Veliparib (ABT-888)

Catalog No.S1004 Synonyms: NSC 737664

Veliparib (ABT-888) Chemical Structure

Molecular Weight(MW): 244.29

Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.

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Cited by 43 Publications

10 Customer Reviews

  • Chromosomal single-strand break repair rates in the indicated RPE-1 cell lines following treatment with 50 μM H2O2 in the presence/absence of 10 μM of the PARP inhibitor (PARPi) Veliparib, as measured by alkaline comet assay. Data are the mean tail moment of 100 cells per sample per experiment and are the average (-/+SEM) of three independent experiments. Two-way ANOVA analysis between relevant genotypes is presented (ns= not significant, **= p<0.01, ***= p<0.001).

    Nature, 2017, 541(7635):87-91. Veliparib (ABT-888) purchased from Selleck.

    (A) OVCAR-8 cells were exposed to the indicated concentrations of FdUrd along with vehicle, 3 μM ABT-888 or 300 nM AZD2281 for 24 h. Following washing, ABT-888 and AZD2281 were re-added to the plates initially exposed to these agents, and cells were cultured in the continued presence of ABT-888 and AZD2281 for 8 d until colonies formed. (B) OVCAR-8 cells were exposed continuously to the indicated agents for 8 d. (C) OVCAR-8 cells treated as in (A) except that the indicated concentrations of ABT-888 were used.

    Cancer Research, 2011, 71: 4944-4954. Veliparib (ABT-888) purchased from Selleck.

  • OVCAR-8 cells were plated, treated with indicated concentrations of FdUrd and 3 μM ABT-888 using the exposure schemes depicted in (C) and assayed for clonogenicity (D).

    Cancer Research, 2011, 71: 4944-4954. Veliparib (ABT-888) purchased from Selleck.

     

    Number of foci detected using laser confocal microscopy and fluorescent Fluor 647 anti-H2A.X-phosphorylated (Ser139) antibody. Double-stranded breaks (red) are clearly augmented in cells incubated with 500 nmol/l of ABT-888 and 500 nmol/l of AZD-2281 compared with PBS and 1% dimethyl sulfoxide controls. Image analysis was performed using ImageJ and the ‘analyze particle’ function.

    Nucl Med Commun 2011 32, 1046-1051. Veliparib (ABT-888) purchased from Selleck.

  • Logarithmic growth curves of human Burkitt lymphoma cells over 5 days with 500 nmol/l of ABT-888 and AZD-2281 in combination with 0 Gy (a), 4 Gy (b), 8 Gy (c), and 12 Gy (d) of external beam radiation. The maximal relative reduction was 65.5% of viable cells and occurred with AZD-2281 (500 nmol/l) on day 5. DMSO, dimethyl sulfoxide.

    Nucl Med Commun 2011 32(11), 1046-51. Veliparib (ABT-888) purchased from Selleck.

    Colorimetric poly(ADP-ribose) polymerase (PARP) activity assay showing the relative activity of the PARP-1 enzyme in Raji lymphocyte tumor cells. Results show a highly significant difference in PARP activity in the controls [PBS and dimethyl sulfoxide (DMSO)] compared with 24 h incubation with 500 nmol/l of ABT-888 and 500 nmol/l of AZD-2281. A significant increase in PARP enzyme activity is shown in DMSO-incubated cells compared with PBS control.* P < 0.05.

    Nucl Med Commun 2011 32(11), 1046-51. Veliparib (ABT-888) purchased from Selleck.

  • T47D breast cancer cells were pretreated with indicated concentrations of ABT-888

     

     

    Dr.Zhang of Tianjin Medical University. Veliparib (ABT-888) purchased from Selleck.

    in vivo suppression of PAR formation by the PARP inhibitor ABT-888 upon induction of DNA damage

    Primary human lung fibroblast cells (MRC-5) were pre-treated with the indicated concentration of the PARP inhibitor ABT-888 for two hours. Oxidative DNA damage was induced by 500 µM H2O2 for 10 min and cellular PARP activity was measured by immuno-staining of poly(ADP)-ribose (PAR) (right panels). The in vivo effect of PARP inhibition was compared to cells without DNA damage induction and inhibitor (control) and H2O2-treated cells without inhibitor.
    Average nuclear PAR staining intensities of more than 50 cells were statistically analysed by Kruskal-Wallis and the post-hoc Dunn’s Multiple Comparison tests (left panel). Asterisks indicate highly significant (p<1%) differences to H2O2-treated cells without PARP inhibitor. Thick horizontal bars mark medians and error bars the interquartile range.
     
     

     

    David Schrmann from University of Base. Veliparib (ABT-888) purchased from Selleck.

  • Caption:  451 Lu is a melanoma cell line with high PARP expression that is resistant to temozolomide.  Treatment with 25 µM ABT-888 greatly increased sensitivity to temozolomide compared to cells without ABT-888 treatment as measured by MTS assay.

     

     

    Dr. Steve Reuland from University of Colorado Denver. Veliparib (ABT-888) purchased from Selleck.

    Effect of ABT-888 on the viability of endometrial cancer cell line Hec50 and Ishikawa and ovarian cancer cell line SKOV3,Caov3 and PA-1 was detected by WST-1 method after 3 days treatment.

     
     

     

    Dr. Xiangbing Meng of University of Iowa. Veliparib (ABT-888) purchased from Selleck.

Purity & Quality Control

Choose Selective PARP Inhibitors

Biological Activity

Description Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.
Features Increases the efficacy of common cancer therapies such as radiation and alkylating agents.
Targets
PARP2 [1]
(Cell-free assay)
PARP1 [1]
(Cell-free assay)
2.9 nM(Ki) 5.2 nM(Ki)
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C41 NWLsRmVGU2mwYYPlJGF{e2G7 Ml7jN|AhdWmw M1TYVmlvcGmkaYTpc44hd2ZiUFHSVFEhf2m2aDDFR|UxKG:oIECuNFAzKM7:TR?= NY\ZRWhVOTl6OEi3OlA>
Jurkat MWXLbY5ie2ViQYPzZZk> M1TVbFk3KGh? Mn;rSG1UVw>? NEDWUplKdmirYnn0bY9vKG:oIGDBVnAyKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBk\WyuII\pZYJqdGm2eTD3bZRpKEWFNUCgc4YhOyEQvF2= MVSyN|g2ODF7OR?=
Capan1 NWDmTIVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV63NkBp NWG2d2NJTE2VTx?= MknPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDCVmNCOiCpZX7lJI12fGG2ZXSgbJVu[W5iQ3HwZY4yKGOnbHzzJJdqfGhiSVO1NEBw\iB|OT63JO69VQ>? MnjxNlQ{QTh|OEO=
DT40 Mm\CR5l1d3SxeHnjJGF{e2G7 M1qzOlczKGh? MVXEUXNQ NWTQNoNKS3m2b4TvfIlkcXS7IHHnZYlve3RiY3jpZ4tmdiCEUlPBNk1l\W[rY3nlcpQhTFR2MDDj[Yxtew>? MmfsNlQ6OjJ3OEe=
ML-1 NWDSUnFkSXCxcITveIlkKEG|c3H5 NETn[lkzNjVizszN NHy4WlUzPCCq M{f0cmROW09? NY[4PYd1W3mwZYLnbZN1cWOjbHz5JIVvcGGwY3XzJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m|IHnuJG1NNTFiY3XscJM> NYrTTmdROjR6OUWxN|U>
HCT-116 M3XKfmtqdmG|ZTDBd5NigQ>? MUSwMlUh|ryP M4H1VFI1KGh? MX;QRXJRKGGldHn2bZR6KGSnY4LlZZNmew>? MXSyN|A2PDJzMx?=
UM-SCC1 NFezV2lEgXSxdH;4bYMhSXO|YYm= MXWxNEDPxE1? MorwNlQhcA>? M1foT3Jm\HWlZYOgeIhmKGOnbHygeoli[mmuaYT5 NGrkeWIzOTlzMk[yNC=>
FaDu MUnDfZRwfG:6aXOgRZN{[Xl? M{nq[FExKM7:TR?= NXGwVlRXOjRiaB?= NIr3ZppT\WS3Y3XzJJRp\SClZXzsJJZq[WKrbHn0fS=> MVKyNVkyOjZ{MB?=
PC-3 NULNS2tUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorpNVAh|ryP M2DsPWlv\HWlZYOgZUB{cWewaX\pZ4FvfCCrbnjpZol1cW:wIHnuJINwdG:weTDmc5Ju[XSrb39CpC=> NYD3cJhWOjF3N{G5NVI>
EoL-1-cell M{m2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFwMEe5PEDPxE1? NXTXN2xQW0GQR1XS
NCI-SNU-5 M3TBWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\WfmlEPTB;Mz6xNlg1OSEQvF2= MVfTRW5ITVJ?
BV-173 NV;NNYN5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTVwNEW0NFkh|ryP MYnTRW5ITVJ?
HCC1806 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljnTWM2OD13Lke1NVc{KM7:TR?= NEW5[mFUSU6JRWK=
COLO-680 MkHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTZwMkG0NFYh|ryP MYHTRW5ITVJ?
HCC2218 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTdwN{m3NFQh|ryP M4LBNHNCVkeHUh?=
SK-MEL-24 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrIcohSUUN3ME23MlgyQTJ2IN88US=> M{L5enNCVkeHUh?=
NCI-H720 NGH5bGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRThwNEO2NFMh|ryP Mne2V2FPT0WU
KASUMI-1 M3XrNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jwbWlEPTB;OD64PVI3PiEQvF2= NEXWU4ZUSU6JRWK=
HAL-01 NFXZW2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4W2bWlEPTB;OT64PFYzKM7:TR?= MVrTRW5ITVJ?
CAL-33 NHXSbFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHIVoxoUUN3ME2xNE41OzRizszN NW\UOGc2W0GQR1XS
SK-MEL-1 MnPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXhWYJrUUN3ME2xNk41PjZ|IN88US=> MXHTRW5ITVJ?
Ramos-2G6-4C10 NU\0[JdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTkTWM2OD1zMj60O|UzKM7:TR?= MkLNV2FPT0WU
KY821 Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHCe3hKSzVyPUGyMlQ5PSEQvF2= NGT5NGtUSU6JRWK=
HEC-1 NHTFd3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7KTWM2OD1zMj65NVk3KM7:TR?= M3rvZnNCVkeHUh?=
SK-NEP-1 MojRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37vZ2lEPTB;MUOuNVY3KM7:TR?= MUfTRW5ITVJ?
MN-60 MorMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XrTGlEPTB;MUOuOVM5QSEQvF2= M1HzeXNCVkeHUh?=
DU-145 NEjueXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLaTWM2OD1zMz65NFU{KM7:TR?= NEPmSHRUSU6JRWK=
EW-3 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HLT2lEPTB;MUSuOVU3PSEQvF2= NXH1e5dKW0GQR1XS
OS-RC-2 NUPleWJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DP[mlEPTB;MUWuPVU5QSEQvF2= M3HqSHNCVkeHUh?=
RPMI-8226 Mlv1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoD4TWM2OD1zNj6yNFQzKM7:TR?= MXPTRW5ITVJ?
ChaGo-K-1 M{K3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHiO4x3UUN3ME2xOk42OzJ3IN88US=> MmPsV2FPT0WU
DEL NGn6b3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HTT2lEPTB;MU[uOlcyPyEQvF2= M3G2RXNCVkeHUh?=
GP5d NFjrd3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnMS2xKSzVyPUG3MlA2OyEQvF2= M3LUdXNCVkeHUh?=
COLO-668 NWCy[Il1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTF5Lk[yPVQh|ryP Mn\IV2FPT0WU
H9 NYnk[mhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTF6LkK4N|Mh|ryP NXu4Tmo3W0GQR1XS
NKM-1 Mm\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\QZ5VDUUN3ME2xPE42OTF7IN88US=> M4fvbHNCVkeHUh?=
KYSE-150 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTF6Lkm5PFYh|ryP NIfYXFFUSU6JRWK=
Daoy MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTF7LkW2OFkh|ryP NV\0WFhxW0GQR1XS
ECC10 NHLUSXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3kWlUzUUN3ME2yNE44PDV3IN88US=> M{XRb3NCVkeHUh?=
A388 MlnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2j1[WlEPTB;MkGuPVA6OSEQvF2= Mof0V2FPT0WU
MHH-NB-11 NHj4NJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvLTWM2OD1{Mz6xN|Y{KM7:TR?= NEfBR2xUSU6JRWK=
HCC1937 M{[1VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHK[oJKSzVyPUK0Mlc1PiEQvF2= NHj4VVZUSU6JRWK=
TGBC11TKB NEL6VlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rvNmlEPTB;MkWuOlg3OyEQvF2= M3XTSXNCVkeHUh?=
CTV-1 MlXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPGWWlPUUN3ME2yOU45QTZ7IN88US=> M4jYd3NCVkeHUh?=
NCI-H2029 MonlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mli4TWM2OD1{Nj60NlM5KM7:TR?= M{nwPHNCVkeHUh?=
HLE M4XPV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfkcm5KSzVyPUK3MlA2PCEQvF2= MXvTRW5ITVJ?
NCI-H1693 NEm4flJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnTOZd7UUN3ME2yO{4zQDl6IN88US=> NGTjN2tUSU6JRWK=
HCC70 M1;DWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTJ5LkeyOFYh|ryP M3H1S3NCVkeHUh?=
BEN NUPGNYVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XHWWlEPTB;MkeuPVU3PiEQvF2= NFu3UoVUSU6JRWK=
LB771 NVLNSGw3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXiZWdpUUN3ME2yPE45Ozd|IN88US=> Mk\NV2FPT0WU
697 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nmXWlEPTB;MkmuNFI{PSEQvF2= NWHJRoM{W0GQR1XS
LU-139 M37vZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXMW2p{UUN3ME2yPU4{PzR6IN88US=> MmXPV2FPT0WU
