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 M33SbGtqdmG|ZTDBd5NigQ>? NI\2OWw{OCCvaX6= M3\QSGlvcGmkaYTpc44hd2ZiUFHSVFEhf2m2aDDFR|UxKG:oIECuNFAzKM7:TR?= Ml\UNVk5QDh5NkC=
Jurkat NY\ab49UU2mwYYPlJGF{e2G7 MmrCPVYhcA>? MULEUXNQ NGq4OZNKdmirYnn0bY9vKG:oIGDBVnAyKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBk\WyuII\pZYJqdGm2eTD3bZRpKEWFNUCgc4YhOyEQvF2= MlS5NlM5PTBzOUm=
Capan1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXZO|IhcA>? M{PJ[2ROW09? NF7DN4dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGJTS0F{IHflcoUhdXW2YYTl[EBpfW2jbjDDZZBidjFiY3XscJMhf2m2aDDJR|UxKG:oIEO5Mlch|ryP MXiyOFM6QDN6Mx?=
DT40 MlXMR5l1d3SxeHnjJGF{e2G7 MXu3NkBp NYr1V5BSTE2VTx?= M2DoOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGOqaXPr[Y4hSlKFQUKt[IVncWOrZX70JGRVPDBiY3XscJM> MkDFNlQ6OjJ3OEe=
ML-1 MljTRZBweHSxdHnjJGF{e2G7 MYOyMlUh|ryP NEe0enkzPCCq MWjEUXNQ MkXnV5lv\XKpaYP0bYNidGy7IHXubIFv[2W|IGTSRWlNNWmwZIXj[YQh[XCxcITvd4l{KGmwIF3MMVEh[2WubIO= M1fmW|I1QDl3MUO1
HCT-116 MmWyT4lv[XOnIFHzd4F6 MXiwMlUh|ryP NHPESGszPCCq MXHQRXJRKGGldHn2bZR6KGSnY4LlZZNmew>? NGLuWpAzOzB3NEKxNy=>
UM-SCC1 Mk\oR5l1d3SxeHnjJGF{e2G7 M4j2fVExKM7:TR?= MmLlNlQhcA>? NGfCSlBT\WS3Y3XzJJRp\SClZXzsJJZq[WKrbHn0fS=> NXTmdFZKOjF7MUK2NlA>
FaDu Moq3R5l1d3SxeHnjJGF{e2G7 NXXkSmt1OTBizszN M1TQblI1KGh? M{Dyd3Jm\HWlZYOgeIhmKGOnbHygeoli[mmuaYT5 M2nCWVIyQTF{NkKw
PC-3 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrUNVAh|ryP Mnv6TY5lfWOnczDhJJNq\26rZnnjZY51KGmwaHnibZRqd25iaX6gZ49td267IH\vdo1ifGmxbtMg M17n[VIyPTdzOUGy
EoL-1-cell M3XMZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVOzeZF1UUN3ME2xMlA4QThizszN NFjsPGhUSU6JRWK=
NCI-SNU-5 NF;3UFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTNwMUK4OFEh|ryP Ml;yV2FPT0WU
BV-173 M{jofGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3vTVRVUUN3ME21MlQ2PDB7IN88US=> Mn;lV2FPT0WU
HCC1806 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfRTWM2OD13Lke1NVc{KM7:TR?= M4T4ZXNCVkeHUh?=
COLO-680 NH[5PIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrwSpNNUUN3ME22MlIyPDB4IN88US=> NE\wPXlUSU6JRWK=
HCC2218 MnXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjy[G5xUUN3ME23Mlc6PzB2IN88US=> Mnv6V2FPT0WU
SK-MEL-24 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDoTWM2OD15LkixPVI1KM7:TR?= NFOxXWRUSU6JRWK=
NCI-H720 MofSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRThwNEO2NFMh|ryP NWPmUlRxW0GQR1XS
KASUMI-1 M2Lxd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRThwOEmyOlYh|ryP NIXwfYdUSU6JRWK=
HAL-01 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTrZZhKSzVyPUmuPFg3OiEQvF2= MnnlV2FPT0WU
CAL-33 MmT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTFyLkSzOEDPxE1? MVLTRW5ITVJ?
