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40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 MV;LbY5ie2ViQYPzZZk> MWSzNEBucW5? M4TYNGlvcGmkaYTpc44hd2ZiUFHSVFEhf2m2aDDFR|UxKG:oIECuNFAzKM7:TR?= MkT6NVk5QDh5NkC=
Jurkat M33lVGtqdmG|ZTDBd5NigQ>? NF:1Xlc6PiCq NUP6V5p7TE2VTx?= NIPlbW9KdmirYnn0bY9vKG:oIGDBVnAyKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBk\WyuII\pZYJqdGm2eTD3bZRpKEWFNUCgc4YhOyEQvF2= MYiyN|g2ODF7OR?=
Capan1 M2r6Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrGb|VVPzJiaB?= NIPJV|VFVVOR Mn;KRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDCVmNCOiCpZX7lJI12fGG2ZXSgbJVu[W5iQ3HwZY4yKGOnbHzzJJdqfGhiSVO1NEBw\iB|OT63JO69VQ>? NYTpdnY3OjR|OUizPFM>
DT40 MkDFR5l1d3SxeHnjJGF{e2G7 NHvudmI4OiCq NXe1S2M2TE2VTx?= MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBkcGmla3XuJGJTS0F{LXTl[olkcWWwdDDEWFQxKGOnbHzz M3v5VlI1QTJ{NUi3
ML-1 NI[2OXBCeG:ydH;0bYMhSXO|YYm= M1\qSlIvPSEQvF2= NHPLcGYzPCCq NEP5SoRFVVOR MWPTfY5memerc4TpZ4FtdHliZX7oZY5k\XNiVGLBTWwucW6mdXPl[EBieG:ydH;zbZMhcW5iTVytNUBk\Wyucx?= MWGyOFg6PTF|NR?=
HCT-116 MkfnT4lv[XOnIFHzd4F6 MUSwMlUh|ryP MmHyNlQhcA>? MojMVGFTWCCjY4Tpeol1gSCmZXPy[YF{\XN? M2LmSFI{ODV2MkGz
UM-SCC1 M{nLR2N6fG:2b4jpZ{BCe3OjeR?= Mor2NVAh|ryP NHK4cFEzPCCq MUDS[YR2[2W|IITo[UBk\WyuII\pZYJqdGm2eR?= MYCyNVkyOjZ{MB?=
FaDu NGTId3hEgXSxdH;4bYMhSXO|YYm= MmnsNVAh|ryP M2HIeVI1KGh? NF75cYRT\WS3Y3XzJJRp\SClZXzsJJZq[WKrbHn0fS=> NHHwT|EzOTlzMk[yNC=>
PC-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUWzVnJ{OTBizszN MWnJcoR2[2W|IHGgd4lodmmoaXPhcpQhcW6qaXLpeIlwdiCrbjDjc4xwdnliZn;ycYF1cW:wwrC= NWrjNmxMOjF3N{G5NVI>
EoL-1-cell MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XqTGlEPTB;MT6wO|k5KM7:TR?= M{LN[nNCVkeHUh?=
NCI-SNU-5 NH\ONo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTNwMUK4OFEh|ryP NFjqVXBUSU6JRWK=
BV-173 NX7wR|Q1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjG[|ZKSzVyPUWuOFU1ODlizszN NUfqWIdsW0GQR1XS
HCC1806 M3zQSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTVwN{WxO|Mh|ryP NY\abHlHW0GQR1XS
COLO-680 MnjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfRTWM2OD14LkKxOFA3KM7:TR?= NGHpfIhUSU6JRWK=
HCC2218 NGr5cmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXzXI1jUUN3ME23Mlc6PzB2IN88US=> NX\ub5dRW0GQR1XS
SK-MEL-24 M2nUNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnu2TWM2OD15LkixPVI1KM7:TR?= NGPqN4VUSU6JRWK=
NCI-H720 M3TFSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIq3cXBKSzVyPUiuOFM3ODNizszN MUnTRW5ITVJ?
KASUMI-1 NX3uTpk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRThwOEmyOlYh|ryP MXTTRW5ITVJ?
HAL-01 NGHtWWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXqZVA5UUN3ME25Mlg5PjJizszN NGXqVVVUSU6JRWK=
CAL-33 M4XCeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFyLkSzOEDPxE1? MU\TRW5ITVJ?
