Veliparib (ABT-888) 化学構造
分子量: 244.29

高品質保証

文献中の引用(37)

カスタマーフィードバック(9)

Quality Control & MSDS

製品説明

  • Compare PARP Inhibitors
    PARP製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • Veliparib (ABT-888)のメカニズム

製品の説明

生物活性

製品説明 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。
ターゲット

PARP1

PARP2

IC50

5.2 nM (Ki)

2.9 nM (Ki) [1]

In vitro試験 ABT-888 is inactive to SIRT2 (>5 μM). [1] ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells. [2] ABT-888 could decrease the PAR levels in both irradiated and nonirradiated H460 cells. ABT-888 also reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. ABT-888 increases apoptosis and autophagy in H460 cells when combination with radiation. [3] ABT-888 also inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. ABT-888 (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. ABT-888 shows effective radiosensitivity in oxic H1299 cells. Furthermore, ABT-888 could attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
C41 MUfLbY5ie2ViQYPzZZk> M{nuVlMxKG2rbh?= NEDSRoFKdmirYnn0bY9vKG:oIGDBVnAyKHerdHigSWM2OCCxZjCwMlAxOiEQvF2= MWKxPVg5QDd4MB?=
Jurkat NVrQVo1DU2mwYYPlJGF{e2G7 M176PVk3KGh? NW\CZ4IxTE2VTx?= MV;Jcohq[mm2aX;uJI9nKFCDUmCxJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDj[YxtKH[rYXLpcIl1gSC5aYToJGVEPTBib3[gN{DPxE1? M1fmT|I{QDVyMUm5
Capan1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYS3NkBp NXy4PXZbTE2VTx?= MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFLSR2EzKGenbnWgcZV1[XSnZDDoeY1idiCFYYDhclEh[2WubIOge4l1cCCLQ{WwJI9nKDN7Lkeg{txO NYXmXoltOjR|OUizPFM>
DT40 M3LkVGN6fG:2b4jpZ{BCe3OjeR?= M1LNflczKGh? Mny1SG1UVw>? NIWwTVREgXSxdH;4bYNqfHliYXfhbY5{fCClaHnjb4VvKEKUQ1GyMYRm\mmlaXXueEBFXDRyIHPlcIx{ M1LUeVI1QTJ{NUi3
ML-1 NEfiXmZCeG:ydH;0bYMhSXO|YYm= MWSyMlUh|ryP Mk[4NlQhcA>? MkLSSG1UVw>? M17LenN6dmW{Z3nzeIlk[WyueTDlcohidmOnczDUVmFKVC2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDNUE0yKGOnbHzz NUexeVhwOjR6OUWxN|U>
HCT-116 MlrDT4lv[XOnIFHzd4F6 MUewMlUh|ryP NHfoVlczPCCq NXrJRWh2WEGUUDDhZ5Rqfmm2eTDk[YNz\WG|ZYO= NHjxeW8zOzB3NEKxNy=>
UM-SCC1 MmXrR5l1d3SxeHnjJGF{e2G7 MUOxNEDPxE1? NHfFVIszPCCq NXixWXRyWmWmdXPld{B1cGViY3XscEB3cWGkaXzpeJk> NHrRb|EzOTlzMk[yNC=>
FaDu MWXDfZRwfG:6aXOgRZN{[Xl? MUOxNEDPxE1? MkPtNlQhcA>? M1n2N3Jm\HWlZYOgeIhmKGOnbHygeoli[mmuaYT5 M3XxXlIyQTF{NkKw
PC-3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV2xbVBYOTBizszN MYPJcoR2[2W|IHGgd4lodmmoaXPhcpQhcW6qaXLpeIlwdiCrbjDjc4xwdnliZn;ycYF1cW:wwrC= MoH1NlE2PzF7MUK=
EoL-1-cell MnvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTFwMEe5PEDPxE1? MW\TRW5ITVJ?
NCI-SNU-5 NXPnWZNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTNwMUK4OFEh|ryP M{Dh[3NCVkeHUh?=
BV-173 M1Xicmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nDSmlEPTB;NT60OVQxQSEQvF2= MYDTRW5ITVJ?
HCC1806 NEGzbmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrQTWM2OD13Lke1NVc{KM7:TR?= MlHYV2FPT0WU
COLO-680 M3XhUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;3doFNUUN3ME22MlIyPDB4IN88US=> M3\5VHNCVkeHUh?=
HCC2218 NIKyO3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PZeWlEPTB;Nz63PVcxPCEQvF2= MWnTRW5ITVJ?
SK-MEL-24 NY\YZ3Z7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTdwOEG5NlQh|ryP MVnTRW5ITVJ?
NCI-H720 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRThwNEO2NFMh|ryP MYPTRW5ITVJ?
KASUMI-1 Mn2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2GzU2lEPTB;OD64PVI3PiEQvF2= NEj6XoZUSU6JRWK=
HAL-01 M4HxVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;LNJdjUUN3ME25Mlg5PjJizszN MXXTRW5ITVJ?
CAL-33 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLuTWM2OD1zMD60N|Qh|ryP NV7N[nI3W0GQR1XS
SK-MEL-1 NIjkXVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYn6NIlrUUN3ME2xNk41PjZ|IN88US=> MkfLV2FPT0WU
Ramos-2G6-4C10 Mo\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnH2TWM2OD1zMj60O|UzKM7:TR?= MUnTRW5ITVJ?
KY821 MlLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfselQ6UUN3ME2xNk41QDVizszN MXHTRW5ITVJ?
HEC-1 M1;uVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTF{LkmxPVYh|ryP Mkf4V2FPT0WU
SK-NEP-1 NXLsU|hLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTF|LkG2OkDPxE1? NXfOcms1W0GQR1XS
MN-60 MmnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LqcmlEPTB;MUOuOVM5QSEQvF2= NEP1XnhUSU6JRWK=
DU-145 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;PNlZKSzVyPUGzMlkxPTNizszN MkDzV2FPT0WU
EW-3 M1TSVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHzTWM2OD1zND61OVY2KM7:TR?= Ml\LV2FPT0WU
OS-RC-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILmWVZKSzVyPUG1Mlk2QDlizszN MYjTRW5ITVJ?
RPMI-8226 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTrOZo4UUN3ME2xOk4zODR{IN88US=> NWG3e5U1W0GQR1XS
ChaGo-K-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\TZ4hKSzVyPUG2MlU{OjVizszN M3fIZnNCVkeHUh?=
DEL M33oWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\OZW5xUUN3ME2xOk43PzF5IN88US=> NVTSe4xKW0GQR1XS
GP5d MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTYNHFKSzVyPUG3MlA2OyEQvF2= MoWzV2FPT0WU
COLO-668 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTF5Lk[yPVQh|ryP NVXRR4F[W0GQR1XS
H9 M4XLZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LR[WlEPTB;MUiuNlg{OyEQvF2= NYrXZ3lyW0GQR1XS
NKM-1 M2jv[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\QcFRKSzVyPUG4MlUyOTlizszN NV7weFhqW0GQR1XS
KYSE-150 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTF6Lkm5PFYh|ryP NG\MOlNUSU6JRWK=
Daoy Ml\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTF7LkW2OFkh|ryP NVH5PIhzW0GQR1XS
ECC10 NFW3[IZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\NOmZKSzVyPUKwMlc1PTVizszN MVnTRW5ITVJ?
A388 NILLcXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDOTWM2OD1{MT65NFkyKM7:TR?= MVfTRW5ITVJ?
MHH-NB-11 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTJ|LkGzOlMh|ryP MU\TRW5ITVJ?
HCC1937 M37oNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTJ2Lke0OkDPxE1? NHe5TJVUSU6JRWK=
TGBC11TKB NIf3R|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTJ3Lk[4OlMh|ryP MoTCV2FPT0WU
CTV-1 M3v2bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnQbXQxUUN3ME2yOU45QTZ7IN88US=> M2rQXnNCVkeHUh?=
NCI-H2029 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnKyTWM2OD1{Nj60NlM5KM7:TR?= MnTBV2FPT0WU
HLE NHq5NJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTJ5LkC1OEDPxE1? MoHPV2FPT0WU
NCI-H1693 M2HmPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjVVppvUUN3ME2yO{4zQDl6IN88US=> M{LrcHNCVkeHUh?=
HCC70 NYjad2ZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonmTWM2OD1{Nz63NlQ3KM7:TR?= M2rlXXNCVkeHUh?=
BEN NHPXb2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTJ5Lkm1OlYh|ryP NE\kWGpUSU6JRWK=
LB771 M1n1[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmq4TWM2OD1{OD64N|c{KM7:TR?= MXLTRW5ITVJ?
697 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml[2TWM2OD1{OT6wNlM2KM7:TR?= NH;IcYtUSU6JRWK=
LU-139 NGHPVY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPmZ4ZKSzVyPUK5MlM4PDhizszN NFfvXZJUSU6JRWK=
EW-13 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3O0UmlEPTB;MkmuN|gyPCEQvF2= NWTQRpdDW0GQR1XS
MOLT-13 NET4OW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJ7LkO4NVQh|ryP NF;o[3ZUSU6JRWK=
L-363 M3PBVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmOzTWM2OD1{OT60O|k5KM7:TR?= MVnTRW5ITVJ?
EM-2 NHvHfnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTJ7LkS5NFEh|ryP M1rBcHNCVkeHUh?=
RS4-11 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXu1O3BwUUN3ME2zNE41OjRzIN88US=> NX3xW5B3W0GQR1XS
A2780 MnrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWr2U3ZnUUN3ME2zNE44PDV5IN88US=> MW\TRW5ITVJ?
