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

高品質保証

カスタマーフィードバック(6)

Quality Control & MSDS

製品説明

  • Compare PARP Inhibitors
    PARP製品生物活性の比較
  • 研究分野

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 MlfDSpVv[3Srb36gRZN{[Xl? M3\sdFAvOS9zL{WwNE8yODByIH7N NILNWI5qdmirYnn0d{BRSVKSIHHjeIl3cXS7IHH0JJN1[XK2aX7nJINwdmOncn70doF1cW:wIH;mJFUxOCCwTR?= M3TKW|I2OTJ6NEW1
BT474 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnCfm42ODBibl2= MlnkNVDjiJNzNdMg[C=> NVXzcW9YemWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>? MnS4NlUyOjh2NUW=
SKBR3 Mk\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjHcWw2ODBibl2= NFThZW8yOOLCk{G1xsBl MmC0doVlfWOnczDj[YxtKGe{b4f0bEBqdiC2aHWg[o92eiCuaX7ld{BidmRic3nncolncWOjboTsfS=> M3vHRVI2OTJ6NEW1
AU565 NEn0UWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWG1NFAhdk1? NEXh[pkyOOLCk{G1xsBl NX3yTm97emWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>? MkD1NlUyOjh2NUW=
EFM192A MkHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M335OFUxOCCwTR?= NXHvPGt[OTEkgKOxOeKh\A>? M4jMXZJm\HWlZYOgZ4VtdCCpcn;3eIghcW5idHjlJIZwfXJibHnu[ZMh[W6mIIPp[45q\mmlYX70cJk> NGj4[oQzPTF{OES1OS=>
MDA-MB-231 MVHGeY5kfGmxbjDBd5NigQ>? NYnuSW02OTBxMkCvOFAh|ryP NV3GSW9FOjRiaB?= NHzJOWZqdmO{ZXHz[ZMheC2DS2SgcIV3\Wy|IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MWGyOFQzODF3Mh?=
MDA-MB-231 NGPvVJZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkTqNE4yNTRyIN88US=> NVPib3JsOjRiaB?= MkPoTWM2OOLCiU5ihKkyPy55N9Mg{txO NV3MdoNGOjR2MkCxOVI>
MDA-MB-231 MUDBdI9xfG:|aYOgRZN{[Xl? MlywNVAwOjBxNECg{txO NF2wU4gzPCCq MWTpcoR2[2W|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7 M33EVFI1PDJyMUWy
MDA-MB-231 NW\6[nJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYSxNE8zOC92MDFOwG0> MVqyOEBp NEO4fmFjdG:la4OgZ4VtdCCleXPs[UBxem:pcnXzd4lwdiCrbjDHNk9OKHCqYYPl NX;DXpdqOjR2MkCxOVI>
H460 NF25RXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUO0NFAhdk1? NIHXO5kzPMLiaB?= M4TwO4lv[3KnYYPld{Bk\WyudXzhdkBz[WSrb4PlcpNqfGm4aYT5 NX7rUHVQOjR2MUG2NVE>
A549  NV;4T3Z6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[2OFAxKG6P M{XtO|I1yqCq MkjybY5kemWjc3XzJINmdGy3bHHyJJJi\Gmxc3Xud4l1cX[rdIm= MXOyOFQyOTZzMR?=
DT40 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTIV2wxUUN3ME2yNUBvVQ>? MYSyOFM2PjhzMx?=
DU145 NFTk[pdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3ES3I{UUN3ME2xPEBvVQ>? M4HIdVI1OzV4OEGz
COLO704 NEHUN3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPJUm5KSzVyPUKuOVIhyrFiMD62O{DPxE1? Mmr5NlM4Ojl2MEK=
OVMANAb NUHsW5hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jPeWlEPTB;Mj61PEDDuSByLkO4JO69VQ>? NUfWb2I{OjN5Mkm0NFI>
OV177 M4T2PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrXTWM2OD1{Lke4JOKyKDBwN{Gg{txO NEjL[3kzOzd{OUSwNi=>
OAW28 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPiTWM2OD1|Lk[xJOKyKDBwMkig{txO M1rFOFI{PzJ7NECy
OVSAHO MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjHTWM2OD1|Lk[0JOKyKDBwM{Og{txO MXuyN|czQTRyMh?=
OVKATE MkHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXPTWM2OD1|Lk[0JOKyKDFwN{mg{txO NW\FdZVsOjN5Mkm0NFI>
OVCAR3 NH71fmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTNwN{SgxtEhOC52MDFOwG0> NEDwVW8zOzd{OUSwNi=>
PEO14 MnLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjVe4x2UUN3ME2zMlg1KMLzIECuO|Yh|ryP M3fjfVI{PzJ7NECy
A2780 M1L0Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\GUmVKSzVyPUOuPVQhyrFiMD6yOUDPxE1? NEX1fpczOzd{OUSwNi=>
OVTOKO MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPKTWM2OD12LkG0JOKyKDFwNUOg{txO NG\2ZYQzOzd{OUSwNi=>
KURAMOCHIb NVXHR4dXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTRwM{SgxtEhOC5{OTFOwG0> NWjQV3A2OjN5Mkm0NFI>
TOV21G MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rjOGlEPTB;NT6wO{DDuSBzLkOwJO69VQ>? M3u4OVI{PzJ7NECy
OVISE MknHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmCxTWM2OD13Lk[4JOKyKDBwMkOg{txO MX:yN|czQTRyMh?=
KK Ml3FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7Y[ZJKSzVyPU[uNVUhyrFiMT60NkDPxE1? MWeyN|czQTRyMh?=