SK-MEL-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmGxTWM2OD1zMj60OlY{KM7:TR?= M1ztRnNCVkeHUh?=
Ramos-2G6-4C10 NGD2U4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjj[HdKSzVyPUGyMlQ4PTJizszN Mn3BV2FPT0WU
KY821 MkDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3ZfJpKSzVyPUGyMlQ5PSEQvF2= NYftUXdYW0GQR1XS
HEC-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HtS2lEPTB;MUKuPVE6PiEQvF2= NXvIZZMyW0GQR1XS
SK-NEP-1 NGPLWlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmj0TWM2OD1zMz6xOlYh|ryP NIrZboJUSU6JRWK=
MN-60 MnTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfGWlBKSzVyPUGzMlU{QDlizszN NWLqbHpmW0GQR1XS
DU-145 NFrwNpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV:yfFJlUUN3ME2xN{46ODV|IN88US=> M1zQd3NCVkeHUh?=
EW-3 MnzwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTF2LkW1OlUh|ryP MVnTRW5ITVJ?
OS-RC-2 NYDuWnlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTF3Lkm1PFkh|ryP M1\lPHNCVkeHUh?=
RPMI-8226 MoPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mom2TWM2OD1zNj6yNFQzKM7:TR?= NGH4TGtUSU6JRWK=
ChaGo-K-1 NWjxXlBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nBNWlEPTB;MU[uOVMzPSEQvF2= M1;LOnNCVkeHUh?=
DEL NFXvR4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXZT3ZKSzVyPUG2MlY4OTdizszN Mo\NV2FPT0WU
GP5d NEX2TVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlO3TWM2OD1zNz6wOVMh|ryP MWjTRW5ITVJ?
COLO-668 NFTGOYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmr0TWM2OD1zNz62Nlk1KM7:TR?= MXPTRW5ITVJ?
H9 NHTaTGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XZdmlEPTB;MUiuNlg{OyEQvF2= M4D3R3NCVkeHUh?=
NKM-1 NWjCZZN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTF6LkWxNVkh|ryP MVrTRW5ITVJ?
KYSE-150 Ml3SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTF6Lkm5PFYh|ryP MVLTRW5ITVJ?
Daoy M4fZZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWT3T4R3UUN3ME2xPU42PjR7IN88US=> NUDLdmFxW0GQR1XS
ECC10 Mn3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkmxTWM2OD1{MD63OFU2KM7:TR?= M{XiWXNCVkeHUh?=
A388 NFnxfo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7aTWM2OD1{MT65NFkyKM7:TR?= MUnTRW5ITVJ?
MHH-NB-11 NWfoSpR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV2wNXVFUUN3ME2yN{4yOzZ|IN88US=> NGnaXGxUSU6JRWK=
HCC1937 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\ofXA6UUN3ME2yOE44PDZizszN MnzXV2FPT0WU
TGBC11TKB NHzDc41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTJ3Lk[4OlMh|ryP M2LxUHNCVkeHUh?=
CTV-1 MlrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\BTWM2OD1{NT64PVY6KM7:TR?= M4[xZnNCVkeHUh?=
NCI-H2029 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYmxW5diUUN3ME2yOk41OjN6IN88US=> MoPqV2FPT0WU
HLE MnTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LCTGlEPTB;MkeuNFU1KM7:TR?= NFjqVmlUSU6JRWK=
NCI-H1693 NW\vcnpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TubGlEPTB;MkeuNlg6QCEQvF2= NH\1OHZUSU6JRWK=
HCC70 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW[4cIdyUUN3ME2yO{44OjR4IN88US=> NVHjOJJqW0GQR1XS
BEN Mn3WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPPTWM2OD1{Nz65OVY3KM7:TR?= MoLGV2FPT0WU
LB771 NYC0WHF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PMOWlEPTB;MkiuPFM4OyEQvF2= MVPTRW5ITVJ?
697 MmL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33jTGlEPTB;MkmuNFI{PSEQvF2= M1G0fnNCVkeHUh?=
LU-139 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvSTWM2OD1{OT6zO|Q5KM7:TR?= MY\TRW5ITVJ?
EW-13 NXXkdmtoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DQZmlEPTB;MkmuN|gyPCEQvF2= MmjmV2FPT0WU
MOLT-13 NUO1OYw6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljDTWM2OD1{OT6zPFE1KM7:TR?= NXnvW3VLW0GQR1XS
L-363 NWHjZY1pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTJ7LkS3PVgh|ryP MVHTRW5ITVJ?
EM-2 M33jXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLBT5hKSzVyPUK5MlQ6ODFizszN NGf5U|RUSU6JRWK=
RS4-11 M16zdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlO2TWM2OD1|MD60NlQyKM7:TR?= Mnf1V2FPT0WU
A2780 MkPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTNyLke0OVch|ryP MnHOV2FPT0WU
KU812 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXG2VoNqUUN3ME2zNk4{PjR{IN88US=> MlrVV2FPT0WU
COLO-684 MmDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXITWM2OD1|Mz6zOVk6KM7:TR?= Mo\TV2FPT0WU
MFE-280 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTN|LkO4PFkh|ryP MojQV2FPT0WU
KG-1 NVOxN281T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PJSmlEPTB;M{OuOlAxOSEQvF2= NF\zNHBUSU6JRWK=
JVM-3 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PlSWlEPTB;M{WuOVg3QCEQvF2= NHvNXIFUSU6JRWK=
MV-4-11 M3zKUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPo[|hKSzVyPUO1Mlg1QTlizszN MXfTRW5ITVJ?
LAMA-84 NWPNRWlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnoTWM2OD1|Nj63N|Q2KM7:TR?= M{nVS3NCVkeHUh?=
MOLT-16 NGXSZVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnK4TWM2OD1|Nj65OVIh|ryP NWrnSGhLW0GQR1XS
H4 M{fNT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;nd|RKSzVyPUO3MlU3PyEQvF2= NYfHRYNlW0GQR1XS
T47D NHTGOXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTN5LkewNVgh|ryP M{TwWnNCVkeHUh?=
CAL-54 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHoXHpXUUN3ME2zO{46PjZizszN NXG5fZRJW0GQR1XS
SW982 M3LnXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXtTGxKSzVyPUO4MlA6QThizszN MV3TRW5ITVJ?
IGROV-1 M4fmfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrnO2hKSzVyPUO5MlM{ODRizszN NWDqbHVDW0GQR1XS
NB14 NWDwTpRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2W0TGlEPTB;NECuO|A{OSEQvF2= M1LH[nNCVkeHUh?=
HCC1187 M2DJbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTRzLkK3O|Eh|ryP M{[4S3NCVkeHUh?=
SBC-1 M4TL[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn70TWM2OD12MT6zNFY{KM7:TR?= NHK0Zo1USU6JRWK=
KARPAS-45 M1PSVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvL[pRzUUN3ME20NU41QDF6IN88US=> Mnf3V2FPT0WU
MOLT-4 NFvucYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTR{LkK1N|gh|ryP M13SOnNCVkeHUh?=
JVM-2 MkixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnaUHI3UUN3ME20Nk46OjB5IN88US=> M{e1c3NCVkeHUh?=
A4-Fuk MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PMOmlEPTB;NEOuOVY6OSEQvF2= NWjGNG5IW0GQR1XS
MDA-MB-361 NYHaTYhHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLHTWM2OD12Mz64OFE1KM7:TR?= NGHvVmhUSU6JRWK=
BALL-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4W0XmlEPTB;NEOuPVU{OiEQvF2= NGrlWIdUSU6JRWK=
T98G MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHzTWM2OD12ND64OVE4KM7:TR?= Mn2zV2FPT0WU
Mo-T MonTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHnTWM2OD12NT62N|g6KM7:TR?= MUnTRW5ITVJ?
MHH-PREB-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\mTWM2OD12NT63OVg2KM7:TR?= NIDpW3JUSU6JRWK=
ALL-PO MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H4bGlEPTB;NEeuN|c6OSEQvF2= MoDsV2FPT0WU
NCI-H510A MlzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXqcHNKSzVyPUS3MlkxOzRizszN MmXRV2FPT0WU
ML-2 M1HMbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LCcGlEPTB;NEmuO|g2PiEQvF2= Ml7pV2FPT0WU

... 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:
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
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
NCT00553189 Completed Solid Tumors|Lymphomas National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) August 9, 2007 Phase 1
NCT03032614 Not yet recruiting Breast Cancer Stage IV|Ovarian Cancer|BRCA1 Mutation|BRCA2 Mutation The University of Texas Health Science Center at San Antonio March 31, 2017 Phase 2
NCT01445522 Completed Neoplasms|Lymphoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) December 3, 2008 Phase 1
NCT01419548 Withdrawn Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 29, 2011 Phase 1
NCT02723864 Recruiting Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) March 22, 2016 Phase 1
NCT00994071 Completed Medulloblastoma|Pontine Glioma|Ependymoma|Astrocytoma|PNET National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) September 22, 2009 Phase 1

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID