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 M3f3W2tqdmG|ZTDBd5NigQ>? NIXTcGo{OCCvaX6= NFnTXXhKdmirYnn0bY9vKG:oIGDBVnAyKHerdHigSWM2OCCxZjCwMlAxOiEQvF2= MlW4NVk5QDh5NkC=
Jurkat NVztXJdUU2mwYYPlJGF{e2G7 NYGzTJVsQTZiaB?= NV[wOoh{TE2VTx?= MXfJcohq[mm2aX;uJI9nKFCDUmCxJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDj[YxtKH[rYXLpcIl1gSC5aYToJGVEPTBib3[gN{DPxE1? MWKyN|g2ODF7OR?=
Capan1 MlywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX23NkBp MYrEUXNQ NIXjS5hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGJTS0F{IHflcoUhdXW2YYTl[EBpfW2jbjDDZZBidjFiY3XscJMhf2m2aDDJR|UxKG:oIEO5Mlch|ryP MV6yOFM6QDN6Mx?=
DT40 MoWzR5l1d3SxeHnjJGF{e2G7 Mn7NO|IhcA>? NXvvPWhnTE2VTx?= NVTUdWtHS3m2b4TvfIlkcXS7IHHnZYlve3RiY3jpZ4tmdiCEUlPBNk1l\W[rY3nlcpQhTFR2MDDj[Yxtew>? NIDaT|czPDl{MkW4Oy=>
ML-1 MV7BdI9xfG:2aXOgRZN{[Xl? MVyyMlUh|ryP NI[3TGczPCCq NUHHWoxUTE2VTx?= M2nOU3N6dmW{Z3nzeIlk[WyueTDlcohidmOnczDUVmFKVC2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDNUE0yKGOnbHzz NIfkZlAzPDh7NUGzOS=>
HCT-116 MnjIT4lv[XOnIFHzd4F6 MV2wMlUh|ryP MVOyOEBp NUXFSFVFWEGUUDDhZ5Rqfmm2eTDk[YNz\WG|ZYO= MVyyN|A2PDJzMx?=
UM-SCC1 NYXodZlbS3m2b4TvfIlkKEG|c3H5 NWPuN|NUOTBizszN NGfNRpUzPCCq NFvvS4RT\WS3Y3XzJJRp\SClZXzsJJZq[WKrbHn0fS=> NGn0UIozOTlzMk[yNC=>
FaDu NEDvR4tEgXSxdH;4bYMhSXO|YYm= MV6xNEDPxE1? MkfUNlQhcA>? MlzyVoVlfWOnczD0bIUh[2WubDD2bYFjcWyrdIm= M37aXlIyQTF{NkKw
PC-3 Mn;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3tNVAh|ryP M3zHVGlv\HWlZYOgZUB{cWewaX\pZ4FvfCCrbnjpZol1cW:wIHnuJINwdG:weTDmc5Ju[XSrb39CpC=> NG\qVJYzOTV5MUmxNi=>
EoL-1-cell MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nMZWlEPTB;MT6wO|k5KM7:TR?= NGfJ[5RUSU6JRWK=
NCI-SNU-5 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vEVmlEPTB;Mz6xNlg1OSEQvF2= MUfTRW5ITVJ?
BV-173 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\oTWM2OD13LkS1OFA6KM7:TR?= M4r4[HNCVkeHUh?=
HCC1806 NHXvR4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkX3TWM2OD13Lke1NVc{KM7:TR?= MVTTRW5ITVJ?
COLO-680 Ml2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTZwMkG0NFYh|ryP NGfSdIZUSU6JRWK=
HCC2218 NUnvZo46T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTdwN{m3NFQh|ryP MX\TRW5ITVJ?
SK-MEL-24 M3TDVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYOwVWtDUUN3ME23MlgyQTJ2IN88US=> NIXncnlUSU6JRWK=
NCI-H720 Mo[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\OeJUxUUN3ME24MlQ{PjB|IN88US=> NYD2[pJRW0GQR1XS
KASUMI-1 MnPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkC5TWM2OD16Lki5NlY3KM7:TR?= NXTPOWh1W0GQR1XS
HAL-01 MlLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLvTWM2OD17Lki4OlIh|ryP M3PMVXNCVkeHUh?=
CAL-33 M{XEXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXLTWM2OD1zMD60N|Qh|ryP NH\XTY5USU6JRWK=
SK-MEL-1 NIrsW|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3O5S2lEPTB;MUKuOFY3OyEQvF2= NFrGRWlUSU6JRWK=
Ramos-2G6-4C10 MoKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGmybZhKSzVyPUGyMlQ4PTJizszN MYjTRW5ITVJ?
KY821 M4GwOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWftcowzUUN3ME2xNk41QDVizszN MYrTRW5ITVJ?
HEC-1 NXzRNmszT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fJU2lEPTB;MUKuPVE6PiEQvF2= MVTTRW5ITVJ?
SK-NEP-1 M13mbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHNZ3FKSzVyPUGzMlE3PiEQvF2= MY\TRW5ITVJ?
MN-60 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrPXVNwUUN3ME2xN{42Ozh7IN88US=> NF;jbVRUSU6JRWK=
DU-145 NGDRUVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHe1U2JKSzVyPUGzMlkxPTNizszN M2PKZ3NCVkeHUh?=
EW-3 M2jTW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTF2LkW1OlUh|ryP MX3TRW5ITVJ?
OS-RC-2 M2PMNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{H0NmlEPTB;MUWuPVU5QSEQvF2= NGrHUlVUSU6JRWK=
RPMI-8226 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTF4LkKwOFIh|ryP M2XJZXNCVkeHUh?=
ChaGo-K-1 M2e2c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\PNY5KSzVyPUG2MlU{OjVizszN M2\FdXNCVkeHUh?=
DEL NUfMPHdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fFVGlEPTB;MU[uOlcyPyEQvF2= MUPTRW5ITVJ?
GP5d M2j6[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\SdJUyUUN3ME2xO{4xPTNizszN NHfkeppUSU6JRWK=
COLO-668 MnjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\VNmlEPTB;MUeuOlI6PCEQvF2= MXPTRW5ITVJ?
H9 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4W3XWlEPTB;MUiuNlg{OyEQvF2= Mm\nV2FPT0WU
NKM-1 NXPpeVM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3t[HUxUUN3ME2xPE42OTF7IN88US=> M2GxfXNCVkeHUh?=
KYSE-150 M{Py[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnFfYpDUUN3ME2xPE46QTh4IN88US=> MlX1V2FPT0WU
Daoy NEPqZ2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlfFTWM2OD1zOT61OlQ6KM7:TR?= M4TCNXNCVkeHUh?=
ECC10 NGDiZmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrKS|dKSzVyPUKwMlc1PTVizszN MnzQV2FPT0WU
A388 NGXtUYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJzLkmwPVEh|ryP M1\KZXNCVkeHUh?=
MHH-NB-11 Mk\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlP3TWM2OD1{Mz6xN|Y{KM7:TR?= M1HYN3NCVkeHUh?=
HCC1937 NH7BenVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3vS5V6UUN3ME2yOE44PDZizszN M3G5XHNCVkeHUh?=
TGBC11TKB NHHnVFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfo[G9NUUN3ME2yOU43QDZ|IN88US=> NWrJUGhJW0GQR1XS
CTV-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moj0TWM2OD1{NT64PVY6KM7:TR?= MlfKV2FPT0WU
NCI-H2029 M1zWPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJ4LkSyN|gh|ryP MUHTRW5ITVJ?
HLE NHLFW5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJ5LkC1OEDPxE1? MmfGV2FPT0WU
NCI-H1693 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvIVmxKSzVyPUK3MlI5QThizszN MoDyV2FPT0WU
HCC70 NInKUJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTZT4R{UUN3ME2yO{44OjR4IN88US=> Mm\6V2FPT0WU
BEN MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LJeGlEPTB;MkeuPVU3PiEQvF2= M3vGNXNCVkeHUh?=
LB771 NIT6SXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTJ6LkizO|Mh|ryP NFT1PIRUSU6JRWK=
697 NFG3N3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XHTWlEPTB;MkmuNFI{PSEQvF2= MoX2V2FPT0WU
LU-139 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXmXoxUUUN3ME2yPU4{PzR6IN88US=> NFe1OXBUSU6JRWK=
EW-13 M{fCW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIW4NGtKSzVyPUK5MlM5OTRizszN MX\TRW5ITVJ?
MOLT-13 NWfTOYtWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3W4WWlEPTB;MkmuN|gyPCEQvF2= MUDTRW5ITVJ?
L-363 NVe5eVVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\jNmhKSzVyPUK5MlQ4QThizszN MkHEV2FPT0WU
EM-2 NHvRN2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PWPWlEPTB;MkmuOFkxOSEQvF2= M{XsbnNCVkeHUh?=
RS4-11 M3[2XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;EbmlEPTB;M{CuOFI1OSEQvF2= M3rJS3NCVkeHUh?=
A2780 NHP0cW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1z6eGlEPTB;M{CuO|Q2PyEQvF2= M2TZ[nNCVkeHUh?=
KU812 NW[0VnBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\zSFFKSzVyPUOyMlM3PDJizszN NWjtcFZZW0GQR1XS
COLO-684 NUL0U2VTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2n3cWlEPTB;M{OuN|U6QSEQvF2= NHHvTlZUSU6JRWK=
MFE-280 NGS4eZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknhTWM2OD1|Mz6zPFg6KM7:TR?= NXfzbWo1W0GQR1XS
KG-1 MnzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fqfWlEPTB;M{OuOlAxOSEQvF2= M4Gye3NCVkeHUh?=
JVM-3 NGPMN2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorQTWM2OD1|NT61PFY5KM7:TR?= MkHsV2FPT0WU
MV-4-11 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjhRpoxUUN3ME2zOU45PDl7IN88US=> NXuySpJ[W0GQR1XS
LAMA-84 M4f6SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTCSoJHUUN3ME2zOk44OzR3IN88US=> M1rHdnNCVkeHUh?=
MOLT-16 M{LZUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HPdWlEPTB;M{[uPVUzKM7:TR?= MYDTRW5ITVJ?
H4 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HZbGlEPTB;M{euOVY4KM7:TR?= NX\JW4dzW0GQR1XS
T47D MkGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\ZdJNQUUN3ME2zO{44ODF6IN88US=> NUf5XWZpW0GQR1XS
CAL-54 NF76XFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTN5Lkm2OkDPxE1? MVnTRW5ITVJ?
SW982 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3PTWM2OD1|OD6wPVk5KM7:TR?= NFrpRnVUSU6JRWK=
IGROV-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYexcpU2UUN3ME2zPU4{OzB2IN88US=> M{\yVHNCVkeHUh?=
NB14 NGW4ZYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTGTWM2OD12MD63NFMyKM7:TR?= MYfTRW5ITVJ?
HCC1187 NVjRbllwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\4UGlEPTB;NEGuNlc4OSEQvF2= MV7TRW5ITVJ?
SBC-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{P2emlEPTB;NEGuN|A3OyEQvF2= M3vnRnNCVkeHUh?=
KARPAS-45 M2PMR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIG4WoZKSzVyPUSxMlQ5OThizszN Ml\kV2FPT0WU
MOLT-4 NX65UYQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHPTWM2OD12Mj6yOVM5KM7:TR?= NFHFOVVUSU6JRWK=
JVM-2 NH3PVIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTR{LkmyNFch|ryP NWPFXYMxW0GQR1XS
A4-Fuk MnrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7UT29KSzVyPUSzMlU3QTFizszN MUXTRW5ITVJ?
MDA-MB-361 NV\3OY1NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTR|Lki0NVQh|ryP NV31U3Q6W0GQR1XS
BALL-1 M{T0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTR|Lkm1N|Ih|ryP NFrxXo1USU6JRWK=
T98G MnezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTR2Lki1NVch|ryP NXPzRop2W0GQR1XS
Mo-T Mn7nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXTSHNKSzVyPUS1MlY{QDlizszN NXjvRVVPW0GQR1XS
MHH-PREB-1 NVHhXY41T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTR3Lke1PFUh|ryP MWrTRW5ITVJ?
ALL-PO M2rnV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITlUHNKSzVyPUS3MlM4QTFizszN NVrvVHM3W0GQR1XS
NCI-H510A MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTR5LkmwN|Qh|ryP NVztOndkW0GQR1XS
ML-2 M{XXdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX20cJhMUUN3ME20PU44QDV4IN88US=> MYTTRW5ITVJ?

... 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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Rating
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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