RMUGS MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzhTWM2OD15LkCzJOKyKDFwOEOg{txO MV2yN|czQTRyMh?=
PEO6 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP6TWM2OD15LkC2JOKyKDBwN{Sg{txO M1fENlI{PzJ7NECy
OVCA429 NXzGcGJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnKzTWM2OD16LkK5JOKyKDFwNkSg{txO M{\BbVI{PzJ7NECy
OV167 NGnsTFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDUbo9LUUN3ME24MlM{KMLzIEGuNVgh|ryP MnzhNlM4Ojl2MEK=
RMG1 MmGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\pS4VKSzVyPUmuN|IhyrFiMj6zOkDPxE1? NGjxc2szOzd{OUSwNi=>
OVCAR5 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkH2TWM2OD17LkWwJOKyKDJwNUmg{txO NHP2ToczOzd{OUSwNi=>
EFO21 NVLxUndYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPHTWM2OD17LkmyJOKyKDFwOEeg{txO NYXUS4FOOjN5Mkm0NFI>
ES2 NULX[YZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rpUmlEPTB;MUCuNVIhyrFiMT6yN{DPxE1? NYr6dVR7OjN5Mkm0NFI>
Tyk-nu NEjJV|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLlTWM2OD1zMD6yNEDDuSBzLkGyJO69VQ>? MXGyN|czQTRyMh?=
CAOV3 NYnIZW9xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTFyLkO3JOKyKDBwOEeg{txO NETBRYUzOzd{OUSwNi=>
OV207 M3TrdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTF{LkK3JOKyKDBwM{Kg{txO NEjJ[5czOzd{OUSwNi=>
HEY NV;GeIFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFW5T3pKSzVyPUGzMlAyKMLzIECuO|Uh|ryP MkD6NlM4Ojl2MEK=
DOV13 Mm\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRjF3IN88US=> MViyN|czQTRyMh?=
EFO27 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrsTWM2OD5zNTFOwG0> M2fQOFI{PzJ7NECy
HEY C2 MlH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjBTWM2OD5zNTFOwG0> NH3ORXEzOzd{OUSwNi=>
KOC-7cc MomzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvRWnZ5UUN3ME6xOUDPxE1? MnzRNlM4Ojl2MEK=
MCASb M{TYOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{mzWGlEPTB-MUWg{txO M33DOlI{PzJ7NECy
OAW42 M3e3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{S3c2lEPTB-MUWg{txO NX:0PItTOjN5Mkm0NFI>
OV2008 MoKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LZUmlEPTB-MUWg{txO Mnq3NlM4Ojl2MEK=
OV90 NV:0TGhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRjF3IN88US=> NUTm[Wd4OjN5Mkm0NFI>
OVCA420b NVnod|BkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRjF3IN88US=> M3nMfVI{PzJ7NECy
OVCA432 MliwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGKxd5NKSzVyPkG1JO69VQ>? NYraWno1OjN5Mkm0NFI>
PEA2 MlLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTuZXM{UUN3ME6xOUDPxE1? M1TZWlI{PzJ7NECy
SKOV3 NIrQOVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWG1RXN1UUN3ME6xOUDPxE1? M{LR[VI{PzJ7NECy
TOV112D NFrkR2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILEN28xNTNizszN NVzD[Ic5UUN3ME6xOUDPxE1? M1POTVI{PzJ7NECy
C4-2 NFzLNWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYiwMVMh|ryP MmmwNVQh\A>? MlzoSG1UVw>? MV7k[YNz\WG|ZYOgZ49td267IH71cYJmeiCmb4PlJIRmeGWwZHXueIx6 NX3ZU4cyOjN3NkWyOFQ>
PC3 Mny1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfqVZoxNTNizszN MYmxOEBl MVPEUXNQ MmOw[IVkemWjc3XzJINwdG:weTDueY1j\XJiZH;z[UBl\XCnbnTlcpRtgQ>? MUiyN|U3PTJ2NB?=
DU145 NXS3fmx6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTsbY0xNTNizszN MkfYNVQh\A>? MVzEUXNQ M4\F[oRm[3KnYYPld{Bkd2yxbomgcpVu[mW{IHTvd4Uh\GWyZX7k[Y51dHl? MWGyN|U3PTJ2NB?=
VCaP  M{fFcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVWwMVMh|ryP MmrNNVQh\A>? NYnqfpE4TE2VTx?= NWHhe|Ez\GWlcnXhd4V{KGOxbH;ufUBvfW2kZYKg[I9{\SCmZYDlcoRmdnSueR?= NV\6SVhKOjN3NkWyOFQ>
LNCaP  NVnEXFVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3z1ZlAuOyEQvF2= MUexOEBl MX;EUXNQ NYXOZVlM\GWlcnXhd4V{KGOxbH;ufUBvfW2kZYKg[I9{\SCmZYDlcoRmdnSueR?= NEXTdXIzOzV4NUK0OC=>
MDA-MB-468 MX\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVjJR|UxRTlwNzFOwG0> M3TTe|IzPjd6MU[x
MDA-MB-231 NYjOW3RmS2WubDDWbYFjcWyrdImgRZN{[Xl? MkTrTWM2OD1zMzFOwG0> MkiyNlI3PzhzNkG=
Cal-51 MnP0R4VtdCCYaXHibYxqfHliQYPzZZk> M1jsNmlEPTB;OD62JO69VQ>? M4XOUlIzPjd6MU[x

... 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

カスタマーフィードバック (6)


Click to enlarge
Rating
Source Eur J Cancer, 2014, 50(15), 2725-34. Rucaparib (AG-014699,PF-01367338) purchased from Selleck
Method Clonogenic assays
Cell Lines BT474 cells
Concentrations 500, 1000 nM
Incubation Time 10-15 days
Results Rucaparib significantly reduced clonogenic growth and PAR production at the concentration of 300 nM, and the effect was greater at a higher concentration of 1000 nM. Of note, pharmacokinetic data from a phase I trial suggest that these are clinically achievable plasma concentrations.

Click to enlarge
Rating
Source Eur J Cancer, 2014, 50(15), 2725-34. Rucaparib (AG-014699,PF-01367338) purchased from Selleck
Method Western blot
Cell Lines BT-474 cells
Concentrations 0.01-1000 nM
Incubation Time 6 h
Results It tested the drug rucaparib, which target PARP. It decided to test two different PARP inhibitors to reasonably study whether effects on cell growth were class-dependent instead of drug dependent. It confirmed that rucaparib inhibited PARP activity, as assayed by western blot of its product (poly ADP-ribose (PAR) levels), at starting concentrations of 500 nM of rucaparib.

Click to enlarge
Rating
Source J Biol Chem, 2012, 287, 39824-33. Rucaparib (AG-014699,PF-01367338) purchased from Selleck
Method Western Blotting
Cell Lines HaCaT cells
Concentrations 1 μM
Incubation Time 30 min
Results preincubation of purified PARP-1 with AG-014699, a potent PARP inhibitor , prior to PARP-1 activation led to decreased associa-tion between PARP-1 and XPA.