KU812 NGf5bpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHX3XWxKSzVyPUOyMlM3PDJizszN NYrscoZlW0GQR1XS
COLO-684 NVT0XmNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTN|LkO1PVkh|ryP M3rXd3NCVkeHUh?=
MFE-280 M{XpWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXu4V5BrUUN3ME2zN{4{QDh7IN88US=> MkPzV2FPT0WU
KG-1 MojNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nqeGlEPTB;M{OuOlAxOSEQvF2= MoXDV2FPT0WU
JVM-3 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVq5[WQ1UUN3ME2zOU42QDZ6IN88US=> NWDEcIFNW0GQR1XS
MV-4-11 NVqyU4VtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYGyV5QxUUN3ME2zOU45PDl7IN88US=> M1uxfnNCVkeHUh?=
LAMA-84 NH;MV5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTN4LkezOFUh|ryP Ml7MV2FPT0WU
MOLT-16 MljFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3r6bmlEPTB;M{[uPVUzKM7:TR?= MmXZV2FPT0WU
H4 NXjLWotwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXwTWM2OD1|Nz61Olch|ryP MWjTRW5ITVJ?
T47D NVjwVmI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTN5LkewNVgh|ryP MVTTRW5ITVJ?
CAL-54 Mn\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2e2SWlEPTB;M{euPVY3KM7:TR?= MojsV2FPT0WU
SW982 MnfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmD6TWM2OD1|OD6wPVk5KM7:TR?= NV:zXm5UW0GQR1XS
IGROV-1 NIDOPGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonGTWM2OD1|OT6zN|A1KM7:TR?= NHvJUYxUSU6JRWK=
NB14 MmC5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmL4TWM2OD12MD63NFMyKM7:TR?= M2\vUHNCVkeHUh?=
HCC1187 NHHYS5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXtTlJTUUN3ME20NU4zPzdzIN88US=> MXHTRW5ITVJ?
SBC-1 NGXKflNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLETWM2OD12MT6zNFY{KM7:TR?= MnHpV2FPT0WU
KARPAS-45 MojWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHVXVhNUUN3ME20NU41QDF6IN88US=> NE\4TmtUSU6JRWK=
MOLT-4 NUfDb3RbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3PTWM2OD12Mj6yOVM5KM7:TR?= MWnTRW5ITVJ?
JVM-2 NUjWflkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTR{LkmyNFch|ryP MWfTRW5ITVJ?
A4-Fuk NYjISo84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjEbo9KSzVyPUSzMlU3QTFizszN NXT5OmpMW0GQR1XS
MDA-MB-361 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDVTWM2OD12Mz64OFE1KM7:TR?= Ml\NV2FPT0WU
BALL-1 M1q1Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTR|Lkm1N|Ih|ryP MX;TRW5ITVJ?
T98G MlHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPnT2xKSzVyPUS0Mlg2OTdizszN Mk\CV2FPT0WU
Mo-T MmqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPmNHlKSzVyPUS1MlY{QDlizszN M4PvdHNCVkeHUh?=
MHH-PREB-1 NXvHSFVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITFbotKSzVyPUS1Mlc2QDVizszN NVzpe5RRW0GQR1XS
ALL-PO NFPqdHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7LWGo3UUN3ME20O{4{PzlzIN88US=> MmKyV2FPT0WU
NCI-H510A NEHNU|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7Tb2xtUUN3ME20O{46ODN2IN88US=> NGrNWXhUSU6JRWK=
ML-2 NYXLUFFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTCdXZ6UUN3ME20PU44QDV4IN88US=> MmXWV2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo試験 The oral bioavailability of ABT-888 is 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys after oral administration. [1] ABT-888 (25 mg/kg i.p.) could improve tumor growth delay in a NCI-H460 xenograft model with well tolerated. Combination with radiation, ABT-888 decreases the tumor vessel formation. [3] ABT-888 reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg in A375 and Colo829 xenograft models and the suppression could be maintained over time. [4]
臨床試験 A Phase I study of evaluating the bioavailability and food effect of three formulations of ABT-888 on pharmacokinetics in subjects with solid tumors has been completed.
特集 Increases the efficacy of common cancer therapies such as radiation and alkylating agents.

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

In vitro PARP assays PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 μM [3H]NAD+ (1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Reactions are terminated with 1.5 mM benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter.

動物実験:

[1]

動物モデル NCI-H460, H460, B16F10 and 9L xenografts in C57BL/6 mice
製剤 Formulated in solution containing 0.9% NaCl adjusted to pH 4.0
投薬量 ~25 mg/kg
投与方法 Orally administered

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 Veliparib (ABT-888) SDF
分子量 244.29
化学式

C13H16N4O

CAS No. 912444-00-9
保管 2年-20℃
6月-80℃in solvent
別名 NSC 737664
溶解度 (25°C) * In vitro DMSO 17 mg/mL (69.58 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 0.5% methylcellulose/0.2% Tween 80 5 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 (R)-2-(2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-4-carboxamide

カスタマーフィードバック (9)


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Source , , Cancer Research, 2011, 71: 4944-4954. Veliparib (ABT-888) purchased from Selleck
Method Clonogenic Assays
Cell Lines OVCAR-8 cells
Concentrations 3 µmol/L
Incubation Time 8 d
Results A: Both PARP inhibitors markedly increased killing when cells were co-exposed to FdUrd and the PARP inhibitor for 24 h (Fig. A), followed by continuous treatment with the PARP inhibitor. B: The concentration of FdUrd that inhibited proliferation by 50% (IC50) was reduced when cells were continuously exposed to ABT-888 and ABT-888 also potentiated the effects of FdUrd in OVCAR-8. C: The data indicated strong synergistic killing over a wide range of concentrations.

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Rating
Source , , Cancer Research, 2011, 71: 4944-4954. Veliparib (ABT-888) purchased from Selleck
Method Clonogenic Assays
Cell Lines OVCAR-8 cells
Concentrations 3 µmol/L
Incubation Time 8 d
Results :We compared a series of FdUrd and ABT-888 exposure schemes (Fig. C). Modestly increased cytotoxicity was observed when OVCAR-8 cells were exposed to FdUrd and ABT-888 simultaneously for 24 h (Sequence II), compared to FdUrd alone (Sequence I)(Fig. D). Similarly, exposure to FdUrd alone for 24 h followed by continuous incubation with ABT-888 modestly increased cytotoxicity over FdUrd alone (Sequence III). In contrast, the most robust killing was seen with Sequences IV and V, in which cells were simultaneously exposed to FdUrd and ABT-888, followed by continuous ABT-888 treatment after FdUrd removal.

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Source Nucl Med Commun, 2011, 32, 1046-1051. Veliparib (ABT-888) purchased from Selleck
Method Laser confocal microscopy/fluorescent H2AX Antibody Staining
Cell Lines Epstein–Barr virus-infected Raji lymphocyte tumor cells
Concentrations 500 nM
Incubation Time 2 h
Results The Fluor-647 anti-H2A.X-phosphorylated (Ser139) antibody stained significantly more double-stranded breaks in cells treated with ABT-888 and AZD-2281 compared with controls at 8 and 12 Gy (P<0.05).

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Source Nucl Med Commun, 2011, 32(11), 1046-51. Veliparib (ABT-888) purchased from Selleck
Method Cell growth assay
Cell Lines human Burkitt lymphoma cells
Concentrations 500 nmol/l
Incubation Time 0-5 d
Results A volume of 500 nmol/l ABT-888 and AZD-2281 showed a moderate intrinsc effect on cell proliferation on days 3–5 (Fig. a). ABT-888 and AZD-2281 showed a significant ( P < 0.05) reduction in lymphoma cell growth on days 2–5 (Fig. b–d).

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Source Nucl Med Commun, 2011, 32(11), 1046-51. Veliparib (ABT-888) purchased from Selleck
Method PARP activity assay
Cell Lines Raji lymphocyte tumor cells
Concentrations 500 nmol/l
Incubation Time 24 h
Results

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Source Dr.Zhang of Tianjin Medical University. Veliparib (ABT-888) purchased from Selleck
Method Western blot
Cell Lines T47D breast cancer cells
Concentrations 0-5 μM
Incubation Time
Results

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Source David Schrmann from University of Base. Veliparib (ABT-888) 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 1-100 nM
Incubation Time 2 h
Results

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Source Dr. Steve Reuland from University of Colorado Denver. Veliparib (ABT-888) purchased from Selleck
Method MTS assay
Cell Lines 451 Lu cells
Concentrations 0-400 μM
Incubation Time 120 h
Results Treatment with 25 µM ABT-888 greatly increased sensitivity to temozolomide compared to cells without ABT-888 treatment as measured by MTS assay.

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Source Dr. Xiangbing Meng of University of Iowa. Veliparib (ABT-888) purchased from Selleck
Method WST-1 method
Cell Lines Hec50/Ishikawa/SKOV3/Caov3/PA-1 cell line
Concentrations 0-12000 nM
Incubation Time 3 d
Results ABT-888 decreased the viability of the endometrial cancer cell line Hec50 and Ishikawa and ovarian cancer cell line SKOV3,Caov3 and PA-1 in a dose-dependent manner.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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