Veliparib (ABT-888)

目录号:S1004 别名: NSC 737664

Veliparib (ABT-888) Chemical Structure

Molecular Weight(MW): 244.29

Veliparib (ABT-888)是一种有效的PARP1PARP2抑制剂,无细胞试验中Ki分别为5.2 nM和2.9 nM,对SIRT2没有活性。Phase 3。

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客户购买Selleck的此次产品后发表的文献42篇:

客户使用该产品的9个实验数据:

  • (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.

产品安全说明书

PARP抑制剂选择性比较

生物活性

产品描述 Veliparib (ABT-888)是一种有效的PARP1PARP2抑制剂,无细胞试验中Ki分别为5.2 nM和2.9 nM,对SIRT2没有活性。Phase 3。
特性 ABT-888增强常见癌症疗法的效果,比如放射疗法和烷基化剂。
靶点
PARP2 [1]
(Cell-free assay)
PARP1 [1]
(Cell-free assay)
2.9 nM(Ki) 5.2 nM(Ki)
体外研究

ABT-888有效抑制PARP,作用于PARP-1和PARP-2时Ki值分别为5.2和2.9 nM。ABT-888降低肺癌H460细胞中克隆基因的存活率,且抑制DNA修复。[1]ABT-888抑制C41细胞,EC50为2 nM。[2] ABT-888和放射物联用减少肿瘤血管的形成。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C41 M{fHXGtqdmG|ZTDBd5NigQ>? M17oUVMxKG2rbh?= M2jnb2lvcGmkaYTpc44hd2ZiUFHSVFEhf2m2aDDFR|UxKG:oIECuNFAzKM7:TR?= MV[xPVg5QDd4MB?=
Jurkat M1fPbGtqdmG|ZTDBd5NigQ>? NYfaPVcyQTZiaB?= NX:3eXQ1TE2VTx?= NF\JeYNKdmirYnn0bY9vKG:oIGDBVnAyKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBk\WyuII\pZYJqdGm2eTD3bZRpKEWFNUCgc4YhOyEQvF2= M4XTPFI{QDVyMUm5
Capan1 NUnMUXF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWi3NkBp MljDSG1UVw>? NFfTTZRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGJTS0F{IHflcoUhdXW2YYTl[EBpfW2jbjDDZZBidjFiY3XscJMhf2m2aDDJR|UxKG:oIEO5Mlch|ryP MYGyOFM6QDN6Mx?=
DT40 MW\DfZRwfG:6aXOgRZN{[Xl? NFrYelc4OiCq NGXXdVBFVVOR MkK1R5l1d3SxeHnjbZR6KGGpYXnud5Qh[2irY3vlckBDWkODMj3k[YZq[2mnboSgSHQ1OCClZXzsdy=> M3u4flI1QTJ{NUi3
ML-1 MmLiRZBweHSxdHnjJGF{e2G7 M3izWlIvPSEQvF2= M{X2OlI1KGh? MUPEUXNQ NGPwe29UgW6ncnfpd5Rq[2GubImg[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXNiaX6gUWwuOSClZXzsdy=> NHTVbY8zPDh7NUGzOS=>
HCT-116 MkLKT4lv[XOnIFHzd4F6 MWGwMlUh|ryP MYSyOEBp MXrQRXJRKGGldHn2bZR6KGSnY4LlZZNmew>? NYrsVZZ[OjNyNUSyNVM>
UM-SCC1 NYjUNo44S3m2b4TvfIlkKEG|c3H5 NYnvV5VjOTBizszN Mn\NNlQhcA>? NGOy[lhT\WS3Y3XzJJRp\SClZXzsJJZq[WKrbHn0fS=> NH;ySW0zOTlzMk[yNC=>
FaDu MWTDfZRwfG:6aXOgRZN{[Xl? NU[wUIxnOTBizszN M1T4b|I1KGh? MXnS[YR2[2W|IITo[UBk\WyuII\pZYJqdGm2eR?= MlzWNlE6OTJ4MkC=
PC-3 NIfoZoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWixNEDPxE1? NIPjSm9KdmS3Y3XzJIEhe2mpbnnmbYNidnRiaX7obYJqfGmxbjDpckBkd2yxbomg[o9zdWG2aX;uxsA> NXzIZ4xJOjF3N{G5NVI>
EoL-1-cell M1zmXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTFwMEe5PEDPxE1? MlG1V2FPT0WU
NCI-SNU-5 NGO5XmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfaUopKSzVyPUOuNVI5PDFizszN NGjwfpBUSU6JRWK=
BV-173 M4TaZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4ToXWlEPTB;NT60OVQxQSEQvF2= MlziV2FPT0WU
HCC1806 M1PIeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLZTWM2OD13Lke1NVc{KM7:TR?= NILiRYVUSU6JRWK=
COLO-680 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XIWWlEPTB;Nj6yNVQxPiEQvF2= M1GxXnNCVkeHUh?=
HCC2218 MoLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTdwN{m3NFQh|ryP M1zWPXNCVkeHUh?=
SK-MEL-24 NV[0WVVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\XWYgxUUN3ME23MlgyQTJ2IN88US=> MVfTRW5ITVJ?
NCI-H720 NIe1XpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37DUmlEPTB;OD60N|YxOyEQvF2= NYSzUpQ2W0GQR1XS
KASUMI-1 M4LLZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\jXHdOUUN3ME24Mlg6OjZ4IN88US=> MVjTRW5ITVJ?
HAL-01 NEe5TJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTlwOEi2NkDPxE1? NGLWRlhUSU6JRWK=
CAL-33 M4jrbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTKTWM2OD1zMD60N|Qh|ryP Mn;HV2FPT0WU
SK-MEL-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPzT45KSzVyPUGyMlQ3PjNizszN MV;TRW5ITVJ?