Click to enlarge
Rating
Source Oral Oncol, 2014, 50(9), 825-31. Rucaparib (AG-014699,PF-01367338) purchased from Selleck
Method Fluorescence assay
Cell Lines HN4, SAS cells
Concentrations 10 uM
Incubation Time 24 h
Results For treatment with positive control (2 Gy IR), we found this to be the case. In sensitive cell lines, the median foci formation decreased and conversely, RAD51 foci formation in resistant cell lines increased after exposure to 2 Gy.

Click to enlarge
Rating
Source Urol Oncol, 2014, 32(5), 720-6. Rucaparib (AG-014699,PF-01367338) purchased from Selleck
Method CCK-8, flow cytometry, annexin V-FITC/PI staining
Cell Lines PC3 cells
Concentrations 10 uM
Incubation Time 24-48 h
Results The number of PC3 cells decreased significantly and the shape of PC3 cells became irregular after treatment with transfecting INPP4B gene combined with AG014699 treatment compared with single treatment (A). Next, it tested the proliferation of PC3 cells under the combined treatment. Compared with control, which combined with AG014699, the vitality of cells was 49.85%?.30%, 26.30%?.81%, and 9.72%?.10% after 24, 36, and 48 hours. Significant growth inhibition could be observed upon combination than transfection of INPP4B gene and AG014699 given separately (P<0.05) (B). Then the cell cycle distribution was detected. Transfection of INPP4B gene combined with AG014699 treatment caused a G1 arrest (C). Finally, we analyzed cell apoptosis, finding that compared with AG014699 alone, combination with transfection of INPP4B gene did not result in any further significant increase apoptosis rate (D).

Click to enlarge
Rating
Source Dr. David Schrmann from University of Base. Rucaparib (AG-014699,PF-01367338) purchased from Selleck
Method Kruskal-Wallis and the post-hoc Dunn’s Multiple Comparison tests, immuno-staining
Cell Lines Primary human lung fibroblast cells (MRC-5)
Concentrations 0-1 μM
Incubation Time 2 h
Results

文献中の引用 (14)

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related PARP 阻害剤

  • G007-LK

    G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.

  • NU1025

    NU1025 is a potent PARP inhibitor with IC50 of 400 nM.

  • SCR7

    SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ).

  • Blasticidin S HCl

    Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes, and acts as a DNA and protein synthesis inhibitor, used to select transfected cells carrying bsr or BSD resistance genes.

  • Olaparib (AZD2281, Ku-0059436)

    Olaparib(AZD2281, KU0059436)は1種の選択の阻害剤 、 PARP-1 と PARP-2 に作用する時、IC50 がそれぞれ 5 nM と 1 nMになる。

    Features:A potent PARP inhibitor (currently in late stage clinical trials).

  • Veliparib (ABT-888)

    Veliparib (ABT-888)は、PARP1PARP2の強力な阻害剤で、Kiがそれぞれ 5.2 nM と 2.9 nMになる。

    Features:Increases the efficacy of common cancer therapies such as radiation and alkylating agents.

  • Talazoparib (BMN 673)

    Talazoparib (BMN 673)は、新しい PARP 阻害剤で、IC50 が 0.58 nMです。

    Features:Most potent and selective PARPi reported thus far.

  • Iniparib (BSI-201)

    Iniparib (BSI-201)は、推定のPoly(ADPリボース)ポリメラーゼ(PARP I)阻害剤です

  • PJ34 HCl

    PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

    Features:Water-soluble PARP1/2 inhibitor with >10,000-fold potentcy vs. 3-aminobenzamide (prototypical PARP inhibitor). Potential uses in cardiovascular diseases (stroke, cerebral ischemia, & myocardial ischemia).

最近チェックしたアイテム

Tags: Rucaparib (AG-014699,PF-01367338)を買う | Rucaparib (AG-014699,PF-01367338)供給者 | Rucaparib (AG-014699,PF-01367338)を購入する | Rucaparib (AG-014699,PF-01367338)費用 | Rucaparib (AG-014699,PF-01367338)生産者 | オーダーRucaparib (AG-014699,PF-01367338) | Rucaparib (AG-014699,PF-01367338)代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