EW-13 M3zZU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LDe2lEPTB;MkmuN|gyPCEQvF2= MULTRW5ITVJ?
MOLT-13 Mlm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2ixdWlEPTB;MkmuN|gyPCEQvF2= NHL5NJBUSU6JRWK=
L-363 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfZZXhoUUN3ME2yPU41Pzl6IN88US=> M3LaeXNCVkeHUh?=
EM-2 NEiy[4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\BNmlEPTB;MkmuOFkxOSEQvF2= M2jDOHNCVkeHUh?=
RS4-11 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvUPI5KSzVyPUOwMlQzPDFizszN M1u3NnNCVkeHUh?=
A2780 M{LySmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljRTWM2OD1|MD63OFU4KM7:TR?= NYTFUnkzW0GQR1XS
KU812 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvZWZBvUUN3ME2zNk4{PjR{IN88US=> MVfTRW5ITVJ?
COLO-684 NFvZW25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLJZ4h5UUN3ME2zN{4{PTl7IN88US=> MVjTRW5ITVJ?
MFE-280 MoC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\3XWlEPTB;M{OuN|g5QSEQvF2= M2DVUHNCVkeHUh?=
KG-1 M3TDUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPOTmtEUUN3ME2zN{43ODBzIN88US=> MYLTRW5ITVJ?
JVM-3 M1;5XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInk[|JKSzVyPUO1MlU5PjhizszN Mn\GV2FPT0WU
MV-4-11 NHG4PYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjVO4tKSzVyPUO1Mlg1QTlizszN NWTMPGF[W0GQR1XS
LAMA-84 MnqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DBZmlEPTB;M{[uO|M1PSEQvF2= Moe1V2FPT0WU
MOLT-16 M{D4fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnP1TWM2OD1|Nj65OVIh|ryP MoW2V2FPT0WU
H4 MkDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTN5LkW2O{DPxE1? MYHTRW5ITVJ?
T47D NEXxXYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTN5LkewNVgh|ryP MkPRV2FPT0WU
CAL-54 M1SzRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3yTWM2OD1|Nz65OlYh|ryP NGXMU3BUSU6JRWK=
SW982 M2fDNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHQOpVKSzVyPUO4MlA6QThizszN NHrlcYVUSU6JRWK=
IGROV-1 MnjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTN7LkOzNFQh|ryP NVe1fpRNW0GQR1XS
NB14 MkDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPMTWM2OD12MD63NFMyKM7:TR?= Mli2V2FPT0WU
HCC1187 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DYSmlEPTB;NEGuNlc4OSEQvF2= NUTMSGRbW0GQR1XS
SBC-1 NWC3Zm9QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\OPYJRUUN3ME20NU4{ODZ|IN88US=> M3qxcnNCVkeHUh?=
KARPAS-45 M{LnSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml62TWM2OD12MT60PFE5KM7:TR?= NXPrSGhzW0GQR1XS
MOLT-4 NGnvVpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\IcWdIUUN3ME20Nk4zPTN6IN88US=> NYPiVWFKW0GQR1XS
JVM-2 NF24O|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPzV2IyUUN3ME20Nk46OjB5IN88US=> NFjXclNUSU6JRWK=
A4-Fuk M1PLbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInXcZNKSzVyPUSzMlU3QTFizszN MW\TRW5ITVJ?
MDA-MB-361 Mne0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTR|Lki0NVQh|ryP MUjTRW5ITVJ?
BALL-1 NEDW[opIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTR|Lkm1N|Ih|ryP MoLLV2FPT0WU
T98G Mon6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXLfVNDUUN3ME20OE45PTF5IN88US=> NXy4WI5jW0GQR1XS
Mo-T MoDSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTR3Lk[zPFkh|ryP MXXTRW5ITVJ?
MHH-PREB-1 NXfEOHl{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33kVmlEPTB;NEWuO|U5PSEQvF2= NGDQVG5USU6JRWK=
ALL-PO MlLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TnNGlEPTB;NEeuN|c6OSEQvF2= M4e5PHNCVkeHUh?=
NCI-H510A MlLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnBTWM2OD12Nz65NFM1KM7:TR?= NGSwWXpUSU6JRWK=
ML-2 NEXKdXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXu[GhZUUN3ME20PU44QDV4IN88US=> Moi4V2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / p-AKT(S473) / p-AKT(T308) / p-ERK / p-p38; 

PubMed: 22678161     


Effects of AG-014699, AZD-2281, ABT-888, or BSI-201 on the phosphorylation status of Stat3, Akt, ERK, and p38 in MDA-MB-468, MDA-MB-231, and Cal-51 cells after 72 h of treatment

22678161
Immunofluorescence
HuR; 

PubMed: 28687616     


Immunofluorescent images of HuR (green) in MIA PaCa-2 cells treated with PARPi for 12hr. Nuclei were stained with DAPI. Magnification 40X.

BRCA1; 

PubMed: 21917757     


Effects of ABT-888 and/or bortezomib on BRCA1 and RAD51 foci formation. BRCA1 and RAD1 foci induced by ABT-888 were completely resolved in cells cotreated with bortezomib. Image acquisition was performed with an epifluorescence microscope (BX51; Olympus) and multispectral color camera (Nuance FX; CRi) with a 60× or 100× magnification lens and oil immersion.

28687616 21917757
Growth inhibition assay
Cell viability (TNBC cell lines); 

PubMed: 27880910     


BRCA-proficient TNBC cell lines were treated with veliparib in the absence and presence of dinaciclib, demonstrating reduced IC50 values in the presence of dinaciclib.

Cell viability (melanoma cells); 

PubMed: 29956724     


Dose-dependent inhibitory effect of ABT-888 on melanoma cell proliferation. Human melanoma cell lines were exposed to diluents (control; CTRL) or increasing concentrations of ABT-888 for 72 h and their viability was assessed by MTT assay. Absorbance was detected at 540 nm with a microplate reader and data were expressed as a percentage of the CTRL. Data are the means ± SD of 3 experiments performed in triplicate. Statistical significance was calculated against the CTRL (*P<0.05; **P<0.01).

27880910 29956724
In vivo 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]

Protocol

Animal Research:

[1]

+ Expand
  • Animal Models: NCI-H460, H460, B16F10 and 9L xenografts in C57BL/6 mice
  • Formulation: Formulated in solution containing 0.9% NaCl adjusted to pH 4.0
  • Dosages: ~25 mg/kg
  • Administration: Orally administered
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 17 mg/mL (69.58 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose+0.2% Tween 80
For best results, use promptly after mixing.
5 mg/mL

* 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.

Chemical Information

Molecular Weight 244.29
Formula

C13H16N4O

CAS No. 912444-00-9
Storage powder
in solvent
Synonyms NSC 737664

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03400306 Not yet recruiting Cancer - Ovarian AbbVie May 10 2020 Phase 1
NCT03400306 Not yet recruiting Cancer - Ovarian AbbVie May 10 2020 Phase 1
NCT03044795 Not yet recruiting Cancer University Medical Center Groningen|AbbVie|Dutch Cancer Society November 2018 Phase 2
NCT03044795 Not yet recruiting Cancer University Medical Center Groningen|AbbVie|Dutch Cancer Society November 2018 Phase 2
NCT03581292 Recruiting Anaplastic Astrocytoma|Glioblastoma|Malignant Glioma National Cancer Institute (NCI) October 31 2018 Phase 2
NCT03581292 Recruiting Anaplastic Astrocytoma|Glioblastoma|Malignant Glioma National Cancer Institute (NCI) October 31 2018 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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PARP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID