJdKSzVyPkG1JO69VQ>? NGD3dpIzOzd{OUSwNi=>
C4-2 M4LjS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXq3U5pFOC1|IN88US=> M3LPNlE1KGR? M{\RPGROW09? MkjP[IVkemWjc3XzJINwdG:weTDueY1j\XJiZH;z[UBl\XCnbnTlcpRtgQ>? Mk\YNlM2PjV{NES=
PC3 NES1XYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPremwxNTNizszN NHW0NlMyPCCm NU\Q[o4{TE2VTx?= Morl[IVkemWjc3XzJINwdG:weTDueY1j\XJiZH;z[UBl\XCnbnTlcpRtgQ>? M3fIU|I{PTZ3MkS0
DU145 NGDpTo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYqwMVMh|ryP NVHSN4dEOTRiZB?= MULEUXNQ NES4e2Nl\WO{ZXHz[ZMh[2:ub375JI52dWKncjDkc5NmKGSncHXu[IVvfGy7 MUOyN|U3PTJ2NB?=
VCaP  NYLCUXRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:wMVMh|ryP MnTKNVQh\A>? MlrHSG1UVw>? NIPGeG1l\WO{ZXHz[ZMh[2:ub375JI52dWKncjDkc5NmKGSncHXu[IVvfGy7 NX7XT4ZZOjN3NkWyOFQ>
LNCaP  NFK4NGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvRNE0{KM7:TR?= MmXrNVQh\A>? M4nTS2ROW09? NHzQSVRl\WO{ZXHz[ZMh[2:ub375JI52dWKncjDkc5NmKGSncHXu[IVvfGy7 MkLMNlM2PjV{NES=
MDA-MB-468 MmXXR4VtdCCYaXHibYxqfHliQYPzZZk> NGTsW|NKSzVyPUmuO{DPxE1? M1ThfVIzPjd6MU[x
MDA-MB-231 M3\UZmNmdGxiVnnhZoltcXS7IFHzd4F6 MkXYTWM2OD1zMzFOwG0> Mmf6NlI3PzhzNkG=
Cal-51 NUGwTnVZS2WubDDWbYFjcWyrdImgRZN{[Xl? MXTJR|UxRThwNjFOwG0> NWC3WZZsOjJ4N{ixOlE>

... 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 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 84 mg/mL (199.35 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
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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