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 NIS5U5BHfW6ldHnvckBCe3OjeR?= MX2wMlEwOS93MECvNVAxOCCwTR?= Mn7UbY5pcWKrdIOgVGFTWCCjY4Tpeol1gSCjdDDzeIFzfGmwZzDjc45k\XKwdILheIlwdiCxZjC1NFAhdk1? NVjWT4VUOjVzMki0OVU>
BT474 NXj6OmZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HqdVUxOCCwTR?= M3qwUFEx6oDVMUZCpIQ> MnXFdoVlfWOnczDj[YxtKGe{b4f0bEBqdiC2aHWg[o92eiCuaX7ld{BidmRic3nncolncWOjboTsfS=> NGTZZlIzPTF{OES1OS=>
SKBR3 NXezbJRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILU[|E2ODBibl2= M{iyS|Ex6oDVMUZCpIQ> NV\oPGY{emWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>? Mn7JNlUyOjh2NUW=
AU565 NY\JUWd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEWyOmY2ODBibl2= Ml\1NVDjiJNzNdMg[C=> MVry[YR2[2W|IHPlcIwh\3Kxd4ToJIlvKHSqZTDmc5VzKGyrbnXzJIFv\CC|aXfubYZq[2GwdHz5 NIPnSY4zPTF{OES1OS=>
EFM192A MnzpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYG1NFAhdk1? MX2xNQKBmzF3wrDk MWjy[YR2[2W|IHPlcIwh\3Kxd4ToJIlvKHSqZTDmc5VzKGyrbnXzJIFv\CC|aXfubYZq[2GwdHz5 NX\4eXNoOjVzMki0OVU>
MDA-MB-231 NIXBd3JHfW6ldHnvckBCe3OjeR?= NHOyZZIyOC9{MD:0NEDPxE1? NF7kT5IzPCCq MWfpcoNz\WG|ZYOgdE1CU1RibHX2[Yx{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MUGyOFQzODF3Mh?=
MDA-MB-231 M1nJeWNmdGxiVnnhZoltcXS7IFHzd4F6 NYSwVndUOC5zLUSwJO69VQ>? MlyxNlQhcA>? NVTURolrUUN3MPMAjV3jiIlzNz63O:Kh|ryP MlrzNlQ1OjBzNUK=
MDA-MB-231 MoXHRZBweHSxc3nzJGF{e2G7 MorNNVAwOjBxNECg{txO NFraSVgzPCCq NVKwVXN3cW6mdXPld{BieG:ydH;zbZMh\G:|ZTDk[ZBmdmSnboTsfS=> NFH5cGUzPDR{MEG1Ni=>
MDA-MB-231 M1;Yemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmf3NVAwOjBxNECg{txO NGXHN20zPCCq NH:xVYVjdG:la4OgZ4VtdCCleXPs[UBxem:pcnXzd4lwdiCrbjDHNk9OKHCqYYPl NUnWTHBEOjR2MkCxOVI>
H460 M2HjPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHnOFAxKG6P NUG0OHpCOjUEoHi= Mlz6bY5kemWjc3XzJINmdGy3bHHyJJJi\Gmxc3Xud4l1cX[rdIm= Mm\XNlQ1OTF4MUG=
A549  Mn30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXaOFAxKG6P MkT2NlTDqGh? MV3pcoNz\WG|ZYOgZ4VtdHWuYYKgdoFlcW:|ZX7zbZRqfmm2eR?= NYe0Z5NlOjR2MUG2NVE>
DT40 NXPtSphUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjYTWM2OD1{MTDuUS=> NVzSPIFbOjR|NU[4NVM>
DU145 M2TkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTF6IH7N NXPFPHdzOjR|NU[4NVM>
COLO704 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHGxTGxKSzVyPUKuOVIhyrFiMD62O{DPxE1? MmTUNlM4Ojl2MEK=
OVMANAb Mlq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTFd4Z5UUN3ME2yMlU5KMLzIECuN|gh|ryP MnPZNlM4Ojl2MEK=
OV177 NV[xT3JHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTJwN{igxtEhOC55MTFOwG0> M4nJUlI{PzJ7NECy
OAW28 M1H4Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGi4cpBKSzVyPUOuOlEhyrFiMD6yPEDPxE1? M33yVFI{PzJ7NECy
OVSAHO MlXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vzc2lEPTB;Mz62OEDDuSByLkOzJO69VQ>? M2rRTFI{PzJ7NECy
OVKATE NXHVOG9oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTNwNkSgxtEhOS55OTFOwG0> MlfoNlM4Ojl2MEK=
OVCAR3 NYfMVHI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfDOJRQUUN3ME2zMlc1KMLzIECuOFAh|ryP MXqyN|czQTRyMh?=
PEO14 NXniXIlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPUdYJKSzVyPUOuPFQhyrFiMD63OkDPxE1? NHn5PVMzOzd{OUSwNi=>
A2780 NFzrfnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTNwOUSgxtEhOC5{NTFOwG0> M33oXlI{PzJ7NECy
OVTOKO NYDMeVlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjETWM2OD12LkG0JOKyKDFwNUOg{txO NYjUXIxiOjN5Mkm0NFI>
KURAMOCHIb M4LjZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrnO3ZKSzVyPUSuN|QhyrFiMD6yPUDPxE1? NX3vW3FoOjN5Mkm0NFI>
TOV21G Mn;mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TSPWlEPTB;NT6wO{DDuSBzLkOwJO69VQ>? MW[yN|czQTRyMh?=
OVISE MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mor6TWM2OD13Lk[4JOKyKDBwMkOg{txO NYXyToJwOjN5Mkm0NFI>
KK MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrWTWM2OD14LkG1JOKyKDFwNEKg{txO NHS5PHIzOzd{OUSwNi=>
RMUGS NEXXRnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3q3TGlEPTB;Nz6wN{DDuSBzLkizJO69VQ>? M4TLR|I{PzJ7NECy
PEO6 NXn0fGh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPPTWM2OD15LkC2JOKyKDBwN{Sg{txO NUTqNVJsOjN5Mkm0NFI>
OVCA429 NULh[2VUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRThwMkmgxtEhOS54NDFOwG0> NV\TPIIyOjN5Mkm0NFI>
