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 Mn;OT4lv[XOnIFHzd4F6 NIL2fFI{OCCvaX6= M3\hUGlvcGmkaYTpc44hd2ZiUFHSVFEhf2m2aDDFR|UxKG:oIECuNFAzKM7:TR?= NXPCXW9GOTl6OEi3OlA>
Jurkat NVnZNmdYU2mwYYPlJGF{e2G7 MV:5OkBp MmrHSG1UVw>? M4LqN2lvcGmkaYTpc44hd2ZiUFHSVFEh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJINmdGxidnnhZoltcXS7IIfpeIghTUN3MDDv[kA{KM7:TR?= MUiyN|g2ODF7OR?=
Capan1 Moi4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfaeVJnPzJiaB?= NIfPNGpFVVOR NXPRfHBvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBDWkODMjDn[Y5mKG23dHH0[YQhcHWvYX6gR4Fx[W5zIHPlcIx{KHerdHigTWM2OCCxZjCzPU44KM7:TR?= MVmyOFM6QDN6Mx?=
DT40 MXnDfZRwfG:6aXOgRZN{[Xl? M3y3SFczKGh? NEDUXWpFVVOR MoLhR5l1d3SxeHnjbZR6KGGpYXnud5Qh[2irY3vlckBDWkODMj3k[YZq[2mnboSgSHQ1OCClZXzsdy=> M1:yXVI1QTJ{NUi3
ML-1 NWPlc|RvSXCxcITveIlkKEG|c3H5 NXjRPJBoOi53IN88US=> MlrvNlQhcA>? MYHEUXNQ NFzxeW5UgW6ncnfpd5Rq[2GubImg[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXNiaX6gUWwuOSClZXzsdy=> M3\pbVI1QDl3MUO1
HCT-116 M{DVcGtqdmG|ZTDBd5NigQ>? M{XDSFAvPSEQvF2= MnjmNlQhcA>? NHnZOoRRSVKSIHHjeIl3cXS7IHTlZ5Jm[XOncx?= MX6yN|A2PDJzMx?=
UM-SCC1 M13MfGN6fG:2b4jpZ{BCe3OjeR?= NVfKUG1JOTBizszN MYGyOEBp NYnt[GJ6WmWmdXPld{B1cGViY3XscEB3cWGkaXzpeJk> M3PCN|IyQTF{NkKw
FaDu MnK4R5l1d3SxeHnjJGF{e2G7 MXuxNEDPxE1? NWjX[lg{OjRiaB?= NIC0To9T\WS3Y3XzJJRp\SClZXzsJJZq[WKrbHn0fS=> NVrISYd5OjF7MUK2NlA>
PC-3 MkLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jIZVExKM7:TR?= MmXaTY5lfWOnczDhJJNq\26rZnnjZY51KGmwaHnibZRqd25iaX6gZ49td267IH\vdo1ifGmxbtMg NHT0PFUzOTV5MUmxNi=>
EoL-1-cell Mn21S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nTfmlEPTB;MT6wO|k5KM7:TR?= NUnpN45XW0GQR1XS
NCI-SNU-5 NXTQfJczT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fMZmlEPTB;Mz6xNlg1OSEQvF2= Mli0V2FPT0WU
BV-173 M3TQUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXT6UG53UUN3ME21MlQ2PDB7IN88US=> NUfIO3F3W0GQR1XS
HCC1806 NWjaS3lZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLzTWM2OD13Lke1NVc{KM7:TR?= M330XXNCVkeHUh?=
COLO-680 M4q2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjUTWM2OD14LkKxOFA3KM7:TR?= NFuwbXlUSU6JRWK=
HCC2218 MmLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PLb2lEPTB;Nz63PVcxPCEQvF2= MVXTRW5ITVJ?
SK-MEL-24 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7uVpJsUUN3ME23MlgyQTJ2IN88US=> MUDTRW5ITVJ?
NCI-H720 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVGzUYxGUUN3ME24MlQ{PjB|IN88US=> NFvCcm5USU6JRWK=
KASUMI-1 NGDkNFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRThwOEmyOlYh|ryP NXXXUoc2W0GQR1XS
HAL-01 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXIVpFpUUN3ME25Mlg5PjJizszN M3\TVnNCVkeHUh?=
CAL-33 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jLT2lEPTB;MUCuOFM1KM7:TR?= MkXOV2FPT0WU
SK-MEL-1 NEf4b|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NECxTGhKSzVyPUGyMlQ3PjNizszN MkjFV2FPT0WU
Ramos-2G6-4C10 Mnj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETaV2NKSzVyPUGyMlQ4PTJizszN M4qwT3NCVkeHUh?=
KY821 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHW1T|FKSzVyPUGyMlQ5PSEQvF2= MWLTRW5ITVJ?
HEC-1 NEnZeGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHUTWM2OD1zMj65NVk3KM7:TR?= MmLuV2FPT0WU
SK-NEP-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXLTWM2OD1zMz6xOlYh|ryP NXfRWJpPW0GQR1XS
MN-60 NVXWTWF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPLTWM2OD1zMz61N|g6KM7:TR?= MYDTRW5ITVJ?
DU-145 NVX1TlZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkOyTWM2OD1zMz65NFU{KM7:TR?= NX\qTlRlW0GQR1XS
EW-3 NYrwUY9XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\VeY41UUN3ME2xOE42PTZ3IN88US=> M4[4bHNCVkeHUh?=
OS-RC-2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTF3Lkm1PFkh|ryP NX7nUY1CW0GQR1XS
RPMI-8226 NX;FOlQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHFTWM2OD1zNj6yNFQzKM7:TR?= MXTTRW5ITVJ?
ChaGo-K-1 NXXzeFlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;YZWlEPTB;MU[uOVMzPSEQvF2= M17ZVnNCVkeHUh?=
DEL MmPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEL5bmxKSzVyPUG2MlY4OTdizszN NGHnZppUSU6JRWK=
GP5d MoTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TkS2lEPTB;MUeuNFU{KM7:TR?= MX\TRW5ITVJ?
COLO-668 M4DWZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDCTWM2OD1zNz62Nlk1KM7:TR?= M3LWTnNCVkeHUh?=
H9 NXi1OW94T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnYZ|JKSzVyPUG4MlI5OzNizszN NFLsbHdUSU6JRWK=
NKM-1 M4H0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXZTWM2OD1zOD61NVE6KM7:TR?= MYHTRW5ITVJ?
KYSE-150 NUDEUIY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkOxTWM2OD1zOD65PVg3KM7:TR?= NXe0eYFJW0GQR1XS
Daoy NVH5fFB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\YWmlEPTB;MUmuOVY1QSEQvF2= Mny0V2FPT0WU
ECC10 NYTReJVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFftTZpKSzVyPUKwMlc1PTVizszN NI\GOphUSU6JRWK=
A388 M1K4Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrmWGJmUUN3ME2yNU46ODlzIN88US=> M4fBbHNCVkeHUh?=
MHH-NB-11 Mn3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTJ|LkGzOlMh|ryP NHXQNGVUSU6JRWK=
HCC1937 M3PRUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTJ2Lke0OkDPxE1? M{TjU3NCVkeHUh?=
TGBC11TKB MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJ3Lk[4OlMh|ryP NH7VcldUSU6JRWK=
CTV-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPLWphkUUN3ME2yOU45QTZ7IN88US=> MXrTRW5ITVJ?
NCI-H2029 M{jnOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTJ4LkSyN|gh|ryP NXHoN5pOW0GQR1XS
HLE NVixXG5UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7QNG9KSzVyPUK3MlA2PCEQvF2= NXnvdYRZW0GQR1XS
NCI-H1693 NF3KToJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTJ5LkK4PVgh|ryP MonUV2FPT0WU
HCC70 M2np[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTJ5LkeyOFYh|ryP Mk\MV2FPT0WU
BEN NX;4VmZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DWbmlEPTB;MkeuPVU3PiEQvF2= NVPJOVZ2W0GQR1XS
LB771 M4W3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nXPWlEPTB;MkiuPFM4OyEQvF2= NF7ZSXBUSU6JRWK=
697 NVfuO3FQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1T3c2lEPTB;MkmuNFI{PSEQvF2= MVHTRW5ITVJ?
LU-139 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlOxTWM2OD1{OT6zO|Q5KM7:TR?= NIHQbI9USU6JRWK=
EW-13 M1O1emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV20N4piUUN3ME2yPU4{QDF2IN88US=> MVnTRW5ITVJ?
