Veliparib (ABT-888) 化学構造
分子量: 244.29

高品質保証

文献中の引用(38)

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 NFfhNoZMcW6jc3WgRZN{[Xl? MmC1N|AhdWmw MYjJcohq[mm2aX;uJI9nKFCDUmCxJJdqfGhiRVO1NEBw\iByLkCwNkDPxE1? MnPlNVk5QDh5NkC=
Jurkat NXrpR2o2U2mwYYPlJGF{e2G7 NWfoOHJqQTZiaB?= MXPEUXNQ NIm4XW5KdmirYnn0bY9vKG:oIGDBVnAyKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBk\WyuII\pZYJqdGm2eTD3bZRpKEWFNUCgc4YhOyEQvF2= NIrVZ4EzOzh3MEG5PS=>
Capan1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm[zO|IhcA>? NWj4TYZJTE2VTx?= M3O2U2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRnJESTJiZ3Xu[UBufXSjdHXkJIh2dWGwIFPhdIFvOSClZXzsd{B4cXSqIFnDOVAhd2ZiM{muO{DPxE1? M{LtUFI1Ozl6M{iz
DT40 M17DfGN6fG:2b4jpZ{BCe3OjeR?= NFz3d4I4OiCq M3O4emROW09? MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBkcGmla3XuJGJTS0F{LXTl[olkcWWwdDDEWFQxKGOnbHzz MkfqNlQ6OjJ3OEe=
ML-1 NVfTZ|ZsSXCxcITveIlkKEG|c3H5 NXqyVGFCOi53IN88US=> NUPic2NiOjRiaB?= NUDZUpZ7TE2VTx?= NFvNUXNUgW6ncnfpd5Rq[2GubImg[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXNiaX6gUWwuOSClZXzsdy=> MV:yOFg6PTF|NR?=
HCT-116 NHP5UWxMcW6jc3WgRZN{[Xl? NXvhN|NbOC53IN88US=> NXrnOottOjRiaB?= MYLQRXJRKGGldHn2bZR6KGSnY4LlZZNmew>? MVOyN|A2PDJzMx?=
UM-SCC1 NVTIc3pQS3m2b4TvfIlkKEG|c3H5 NUn1VHl2OTBizszN MoPjNlQhcA>? M13sPXJm\HWlZYOgeIhmKGOnbHygeoli[mmuaYT5 NVzheYE4OjF7MUK2NlA>
FaDu NHnIdWZEgXSxdH;4bYMhSXO|YYm= MlLtNVAh|ryP MVeyOEBp NF7jZ5ZT\WS3Y3XzJJRp\SClZXzsJJZq[WKrbHn0fS=> NWPnSWpiOjF7MUK2NlA>
PC-3 NH3jfYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYr5[YdbOTBizszN MnTVTY5lfWOnczDhJJNq\26rZnnjZY51KGmwaHnibZRqd25iaX6gZ49td267IH\vdo1ifGmxbtMg NXvGS2lYOjF3N{G5NVI>
EoL-1-cell NYX2d4NLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3GTWM2OD1zLkC3PVgh|ryP Ml31V2FPT0WU
NCI-SNU-5 NHKzOIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jW[GlEPTB;Mz6xNlg1OSEQvF2= NXzsSHpLW0GQR1XS
BV-173 NEX1b3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnGOXpMUUN3ME21MlQ2PDB7IN88US=> M4[0fXNCVkeHUh?=
HCC1806 Ml7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTVwN{WxO|Mh|ryP M1PSN3NCVkeHUh?=
COLO-680 M2LKOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTZwMkG0NFYh|ryP MojGV2FPT0WU
HCC2218 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlSyTWM2OD15Lke5O|A1KM7:TR?= NInPPZdUSU6JRWK=
SK-MEL-24 MlOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXZWXhKSzVyPUeuPFE6OjRizszN MkfLV2FPT0WU
NCI-H720 M2T3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXIXXVKSzVyPUiuOFM3ODNizszN MWPTRW5ITVJ?
KASUMI-1 NHfUOnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkT5TWM2OD16Lki5NlY3KM7:TR?= MUXTRW5ITVJ?
HAL-01 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIO4bWFKSzVyPUmuPFg3OiEQvF2= M1nIXXNCVkeHUh?=
CAL-33 M4naeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzPTWM2OD1zMD60N|Qh|ryP MVXTRW5ITVJ?
SK-MEL-1 NIXMTo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnv0TWM2OD1zMj60OlY{KM7:TR?= NVzuXVJ6W0GQR1XS
Ramos-2G6-4C10 NV;icWJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTF{LkS3OVIh|ryP MkDvV2FPT0WU
KY821 NHHEW3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PhT2lEPTB;MUKuOFg2KM7:TR?= MnPqV2FPT0WU
HEC-1 MnrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTF{LkmxPVYh|ryP NGLEXWxUSU6JRWK=
SK-NEP-1 MkPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;HeVlnUUN3ME2xN{4yPjZizszN MnHTV2FPT0WU
MN-60 NYO1WlFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmm5TWM2OD1zMz61N|g6KM7:TR?= NGjyUXlUSU6JRWK=
DU-145 NGH1U3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmO3TWM2OD1zMz65NFU{KM7:TR?= MYrTRW5ITVJ?
EW-3 MnnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfnSYV2UUN3ME2xOE42PTZ3IN88US=> NH3TclFUSU6JRWK=
OS-RC-2 NFf1Z4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrlN3JKSzVyPUG1Mlk2QDlizszN MnLvV2FPT0WU
RPMI-8226 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLnPYFHUUN3ME2xOk4zODR{IN88US=> NFfrN3FUSU6JRWK=
ChaGo-K-1 NHXIOWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3mTWM2OD1zNj61N|I2KM7:TR?= NUnrUVlsW0GQR1XS
DEL M2rKTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLKNpl3UUN3ME2xOk43PzF5IN88US=> NFPkU5lUSU6JRWK=
GP5d M1LwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fCcGlEPTB;MUeuNFU{KM7:TR?= M2fi[3NCVkeHUh?=
COLO-668 NFPUXoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{m0fmlEPTB;MUeuOlI6PCEQvF2= M3jId3NCVkeHUh?=
H9 NF7RR|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkK5TWM2OD1zOD6yPFM{KM7:TR?= MmPrV2FPT0WU
NKM-1 NHOxU4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\FV4FKSzVyPUG4MlUyOTlizszN NXLIOFhoW0GQR1XS
KYSE-150 MkniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DaSWlEPTB;MUiuPVk5PiEQvF2= MoC4V2FPT0WU
Daoy MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTF7LkW2OFkh|ryP NGnkfmVUSU6JRWK=
ECC10 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nhfWlEPTB;MkCuO|Q2PSEQvF2= MXjTRW5ITVJ?
A388 M2K2Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV64dWE3UUN3ME2yNU46ODlzIN88US=> NFi3THpUSU6JRWK=
MHH-NB-11 M1zadmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPwd25mUUN3ME2yN{4yOzZ|IN88US=> MlznV2FPT0WU
HCC1937 NHvLPJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rQbmlEPTB;MkSuO|Q3KM7:TR?= NX\jW2RJW0GQR1XS
TGBC11TKB M4nnVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPYTWM2OD1{NT62PFY{KM7:TR?= MmfxV2FPT0WU
CTV-1 MlHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkj5TWM2OD1{NT64PVY6KM7:TR?= MVrTRW5ITVJ?