OV167 M{[5T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\ZN2lEPTB;OD6zN{DDuSBzLkG4JO69VQ>? MY[yN|czQTRyMh?=
RMG1 MlHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13lcmlEPTB;OT6zNkDDuSB{LkO2JO69VQ>? MkPNNlM4Ojl2MEK=
OVCAR5 M1vodGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzXTWM2OD17LkWwJOKyKDJwNUmg{txO MVKyN|czQTRyMh?=
EFO21 NWr1TFFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[yTWM2OD17LkmyJOKyKDFwOEeg{txO M2rvTVI{PzJ7NECy
ES2 M{HuTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTFyLkGyJOKyKDFwMkOg{txO M4DtPFI{PzJ7NECy
Tyk-nu NF\IOHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTNTWM2OD1zMD6yNEDDuSBzLkGyJO69VQ>? NIDDZXkzOzd{OUSwNi=>
CAOV3 NG\0dFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTFyLkO3JOKyKDBwOEeg{txO Mn34NlM4Ojl2MEK=
OV207 NHHyV3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\mRpBKSzVyPUGyMlI4KMLzIECuN|Ih|ryP M3XlTFI{PzJ7NECy
HEY MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULKV3RDUUN3ME2xN{4xOSEEsTCwMlc2KM7:TR?= MUGyN|czQTRyMh?=
DOV13 M3;zZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHyVpFmUUN3ME6xOUDPxE1? NHn5bZgzOzd{OUSwNi=>
EFO27 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfyTWM2OD5zNTFOwG0> NEjaNZkzOzd{OUSwNi=>
HEY C2 M{XkdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUmzdHhDUUN3ME6xOUDPxE1? NWSwZnZLOjN5Mkm0NFI>
KOC-7cc NH7lZYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjjemJKSzVyPkG1JO69VQ>? MWCyN|czQTRyMh?=
MCASb Mn7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jGdWlEPTB-MUWg{txO M4PXUlI{PzJ7NECy
OAW42 MkezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3EfVJKSzVyPkG1JO69VQ>? M4TpPVI{PzJ7NECy
OV2008 NYPwPY9iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLQTWM2OD5zNTFOwG0> MlvGNlM4Ojl2MEK=
OV90 NG\HZmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRjF3IN88US=> NEHncGczOzd{OUSwNi=>
OVCA420b MlPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDU[WlKSzVyPkG1JO69VQ>? M3q3T|I{PzJ7NECy
OVCA432 M4LiSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\BbGxoUUN3ME6xOUDPxE1? NGL5VI0zOzd{OUSwNi=>
PEA2 M3nhTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXm1Z2g4UUN3ME6xOUDPxE1? M2qwXVI{PzJ7NECy
SKOV3 NEDYWYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3sdVlKSzVyPkG1JO69VQ>? MXSyN|czQTRyMh?=
TOV112D NV\jSYVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILEUosxNTNizszN NHHFNm1KSzVyPkG1JO69VQ>? MkLMNlM4Ojl2MEK=
C4-2 NYn6PGc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHkNE0{KM7:TR?= NE\qdWEyPCCm MnXCSG1UVw>? M1H3OYRm[3KnYYPld{Bkd2yxbomgcpVu[mW{IHTvd4Uh\GWyZX7k[Y51dHl? MU[yN|U3PTJ2NB?=
PC3 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjSNE0{KM7:TR?= NVv1cm1NOTRiZB?= MWnEUXNQ MkXl[IVkemWjc3XzJINwdG:weTDueY1j\XJiZH;z[UBl\XCnbnTlcpRtgQ>? NF33XJUzOzV4NUK0OC=>
DU145 M3XFUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnWNE0{KM7:TR?= NFG1WGQyPCCm M2H3XGROW09? M33sT4Rm[3KnYYPld{Bkd2yxbomgcpVu[mW{IHTvd4Uh\GWyZX7k[Y51dHl? MX:yN|U3PTJ2NB?=
VCaP  NGfnWHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MViwMVMh|ryP NVzBdo5uOTRiZB?= NXfaZZlTTE2VTx?= NEDEUXpl\WO{ZXHz[ZMh[2:ub375JI52dWKncjDkc5NmKGSncHXu[IVvfGy7 NHfiRlUzOzV4NUK0OC=>
LNCaP  NV7TXYRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLlWXRDOC1|IN88US=> M{G2O|E1KGR? M4\LZ2ROW09? NWnZdph5\GWlcnXhd4V{KGOxbH;ufUBvfW2kZYKg[I9{\SCmZYDlcoRmdnSueR?= M1TL[|I{PTZ3MkS0
MDA-MB-468 MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEHnXopKSzVyPUmuO{DPxE1? NVjFd3Q1OjJ4N{ixOlE>
MDA-MB-231 NWm1TXBRS2WubDDWbYFjcWyrdImgRZN{[Xl? MXLJR|UxRTF|IN88US=> MkjtNlI3PzhzNkG=
Cal-51 MkO3R4VtdCCYaXHibYxqfHliQYPzZZk> MU\JR|UxRThwNjFOwG0> M1\2blIzPjd6MU[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.

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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.

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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.

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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)

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  • 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).

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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