MOLT-13 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTJ7LkO4NVQh|ryP MXXTRW5ITVJ?
L-363 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fse2lEPTB;MkmuOFc6QCEQvF2= M3\3VnNCVkeHUh?=
EM-2 NXO0eINST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmP2TWM2OD1{OT60PVAyKM7:TR?= M{HMeHNCVkeHUh?=
RS4-11 NHTrV4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTNyLkSyOFEh|ryP M3XyOHNCVkeHUh?=
A2780 MkLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7aSINKSzVyPUOwMlc1PTdizszN MlH1V2FPT0WU
KU812 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rh[mlEPTB;M{KuN|Y1OiEQvF2= NVnKSlE{W0GQR1XS
COLO-684 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHINFlKSzVyPUOzMlM2QTlizszN M4TndnNCVkeHUh?=
MFE-280 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\zUWlEPTB;M{OuN|g5QSEQvF2= NWjXNlQzW0GQR1XS
KG-1 MoHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTDZVhKUUN3ME2zN{43ODBzIN88US=> MVzTRW5ITVJ?
JVM-3 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDNTWM2OD1|NT61PFY5KM7:TR?= NXLQdVNRW0GQR1XS
MV-4-11 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LETWlEPTB;M{WuPFQ6QSEQvF2= NEP0Z2JUSU6JRWK=
LAMA-84 NF3ER2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTN4LkezOFUh|ryP M{m5[HNCVkeHUh?=
MOLT-16 MlHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7ZTWM2OD1|Nj65OVIh|ryP NV\zdXh6W0GQR1XS
H4 MoXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrOTWM2OD1|Nz61Olch|ryP MmH6V2FPT0WU
T47D MoXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTN5LkewNVgh|ryP Mo\FV2FPT0WU
CAL-54 NVLwWpBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfUeo5KSzVyPUO3Mlk3PiEQvF2= M{HmTXNCVkeHUh?=
SW982 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnkTWM2OD1|OD6wPVk5KM7:TR?= NFvXdo9USU6JRWK=
IGROV-1 M1TZTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HFRWlEPTB;M{muN|MxPCEQvF2= MXXTRW5ITVJ?
NB14 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2T3WGlEPTB;NECuO|A{OSEQvF2= M{fqZXNCVkeHUh?=
HCC1187 NGj0RYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTRzLkK3O|Eh|ryP MkLkV2FPT0WU
SBC-1 NIH2SG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\KTWM2OD12MT6zNFY{KM7:TR?= NXjYZ4JQW0GQR1XS
KARPAS-45 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\vS5RKSzVyPUSxMlQ5OThizszN MlHXV2FPT0WU
MOLT-4 Mo\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTR{LkK1N|gh|ryP NYfncW86W0GQR1XS
JVM-2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHDSIhNUUN3ME20Nk46OjB5IN88US=> M3vW[XNCVkeHUh?=
A4-Fuk MoPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPyUJVKSzVyPUSzMlU3QTFizszN NWLxdZFUW0GQR1XS
MDA-MB-361 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MomxTWM2OD12Mz64OFE1KM7:TR?= MULTRW5ITVJ?
BALL-1 NYS5ZmU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXn6TpVvUUN3ME20N{46PTN{IN88US=> M3q2dXNCVkeHUh?=
T98G M4fGPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTQU4NKSzVyPUS0Mlg2OTdizszN MoPJV2FPT0WU
Mo-T MlfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mme2TWM2OD12NT62N|g6KM7:TR?= NF3ET3VUSU6JRWK=
MHH-PREB-1 NIG2fFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zrV2lEPTB;NEWuO|U5PSEQvF2= NH7r[|NUSU6JRWK=
ALL-PO MnfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXroUmZFUUN3ME20O{4{PzlzIN88US=> MmTQV2FPT0WU
NCI-H510A Moq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX2xTmRxUUN3ME20O{46ODN2IN88US=> M1ezdXNCVkeHUh?=
ML-2 M{\Oe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nSd2lEPTB;NEmuO|g2PiEQvF2= MUDTRW5ITVJ?

... 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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