SK-MEL-1 MkfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTF{LkS2OlMh|ryP NIPVUZNUSU6JRWK=
Ramos-2G6-4C10 NFG0[HVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPoc2w3UUN3ME2xNk41PzV{IN88US=> M13hb3NCVkeHUh?=
KY821 NH22dWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1znTmlEPTB;MUKuOFg2KM7:TR?= MYPTRW5ITVJ?
HEC-1 MlfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjhTWM2OD1zMj65NVk3KM7:TR?= Mn\rV2FPT0WU
SK-NEP-1 NIjUeHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2O3dWlEPTB;MUOuNVY3KM7:TR?= M1PPVnNCVkeHUh?=
MN-60 M2TGR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTF|LkWzPFkh|ryP M4LHZnNCVkeHUh?=
DU-145 NWfCT5pST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDMTWM2OD1zMz65NFU{KM7:TR?= MXzTRW5ITVJ?
EW-3 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFe0RXFKSzVyPUG0MlU2PjVizszN MUnTRW5ITVJ?
OS-RC-2 NF;l[nFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTF3Lkm1PFkh|ryP NU\abnBuW0GQR1XS
RPMI-8226 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkmzTWM2OD1zNj6yNFQzKM7:TR?= NWD5O4ltW0GQR1XS
ChaGo-K-1 MlH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvFbo5KSzVyPUG2MlU{OjVizszN M{n6[XNCVkeHUh?=
DEL NYm1R5NVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLjTWM2OD1zNj62O|E4KM7:TR?= MnXmV2FPT0WU
GP5d MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\rUGlEPTB;MUeuNFU{KM7:TR?= MVrTRW5ITVJ?
COLO-668 NXO4dpVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTF5Lk[yPVQh|ryP NXry[pNoW0GQR1XS
H9 M1LWdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3T6NWlEPTB;MUiuNlg{OyEQvF2= NITpTmZUSU6JRWK=
NKM-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrhTWM2OD1zOD61NVE6KM7:TR?= MW\TRW5ITVJ?
KYSE-150 NEX1R4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrjWnpKSzVyPUG4Mlk6QDZizszN NWfxbY5TW0GQR1XS
Daoy M2TaNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\pTWM2OD1zOT61OlQ6KM7:TR?= Ml3ZV2FPT0WU
ECC10 NVfsO4xoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoOwTWM2OD1{MD63OFU2KM7:TR?= M4TYU3NCVkeHUh?=
A388 NULXRmRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjyWYxRUUN3ME2yNU46ODlzIN88US=> MV7TRW5ITVJ?
MHH-NB-11 NV;ycmN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HJRmlEPTB;MkOuNVM3OyEQvF2= MmPoV2FPT0WU
HCC1937 MkfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37YPWlEPTB;MkSuO|Q3KM7:TR?= MkPJV2FPT0WU
TGBC11TKB MlHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nPcGlEPTB;MkWuOlg3OyEQvF2= MmnhV2FPT0WU
CTV-1 M3S5[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LNN2lEPTB;MkWuPFk3QSEQvF2= NWPT[FVTW0GQR1XS
NCI-H2029 NILzS2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLqc3FtUUN3ME2yOk41OjN6IN88US=> MkHWV2FPT0WU
HLE NXHz[3dYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrIcVZKSzVyPUK3MlA2PCEQvF2= MU\TRW5ITVJ?
NCI-H1693 M320bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXhWIFKSzVyPUK3MlI5QThizszN MkKwV2FPT0WU
HCC70 MojaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PoNWlEPTB;MkeuO|I1PiEQvF2= NG\RS2xUSU6JRWK=
BEN NVOyXmZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTicIVKSzVyPUK3Mlk2PjZizszN NF:yWI1USU6JRWK=
LB771 NVHv[mtMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUixUopvUUN3ME2yPE45Ozd|IN88US=> MUPTRW5ITVJ?
697 NVjVPJVXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PSOWlEPTB;MkmuNFI{PSEQvF2= MVzTRW5ITVJ?
LU-139 M1zRbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXJcXB[UUN3ME2yPU4{PzR6IN88US=> NWrMUmNIW0GQR1XS
EW-13 MmDZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTJ7LkO4NVQh|ryP NWXieYF{W0GQR1XS
MOLT-13 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\pcYpKSzVyPUK5MlM5OTRizszN NFLtVJpUSU6JRWK=
L-363 M1nBSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmi1TWM2OD1{OT60O|k5KM7:TR?= NYPJNIpWW0GQR1XS
EM-2 Mlr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTJ7LkS5NFEh|ryP NVHxR5JuW0GQR1XS
RS4-11 Mn;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HmT2lEPTB;M{CuOFI1OSEQvF2= MnvKV2FPT0WU
A2780 M1vRWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLncIlKSzVyPUOwMlc1PTdizszN NGPqbmFUSU6JRWK=
KU812 NEXLUGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfVe4NlUUN3ME2zNk4{PjR{IN88US=> NIf2UlBUSU6JRWK=
COLO-684 MkfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTN|LkO1PVkh|ryP MVfTRW5ITVJ?
MFE-280 NFTSd2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rNSmlEPTB;M{OuN|g5QSEQvF2= NFXFfFZUSU6JRWK=
KG-1 M1jFOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LrZWlEPTB;M{OuOlAxOSEQvF2= NVPqXm4{W0GQR1XS
JVM-3 NHrSS3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFW0NI5KSzVyPUO1MlU5PjhizszN NHT2WXVUSU6JRWK=
MV-4-11 NXXCNGV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTN3Lki0PVkh|ryP MmLIV2FPT0WU
LAMA-84 MoXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDSWo5KSzVyPUO2Mlc{PDVizszN M13DbXNCVkeHUh?=
MOLT-16 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTN4Lkm1NkDPxE1? M4TXb3NCVkeHUh?=
H4 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzxSGlQUUN3ME2zO{42PjdizszN NHjp[INUSU6JRWK=
T47D M{nYb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGH1dXpKSzVyPUO3MlcxOThizszN M1HuTXNCVkeHUh?=
CAL-54 NFX4RmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDr[YtKSzVyPUO3Mlk3PiEQvF2= MVLTRW5ITVJ?
SW982 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHJTWM2OD1|OD6wPVk5KM7:TR?= NHnhTnhUSU6JRWK=
IGROV-1 M{TIR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTN7LkOzNFQh|ryP NXey[5FTW0GQR1XS
NB14 M32xfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XoOWlEPTB;NECuO|A{OSEQvF2= MYDTRW5ITVJ?
HCC1187 NGHQRYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXUZXdnUUN3ME20NU4zPzdzIN88US=> NYLVfYZtW0GQR1XS
SBC-1 MmTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LnN2lEPTB;NEGuN|A3OyEQvF2= MYjTRW5ITVJ?
KARPAS-45 M1;zXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLCTWM2OD12MT60PFE5KM7:TR?= MmPyV2FPT0WU
MOLT-4 MnrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3DTWM2OD12Mj6yOVM5KM7:TR?= MYXTRW5ITVJ?
JVM-2 NVXZeWhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPxOVU4UUN3ME20Nk46OjB5IN88US=> MXfTRW5ITVJ?
A4-Fuk M{\RRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF:5VYZKSzVyPUSzMlU3QTFizszN NGnHNW1USU6JRWK=
MDA-MB-361 M4\nRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTyTWM2OD12Mz64OFE1KM7:TR?= NXnZPWo2W0GQR1XS
BALL-1 MkXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPhOoV7UUN3ME20N{46PTN{IN88US=> NU[5TZpqW0GQR1XS
T98G MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTR2Lki1NVch|ryP MoD3V2FPT0WU
Mo-T MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfVTWM2OD12NT62N|g6KM7:TR?= Mk\MV2FPT0WU
MHH-PREB-1 NEjGW4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTR3Lke1PFUh|ryP M2HVN3NCVkeHUh?=
ALL-PO NV;qUHR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHWxeY9KSzVyPUS3MlM4QTFizszN NX;k[5I1W0GQR1XS
NCI-H510A NXHpN5RMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnG3TWM2OD12Nz65NFM1KM7:TR?= NIfGT21USU6JRWK=
ML-2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\pVGlEPTB;NEmuO|g2PiEQvF2= NXPTXWZoW0GQR1XS

... 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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Rating
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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