NCI-H2029 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPv[odJUUN3ME2yOk41OjN6IN88US=> NG\UVmhUSU6JRWK=
HLE NI\x[mtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTJ5LkC1OEDPxE1? MlO2V2FPT0WU
NCI-H1693 Mmr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnLdXJKSzVyPUK3MlI5QThizszN NWG4VHg5W0GQR1XS
HCC70 M1;TTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlztTWM2OD1{Nz63NlQ3KM7:TR?= NIDnfIVUSU6JRWK=
BEN M4jCcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3XSYFKSzVyPUK3Mlk2PjZizszN MmrLV2FPT0WU
LB771 M4[yT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTJ6LkizO|Mh|ryP NInaUndUSU6JRWK=
697 NWTHRlFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjjd|BrUUN3ME2yPU4xOjN3IN88US=> NX3pcGtGW0GQR1XS
LU-139 MlywS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXSTWM2OD1{OT6zO|Q5KM7:TR?= MlnPV2FPT0WU
EW-13 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrITJRKSzVyPUK5MlM5OTRizszN MnXiV2FPT0WU
MOLT-13 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fmXGlEPTB;MkmuN|gyPCEQvF2= Mm\4V2FPT0WU
L-363 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\QcGlEPTB;MkmuOFc6QCEQvF2= MoPWV2FPT0WU
EM-2 NYPLPFV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\K[GNJUUN3ME2yPU41QTBzIN88US=> M3T4[nNCVkeHUh?=
RS4-11 MoTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTNyLkSyOFEh|ryP NV7CZ2JTW0GQR1XS
A2780 NHnt[ldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTNyLke0OVch|ryP MnK2V2FPT0WU
KU812 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTN{LkO2OFIh|ryP NWfycGd6W0GQR1XS
COLO-684 NH2wOmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTN|LkO1PVkh|ryP NVLhNGdXW0GQR1XS
MFE-280 M37lSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPtToEyUUN3ME2zN{4{QDh7IN88US=> MljPV2FPT0WU
KG-1 NUjzZ5RzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXWxUXRKUUN3ME2zN{43ODBzIN88US=> MXPTRW5ITVJ?
JVM-3 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTN3LkW4Olgh|ryP NF\NZ2ZUSU6JRWK=
MV-4-11 NYDYRlI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XnbGlEPTB;M{WuPFQ6QSEQvF2= NEXtVXhUSU6JRWK=
LAMA-84 Moi5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHsTWM2OD1|Nj63N|Q2KM7:TR?= MmjWV2FPT0WU
MOLT-16 M3e1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vFNGlEPTB;M{[uPVUzKM7:TR?= NULGcHVrW0GQR1XS
H4 NUK5ZoZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTN5LkW2O{DPxE1? M1PNWnNCVkeHUh?=
T47D NYj2c21zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fNdGlEPTB;M{euO|AyQCEQvF2= M3XiOXNCVkeHUh?=
CAL-54 M{LSd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1yyW2lEPTB;M{euPVY3KM7:TR?= M4rueHNCVkeHUh?=
SW982 MlnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrE[FQ1UUN3ME2zPE4xQTl6IN88US=> M{XxdnNCVkeHUh?=
IGROV-1 NHzwOZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTN7LkOzNFQh|ryP MnrlV2FPT0WU
NB14 NVHSb5N4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPsbJdvUUN3ME20NE44ODNzIN88US=> MkG4V2FPT0WU
HCC1187 M1vId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XoXWlEPTB;NEGuNlc4OSEQvF2= NYGxNI9WW0GQR1XS
SBC-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTRzLkOwOlMh|ryP NWTZbmY4W0GQR1XS
KARPAS-45 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnWTWM2OD12MT60PFE5KM7:TR?= MYLTRW5ITVJ?
MOLT-4 MkLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTR{LkK1N|gh|ryP MorOV2FPT0WU
JVM-2 M3jkNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfnTWM2OD12Mj65NlA4KM7:TR?= NHGzdm5USU6JRWK=
A4-Fuk M2LJdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3uU2tKSzVyPUSzMlU3QTFizszN NH:yWZBUSU6JRWK=
MDA-MB-361 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn35TWM2OD12Mz64OFE1KM7:TR?= NIrke21USU6JRWK=
BALL-1 M4\HfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFyxN|VKSzVyPUSzMlk2OzJizszN M2\LVHNCVkeHUh?=
T98G Mn7rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7NTWM2OD12ND64OVE4KM7:TR?= MWDTRW5ITVJ?
Mo-T NVPtTVFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjo[FBWUUN3ME20OU43Ozh7IN88US=> MUfTRW5ITVJ?
MHH-PREB-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTR3Lke1PFUh|ryP M3WzSHNCVkeHUh?=
ALL-PO NYjJfYV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV32O|dIUUN3ME20O{4{PzlzIN88US=> NWrpNnI{W0GQR1XS
NCI-H510A MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVH2XG5CUUN3ME20O{46ODN2IN88US=> NUfaOnZyW0GQR1XS
ML-2 M33o[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTtTWM2OD12OT63PFU3KM7:TR?= NF;hdlhUSU6JRWK=

... 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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