Ramos-2G6-4C10 M4TkOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILSc4VKSzVyPUGyMlQ4PTJizszN NXPT[WFHW0GQR1XS
KY821 M2K5SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PNfWlEPTB;MUKuOFg2KM7:TR?= NXjyT3pMW0GQR1XS
HEC-1 MofoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnewTWM2OD1zMj65NVk3KM7:TR?= NXHYNFVsW0GQR1XS
SK-NEP-1 Ml;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnBO5NQUUN3ME2xN{4yPjZizszN Mn3CV2FPT0WU
MN-60 MkDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTWS2FVUUN3ME2xN{42Ozh7IN88US=> NUXmOI8yW0GQR1XS
DU-145 NHfQbo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLpTWM2OD1zMz65NFU{KM7:TR?= M{jmNnNCVkeHUh?=
EW-3 NFTYWIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIezdYRKSzVyPUG0MlU2PjVizszN MVzTRW5ITVJ?
OS-RC-2 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjPTWM2OD1zNT65OVg6KM7:TR?= NUnlXI5vW0GQR1XS
RPMI-8226 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXiTWM2OD1zNj6yNFQzKM7:TR?= M3P1dnNCVkeHUh?=
ChaGo-K-1 MkjpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33nXGlEPTB;MU[uOVMzPSEQvF2= NHrrPJNUSU6JRWK=
DEL NX3Te4lQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXITWM2OD1zNj62O|E4KM7:TR?= NEfHR4FUSU6JRWK=
GP5d MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTF5LkC1N{DPxE1? Mk\UV2FPT0WU
COLO-668 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vic2lEPTB;MUeuOlI6PCEQvF2= NFrBTJNUSU6JRWK=
H9 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\0TWM2OD1zOD6yPFM{KM7:TR?= MXrTRW5ITVJ?
NKM-1 MkDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHjV3VKSzVyPUG4MlUyOTlizszN NF:0OGhUSU6JRWK=
KYSE-150 M{HJ[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTF6Lkm5PFYh|ryP MkPjV2FPT0WU
Daoy M3XYc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITrS2JKSzVyPUG5MlU3PDlizszN M3nSTHNCVkeHUh?=
ECC10 M3y5[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH[yNpRKSzVyPUKwMlc1PTVizszN NIjtZY1USU6JRWK=
A388 NXPJNpQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkC1TWM2OD1{MT65NFkyKM7:TR?= MnzWV2FPT0WU
MHH-NB-11 NHHoOphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TVXWlEPTB;MkOuNVM3OyEQvF2= NF3MUm9USU6JRWK=
HCC1937 NF:0NnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHSNJQ6UUN3ME2yOE44PDZizszN NVHjd4o4W0GQR1XS
TGBC11TKB NIOxXGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXrNYZVUUN3ME2yOU43QDZ|IN88US=> NV\LV4tDW0GQR1XS
CTV-1 NYDJWIRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTJ3Lki5Olkh|ryP NWXOdXVPW0GQR1XS
NCI-H2029 NW[2VZo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmCyTWM2OD1{Nj60NlM5KM7:TR?= M{WyenNCVkeHUh?=
HLE NF75[WhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zJVWlEPTB;MkeuNFU1KM7:TR?= M{DqPHNCVkeHUh?=
NCI-H1693 NIDTfINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXhTWM2OD1{Nz6yPFk5KM7:TR?= NVT5fnl3W0GQR1XS
HCC70 M4TsUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWntcYk2UUN3ME2yO{44OjR4IN88US=> NYfFWFdDW0GQR1XS
BEN MkW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XFdWlEPTB;MkeuPVU3PiEQvF2= NUHESoRUW0GQR1XS
LB771 NWLkTWhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoH2TWM2OD1{OD64N|c{KM7:TR?= MUnTRW5ITVJ?
697 NELHUGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTJ7LkCyN|Uh|ryP NIO1bXFUSU6JRWK=
LU-139 Mni5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL6OpJUUUN3ME2yPU4{PzR6IN88US=> MYfTRW5ITVJ?
EW-13 NIi1OG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIe1XXpKSzVyPUK5MlM5OTRizszN Mo\EV2FPT0WU
MOLT-13 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;oTWM2OD1{OT6zPFE1KM7:TR?= M{PG[nNCVkeHUh?=
L-363 NUOzRpdLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml22TWM2OD1{OT60O|k5KM7:TR?= NHzTXWZUSU6JRWK=
EM-2 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHMUGkzUUN3ME2yPU41QTBzIN88US=> MoTQV2FPT0WU
RS4-11 NYXQO3F4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\lTWM2OD1|MD60NlQyKM7:TR?= NXrRdoJ2W0GQR1XS
A2780 M4T3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHy5fWlKSzVyPUOwMlc1PTdizszN Mny0V2FPT0WU
KU812 M2D2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\KUpdOUUN3ME2zNk4{PjR{IN88US=> NIrsbGdUSU6JRWK=
COLO-684 MonhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDFfpRKSzVyPUOzMlM2QTlizszN MnfjV2FPT0WU
MFE-280 NYnvXGUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH[4NnNKSzVyPUOzMlM5QDlizszN M{HZVXNCVkeHUh?=
KG-1 NFf3NmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXW3NIpYUUN3ME2zN{43ODBzIN88US=> M3X3cnNCVkeHUh?=
JVM-3 NXfQcIRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1viNGlEPTB;M{WuOVg3QCEQvF2= MXTTRW5ITVJ?
MV-4-11 MmnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;sbFlKSzVyPUO1Mlg1QTlizszN NGTZPXpUSU6JRWK=
LAMA-84 Mnq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWi1[3ZXUUN3ME2zOk44OzR3IN88US=> M{\1V3NCVkeHUh?=
MOLT-16 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXqTWM2OD1|Nj65OVIh|ryP MVfTRW5ITVJ?
H4 NWrofXBmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH21XXlKSzVyPUO3MlU3PyEQvF2= NWLOXm95W0GQR1XS
T47D M1rXO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnr3TWM2OD1|Nz63NFE5KM7:TR?= MYfTRW5ITVJ?
CAL-54 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\sR2lkUUN3ME2zO{46PjZizszN MleyV2FPT0WU
SW982 MkDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\h[Y9rUUN3ME2zPE4xQTl6IN88US=> MYnTRW5ITVJ?
IGROV-1 MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTQTWM2OD1|OT6zN|A1KM7:TR?= MonjV2FPT0WU
NB14 Mke5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3iwW2lEPTB;NECuO|A{OSEQvF2= MV7TRW5ITVJ?
HCC1187 NXOwU2NDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLzTWM2OD12MT6yO|cyKM7:TR?= MVjTRW5ITVJ?
SBC-1 NGnXSG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTRzLkOwOlMh|ryP MoTXV2FPT0WU
KARPAS-45 NXTUNWxnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DiW2lEPTB;NEGuOFgyQCEQvF2= MVfTRW5ITVJ?
MOLT-4 M1vWcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmr2TWM2OD12Mj6yOVM5KM7:TR?= M3LiV3NCVkeHUh?=
JVM-2 M{fDSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTjbpp[UUN3ME20Nk46OjB5IN88US=> NH6xRVNUSU6JRWK=
A4-Fuk M13pPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfXTWM2OD12Mz61OlkyKM7:TR?= NVL1dWF6W0GQR1XS
MDA-MB-361 M2LFVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXtTWM2OD12Mz64OFE1KM7:TR?= M1;jSXNCVkeHUh?=
BALL-1 MmrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlu5TWM2OD12Mz65OVMzKM7:TR?= M{PFbHNCVkeHUh?=
T98G NGHROI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jHcmlEPTB;NESuPFUyPyEQvF2= MXPTRW5ITVJ?
Mo-T NFrCSFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTR3Lk[zPFkh|ryP M3TYOHNCVkeHUh?=
MHH-PREB-1 NIL3e2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfoTWM2OD12NT63OVg2KM7:TR?= Mn\mV2FPT0WU
ALL-PO M1rWVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2X1eGlEPTB;NEeuN|c6OSEQvF2= MV3TRW5ITVJ?
NCI-H510A NU\QeHpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfDTWM2OD12Nz65NFM1KM7:TR?= NFvoSXhUSU6JRWK=
ML-2 NGGzbnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPHbmV3UUN3ME20PU44QDV4IN88US=> NU\6[GtCW0GQR1XS

... Click to View More Cell Line Experimental Data

体内研究 ABT-888推迟NCI-H460 移植瘤模型的肿瘤生长。ABT-888在B16F10 和9L 移植瘤模型中抑制PARP,从而增强temozolomide的抗癌活性。[1]ABT-888和其他细胞毒素药剂联用作用于MX-1移植瘤模型时显示出强抗癌效力。[2]在A375和 Colo829移植瘤模型中按肿瘤大小,每千克分别加3和12.5 mg ABT-888,可以看到肿瘤内95%以上PAR被抑制。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
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体外PARP实验:

在含有50 mM Tris (pH 为8.0), 1 mM DTT,和 4 mM MgCl2的缓冲溶液中进行酶活性测定。PARP反应包含1.5 μM [3H]-NAD+ (1.6 μCi/mmol), 200 nM 生物素组蛋白 H1, 200 nM slDNA,及1 nM PARP-1或4 nM PARP-2酶。在加有100 μL 反应液的 96孔板上进行SPA检测。在50 μL含有PARP和DNA的2×酶液混合物中加入50 μL 2×NAD+基底混合物,反应开始。加入150 μL 1.5 mM 苯甲酰胺反应停止。170uL反应终止液转移到链霉亲和素包被的闪熔镀层上,温育1小时,用微型板块闪烁计数器计数。
细胞实验:[2]
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  • Cell lines: C41细胞
  • Concentrations: 10 μM 左右
  • Incubation Time: 0.5小时
  • Method: 在96孔板上用ABT-888处理C41细胞0.5小时。用1 mM H2O2破坏DNA10分钟,PARP被激活。用冰冻的PBS冲洗细胞,然后用预冷的甲醇/丙酮(按7:3比例混合)在−20oC下固定10 分钟。风干后,用PBS再溶解,然后用溶有5%脱脂奶粉的PBS- Tween封闭液(0.05%)在室温下阻断0.5小时。细胞和PAR抗体按1:50比例在封闭液中室温下温育1小时,然后用PBS-Tween-20冲洗5分钟,然后加入荧光素-5(6)-异硫氰酸酯 (FITC)-联用的二抗和1μg/mL DAPI封闭液中室温下温育1小时。PBS-Tween-20冲洗5分钟后,用荧光微型版计数器分析数据。
    (Only for Reference)
动物实验:[1]
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  • Animal Models: 携带NCI-H460, H460, B16F10和9L移植瘤的C57BL/6鼠
  • Formulation: 在含0.9% NaCl溶液中配制,调节pH 为4.0
  • Dosages: 25或3.125 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 17 mg/mL (69.58 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
0.5% methylcellulose+0.2% Tween 80
5 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 244.29
化学式

C13H16N4O

CAS号 912444-00-9
稳定性 powder
in solvent
别名 NSC 737664

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01540565 Completed BRCA1 Mutation Carrier|BRCA2 Mutation Carrier|Ovarian Epithelial Tumor|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma National Cancer Institute (NCI) April 9 2012 Phase 2
NCT00553189 Completed Solid Tumors|Lymphomas National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) August 9 2007 Phase 1
NCT03289910 Recruiting Acute Myeloid Leukemia|Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome|Atypical Chronic Myeloid Leukemia BCR-ABL1 Negative|Chronic Myelomonocytic Leukemia|Essential Thrombocythemia|Myelodysplastic/Myeloproliferative Neoplasm|Myelofibrosis|Polycythemia Vera|Recurrent Adult Acute Myeloid Leukemia|Refractory Acute Myeloid Leukemia National Cancer Institute (NCI) June 8 2018 Phase 2
NCT02595905 Recruiting Breast Carcinoma Metastatic in the Brain|Deleterious BRCA1 Gene Mutation|Deleterious BRCA2 Gene Mutation|Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage IV Breast Cancer AJCC v6 and v7|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) July 7 2016 Phase 2
NCT01749397 Active not recruiting Stage IV Fallopian Tube Cancer AJCC v6 and v7|Stage IV Ovarian Cancer AJCC v6 and v7|Stage IV Primary Peritoneal Cancer AJCC v7 National Cancer Institute (NCI) December 7 2012 Phase 1
NCT02163694 Active not recruiting Metastatic Breast Cancer AbbVie August 5 2014 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID