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43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 MmHkT4lv[XOnIFHzd4F6 MYOzNEBucW5? MlzSTY5pcWKrdHnvckBw\iCSQWLQNUB4cXSqIFXDOVAhd2ZiMD6wNFIh|ryP MYixPVg5QDd4MB?=
Jurkat MXvLbY5ie2ViQYPzZZk> M{LZZlk3KGh? MX3EUXNQ NF35fJNKdmirYnn0bY9vKG:oIGDBVnAyKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBk\WyuII\pZYJqdGm2eTD3bZRpKEWFNUCgc4YhOyEQvF2= Mn36NlM5PTBzOUm=
Capan1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVO3NkBp MV3EUXNQ MlvqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDCVmNCOiCpZX7lJI12fGG2ZXSgbJVu[W5iQ3HwZY4yKGOnbHzzJJdqfGhiSVO1NEBw\iB|OT63JO69VQ>? NVjjTppbOjR|OUizPFM>
DT40 NVLYdWt[S3m2b4TvfIlkKEG|c3H5 M4fKRVczKGh? M2fmU2ROW09? M4L2OWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGOqaXPr[Y4hSlKFQUKt[IVncWOrZX70JGRVPDBiY3XscJM> M2DjbVI1QTJ{NUi3
ML-1 MlLHRZBweHSxdHnjJGF{e2G7 NFK1NHMzNjVizszN MU[yOEBp NYO0Z3VyTE2VTx?= Mmi2V5lv\XKpaYP0bYNidGy7IHXubIFv[2W|IGTSRWlNNWmwZIXj[YQh[XCxcITvd4l{KGmwIF3MMVEh[2WubIO= M2PJ[lI1QDl3MUO1
HCT-116 NFPlV3dMcW6jc3WgRZN{[Xl? MVKwMlUh|ryP MmDvNlQhcA>? MmLhVGFTWCCjY4Tpeol1gSCmZXPy[YF{\XN? NUXsbZpUOjNyNUSyNVM>
UM-SCC1 NVzrTolvS3m2b4TvfIlkKEG|c3H5 M4TNUVExKM7:TR?= NX;HUnVIOjRiaB?= MYPS[YR2[2W|IITo[UBk\WyuII\pZYJqdGm2eR?= NXjWc5V5OjF7MUK2NlA>
FaDu MnTBR5l1d3SxeHnjJGF{e2G7 NIPiRlcyOCEQvF2= MnjiNlQhcA>? NXrIVoFpWmWmdXPld{B1cGViY3XscEB3cWGkaXzpeJk> MlPkNlE6OTJ4MkC=
PC-3 NUfVTpNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYCxNEDPxE1? MXzJcoR2[2W|IHGgd4lodmmoaXPhcpQhcW6qaXLpeIlwdiCrbjDjc4xwdnliZn;ycYF1cW:wwrC= M{DEbVIyPTdzOUGy
EoL-1-cell NGnwcmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPIeIxoUUN3ME2xMlA4QThizszN NXXYR3F{W0GQR1XS
NCI-SNU-5 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13FfWlEPTB;Mz6xNlg1OSEQvF2= NYD0fYJWW0GQR1XS
BV-173 NWDjO3VzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjrR2VKSzVyPUWuOFU1ODlizszN NFfudW9USU6JRWK=
HCC1806 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXWxTlN2UUN3ME21Mlc2OTd|IN88US=> NG\DUJBUSU6JRWK=
COLO-680 MoHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrSSmlKSzVyPU[uNlE1ODZizszN M2S4XXNCVkeHUh?=
HCC2218 NUPFSlJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rCdGlEPTB;Nz63PVcxPCEQvF2= MoPTV2FPT0WU
SK-MEL-24 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTwTWM2OD15LkixPVI1KM7:TR?= M3SzcHNCVkeHUh?=
NCI-H720 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRThwNEO2NFMh|ryP M1XjfnNCVkeHUh?=
KASUMI-1 NFv2NlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\X[5BKSzVyPUiuPFkzPjZizszN M17XUXNCVkeHUh?=
HAL-01 M3HrTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTlwOEi2NkDPxE1? MX7TRW5ITVJ?
CAL-33 MkniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\4TWM2OD1zMD60N|Qh|ryP NVfKVnFzW0GQR1XS
SK-MEL-1 NWPjWoVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFz5V5ZKSzVyPUGyMlQ3PjNizszN MY\TRW5ITVJ?
Ramos-2G6-4C10 NW\YUo1PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TxbmlEPTB;MUKuOFc2OiEQvF2= MXfTRW5ITVJ?
KY821 MmX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvmd2tKSzVyPUGyMlQ5PSEQvF2= NGHMNGZUSU6JRWK=
HEC-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTF{LkmxPVYh|ryP MnnnV2FPT0WU
SK-NEP-1 MoLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLET2JKSzVyPUGzMlE3PiEQvF2= MV\TRW5ITVJ?
MN-60 NFX0fYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTF|LkWzPFkh|ryP MlTvV2FPT0WU
DU-145 NH;N[2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfpTWM2OD1zMz65NFU{KM7:TR?= NHXyUWZUSU6JRWK=
EW-3 M3fRUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPqTWM2OD1zND61OVY2KM7:TR?= MlzpV2FPT0WU
OS-RC-2 M3O2T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTF3Lkm1PFkh|ryP NF20TIxUSU6JRWK=
RPMI-8226 NVXyXJZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fmWmlEPTB;MU[uNlA1OiEQvF2= MXLTRW5ITVJ?
ChaGo-K-1 Ml\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;2RnVDUUN3ME2xOk42OzJ3IN88US=> M{DmR3NCVkeHUh?=
DEL M3\Z[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\vcIRPUUN3ME2xOk43PzF5IN88US=> NVfBSFdTW0GQR1XS
GP5d M2LCNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17KUGlEPTB;MUeuNFU{KM7:TR?= MV3TRW5ITVJ?
COLO-668 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTF5Lk[yPVQh|ryP MVnTRW5ITVJ?
H9 NWfaN4xCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPjTWM2OD1zOD6yPFM{KM7:TR?= NVXTbFZUW0GQR1XS
NKM-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rCUmlEPTB;MUiuOVEyQSEQvF2= NUXKc|lbW0GQR1XS
KYSE-150 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Wy[2lEPTB;MUiuPVk5PiEQvF2= MYPTRW5ITVJ?
Daoy NGHMWIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXWTWM2OD1zOT61OlQ6KM7:TR?= MUTTRW5ITVJ?
ECC10 MnPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPrdXNUUUN3ME2yNE44PDV3IN88US=> NVzzSGU1W0GQR1XS
A388 NGPjcYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3i1[WlEPTB;MkGuPVA6OSEQvF2= NIr5WZFUSU6JRWK=
MHH-NB-11 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTJ|LkGzOlMh|ryP MmjaV2FPT0WU
HCC1937 NHS4clVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTJ2Lke0OkDPxE1? MlrMV2FPT0WU
TGBC11TKB MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37WOmlEPTB;MkWuOlg3OyEQvF2= MULTRW5ITVJ?
CTV-1 NF;zVIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nTbGlEPTB;MkWuPFk3QSEQvF2= MVvTRW5ITVJ?
NCI-H2029 NHL3UnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:ySWlEPTB;Mk[uOFI{QCEQvF2= NILxfJlUSU6JRWK=
HLE M4r3TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXzZ4plUUN3ME2yO{4xPTRizszN NWmwd|VZW0GQR1XS
NCI-H1693 NHfsTWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTJ5LkK4PVgh|ryP M2Cze3NCVkeHUh?=
HCC70 NX33NJM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTJ5LkeyOFYh|ryP M3rsbHNCVkeHUh?=
BEN M2LnOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTJ5Lkm1OlYh|ryP NUjrPG95W0GQR1XS
LB771 MoPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnwZW1xUUN3ME2yPE45Ozd|IN88US=> MoP2V2FPT0WU
697 NGHEfJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljZTWM2OD1{OT6wNlM2KM7:TR?= NXnNUGxOW0GQR1XS
LU-139 NF;VWlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPt[|FKSzVyPUK5MlM4PDhizszN MXfTRW5ITVJ?
EW-13 NHnBRWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4f3fGlEPTB;MkmuN|gyPCEQvF2= NF2wNFRUSU6JRWK=
MOLT-13 NELIfnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\ZTWM2OD1{OT6zPFE1KM7:TR?= M1SwW3NCVkeHUh?=
L-363 NYPPXJZ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV71[49VUUN3ME2yPU41Pzl6IN88US=> MlGwV2FPT0WU
EM-2 NFnES5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTJ7LkS5NFEh|ryP NHjveohUSU6JRWK=
RS4-11 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTNyLkSyOFEh|ryP M3XWWHNCVkeHUh?=
A2780 NY\2RoxWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\zTWM2OD1|MD63OFU4KM7:TR?= NFzEV3BUSU6JRWK=
KU812 Mn\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\XZXB6UUN3ME2zNk4{PjR{IN88US=> MnK2V2FPT0WU
COLO-684 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7wTWM2OD1|Mz6zOVk6KM7:TR?= M2rUbHNCVkeHUh?=
MFE-280 M2r0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfWSmxDUUN3ME2zN{4{QDh7IN88US=> NF3kUnlUSU6JRWK=
KG-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITJOGtKSzVyPUOzMlYxODFizszN MVzTRW5ITVJ?
JVM-3 NX\0Vm9xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;TcHdIUUN3ME2zOU42QDZ6IN88US=> M2ToeHNCVkeHUh?=
MV-4-11 MoHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\iRWlEPTB;M{WuPFQ6QSEQvF2= MUfTRW5ITVJ?
LAMA-84 M{n2Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTRTWM2OD1|Nj63N|Q2KM7:TR?= M3npPHNCVkeHUh?=
MOLT-16 M4SxXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTN4Lkm1NkDPxE1? NITLRoxUSU6JRWK=
H4 Mn;YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\vemlEPTB;M{euOVY4KM7:TR?= NVmxWoFmW0GQR1XS
T47D NWLTdYhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\uTGlEPTB;M{euO|AyQCEQvF2= NF\1cmRUSU6JRWK=
CAL-54 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfK[|ZKSzVyPUO3Mlk3PiEQvF2= NVLrdY1GW0GQR1XS
SW982 MoLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTpTWM2OD1|OD6wPVk5KM7:TR?= NVfEeG51W0GQR1XS
IGROV-1 M4LNV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYS2NmtJUUN3ME2zPU4{OzB2IN88US=> MkDSV2FPT0WU
NB14 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWi3e2RDUUN3ME20NE44ODNzIN88US=> NVfSd3ZJW0GQR1XS
HCC1187 NH\YcHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWj2eW5QUUN3ME20NU4zPzdzIN88US=> M3rS[3NCVkeHUh?=
SBC-1 NF;QeGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTRzLkOwOlMh|ryP NGjxOmtUSU6JRWK=
KARPAS-45 MkDoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\OTWM2OD12MT60PFE5KM7:TR?= MWjTRW5ITVJ?
MOLT-4 MlWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4W3N2lEPTB;NEKuNlU{QCEQvF2= NEjm[3pUSU6JRWK=
JVM-2 NV3RVmdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXKNGhYUUN3ME20Nk46OjB5IN88US=> M4G1SXNCVkeHUh?=
A4-Fuk M1HoSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTR|LkW2PVEh|ryP M4Ltc3NCVkeHUh?=
MDA-MB-361 NHXwclJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEn1fnlKSzVyPUSzMlg1OTRizszN NFWwXGlUSU6JRWK=
BALL-1 NIj4NHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTR|Lkm1N|Ih|ryP NWrDOG9ZW0GQR1XS
T98G MnjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTR2Lki1NVch|ryP NFH5VZNUSU6JRWK=
Mo-T MorNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT3WJpKSzVyPUS1MlY{QDlizszN NFz5eHpUSU6JRWK=
MHH-PREB-1 NFe2TGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnyUFZnUUN3ME20OU44PTh3IN88US=> NWHQc|h2W0GQR1XS
ALL-PO MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[2TWM2OD12Nz6zO|kyKM7:TR?= NWnMSplkW0GQR1XS
NCI-H510A NFjVXpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TBSWlEPTB;NEeuPVA{PCEQvF2= NUXmSmE6W0GQR1XS
ML-2 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\qRWJoUUN3ME20PU44QDV4IN88US=> NIXrdpFUSU6JRWK=

... 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
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
NCT03581292 Recruiting Anaplastic Astrocytoma|Glioblastoma|Malignant Glioma National Cancer Institute (NCI) October 31 2018 Phase 2
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
NCT02831179 Withdrawn Functional Pancreatic Neuroendocrine Tumor|Malignant Somatostatinoma|Merkel Cell Carcinoma|Metastatic Adrenal Gland Pheochromocytoma|Metastatic Carcinoid Tumor|Multiple Endocrine Neoplasia Type 1|Multiple Endocrine Neoplasia Type 2A|Multiple Endocrine Neoplasia Type 2B|Neuroendocrine Neoplasm|Non-Functional Pancreatic Neuroendocrine Tumor|Pancreatic Glucagonoma|Pancreatic Insulinoma|Recurrent Adrenal Cortex Carcinoma|Recurrent Adrenal Gland Pheochromocytoma|Recurrent Merkel Cell Carcinoma|Somatostatin-Producing Neuroendocrine Tumor|Stage III Adrenal Cortex Carcinoma|Stage III Thyroid Gland Medullary Carcinoma|Stage IIIA Merkel Cell Carcinoma|Stage IIIB Merkel Cell Carcinoma|Stage IV Adrenal Cortex Carcinoma|Stage IV Merkel Cell Carcinoma|Stage IVA Thyroid Gland Medullary Carcinoma|Stage IVB Thyroid Gland Medullary Carcinoma|Stage IVC Thyroid Gland Medullary Carcinoma|Thymic Carcinoid Tumor|VIP-Producing Neuroendocrine Tumor|Well Differentiated Adrenal Cortex Carcinoma|Zollinger Ellison Syndrome Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) December 2017 Phase 1
NCT03032614 Withdrawn Breast Cancer Stage IV|Ovarian Cancer|BRCA1 Mutation|BRCA2 Mutation The University of Texas Health Science Center at San Antonio September 30 2017 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID