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 MnLaT4lv[XOnIFHzd4F6 MWSzNEBucW5? MYXJcohq[mm2aX;uJI9nKFCDUmCxJJdqfGhiRVO1NEBw\iByLkCwNkDPxE1? Mn;6NVk5QDh5NkC=
Jurkat MX;LbY5ie2ViQYPzZZk> NIHkOVQ6PiCq NGLON2lFVVOR NFrZd3VKdmirYnn0bY9vKG:oIGDBVnAyKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBk\WyuII\pZYJqdGm2eTD3bZRpKEWFNUCgc4YhOyEQvF2= MnvINlM5PTBzOUm=
Capan1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zhe|czKGh? M3HVemROW09? MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFLSR2EzKGenbnWgcZV1[XSnZDDoeY1idiCFYYDhclEh[2WubIOge4l1cCCLQ{WwJI9nKDN7Lkeg{txO NHHUR5ozPDN7OEO4Ny=>
DT40 M1XkfmN6fG:2b4jpZ{BCe3OjeR?= M4TzWFczKGh? NF7FWZlFVVOR NHzJbXFEgXSxdH;4bYNqfHliYXfhbY5{fCClaHnjb4VvKEKUQ1GyMYRm\mmlaXXueEBFXDRyIHPlcIx{ Ml;0NlQ6OjJ3OEe=
ML-1 MVfBdI9xfG:2aXOgRZN{[Xl? NH:xUHYzNjVizszN M3i2SlI1KGh? MV\EUXNQ M{fEUXN6dmW{Z3nzeIlk[WyueTDlcohidmOnczDUVmFKVC2rbnT1Z4VlKGGyb4D0c5NqeyCrbjDNUE0yKGOnbHzz NVz3WYY5OjR6OUWxN|U>
HCT-116 NWXobHo5U2mwYYPlJGF{e2G7 MWCwMlUh|ryP M2q5O|I1KGh? M1G5b3BCWlBiYXP0bZZqfHliZHXjdoVie2W| NYTsU3I2OjNyNUSyNVM>
UM-SCC1 MVzDfZRwfG:6aXOgRZN{[Xl? NH;pU2gyOCEQvF2= MV:yOEBp Mmr2VoVlfWOnczD0bIUh[2WubDD2bYFjcWyrdIm= M1XJdFIyQTF{NkKw
FaDu MkCxR5l1d3SxeHnjJGF{e2G7 NWHWV4R7OTBizszN NUnzT45zOjRiaB?= NUTOeI5MWmWmdXPld{B1cGViY3XscEB3cWGkaXzpeJk> MX:yNVkyOjZ{MB?=
PC-3 M4rSZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHCSY1QOTBizszN NH7mVZNKdmS3Y3XzJIEhe2mpbnnmbYNidnRiaX7obYJqfGmxbjDpckBkd2yxbomg[o9zdWG2aX;uxsA> NH;WZ5czOTV5MUmxNi=>
EoL-1-cell NYryXHFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTFwMEe5PEDPxE1? MXfTRW5ITVJ?
NCI-SNU-5 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PtXGlEPTB;Mz6xNlg1OSEQvF2= M2HZcHNCVkeHUh?=
BV-173 MlPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTVwNEW0NFkh|ryP NGDYSGNUSU6JRWK=
HCC1806 NXj5TnpCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTVwN{WxO|Mh|ryP M{f4eXNCVkeHUh?=
COLO-680 MnPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrsb2FKSzVyPU[uNlE1ODZizszN MXLTRW5ITVJ?
HCC2218 MnvTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXqTWM2OD15Lke5O|A1KM7:TR?= MnHIV2FPT0WU
SK-MEL-24 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnu1TWM2OD15LkixPVI1KM7:TR?= M4WxNnNCVkeHUh?=
NCI-H720 NH:1PHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPITWM2OD16LkSzOlA{KM7:TR?= NHXPcFVUSU6JRWK=
KASUMI-1 M1fp[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHwNJNKSzVyPUiuPFkzPjZizszN Mom4V2FPT0WU
HAL-01 NWHSZVAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rITGlEPTB;OT64PFYzKM7:TR?= NXTE[lF3W0GQR1XS
CAL-33 NYfTb3FFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTFyLkSzOEDPxE1? MlfRV2FPT0WU
SK-MEL-1 NGjGW5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTF{LkS2OlMh|ryP NUHZfopuW0GQR1XS
Ramos-2G6-4C10 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHJT2NwUUN3ME2xNk41PzV{IN88US=> MVjTRW5ITVJ?
KY821 NYX5e4czT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moj4TWM2OD1zMj60PFUh|ryP M3f3NnNCVkeHUh?=
HEC-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TaVmlEPTB;MUKuPVE6PiEQvF2= MlnVV2FPT0WU
SK-NEP-1 NH7JfnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PndWlEPTB;MUOuNVY3KM7:TR?= M3nheXNCVkeHUh?=
MN-60 NYexNoZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPYcVZNUUN3ME2xN{42Ozh7IN88US=> Mmr0V2FPT0WU
DU-145 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rJN2lEPTB;MUOuPVA2OyEQvF2= MXnTRW5ITVJ?
EW-3 NUXV[W5pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTF2LkW1OlUh|ryP NEDJRmxUSU6JRWK=
OS-RC-2 MkX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHRTWM2OD1zNT65OVg6KM7:TR?= M{LGUXNCVkeHUh?=
RPMI-8226 Mk\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTF4LkKwOFIh|ryP M{C4NHNCVkeHUh?=
ChaGo-K-1 M4S2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonFTWM2OD1zNj61N|I2KM7:TR?= MUHTRW5ITVJ?
DEL MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIP0WXdKSzVyPUG2MlY4OTdizszN MmnxV2FPT0WU
GP5d M{jCO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTF5LkC1N{DPxE1? NWnp[VRQW0GQR1XS
COLO-668 M4ToSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDKR4JnUUN3ME2xO{43Ojl2IN88US=> NEHNdWFUSU6JRWK=
H9 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljsTWM2OD1zOD6yPFM{KM7:TR?= NGLjeJVUSU6JRWK=
NKM-1 M3naOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXab5RKSzVyPUG4MlUyOTlizszN MY\TRW5ITVJ?
KYSE-150 NYf0fHhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTF6Lkm5PFYh|ryP NIfQbYFUSU6JRWK=
Daoy NGHkZ3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTF7LkW2OFkh|ryP M{nxdHNCVkeHUh?=
ECC10 MnzIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zmSGlEPTB;MkCuO|Q2PSEQvF2= MV;TRW5ITVJ?
A388 Ml3lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\sS2lEPTB;MkGuPVA6OSEQvF2= Mly4V2FPT0WU
MHH-NB-11 MnnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vZS2lEPTB;MkOuNVM3OyEQvF2= M4n1OnNCVkeHUh?=
HCC1937 MoO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjQW2pKSzVyPUK0Mlc1PiEQvF2= Ml3zV2FPT0WU
TGBC11TKB NEX5[YpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDC[VZKSzVyPUK1MlY5PjNizszN MojXV2FPT0WU
CTV-1 MmO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTJ3Lki5Olkh|ryP NH33bXRUSU6JRWK=
NCI-H2029 MmDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml65TWM2OD1{Nj60NlM5KM7:TR?= MnLLV2FPT0WU
HLE MkHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXUR4NKSzVyPUK3MlA2PCEQvF2= NGfE[lFUSU6JRWK=
NCI-H1693 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLFTWM2OD1{Nz6yPFk5KM7:TR?= MY\TRW5ITVJ?
HCC70 NYfVVZhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\iW|Z1UUN3ME2yO{44OjR4IN88US=> NIfocFlUSU6JRWK=
BEN NUC1bmVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LZUGlEPTB;MkeuPVU3PiEQvF2= MUHTRW5ITVJ?
LB771 Mln4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEf1Xo9KSzVyPUK4Mlg{PzNizszN NFnqemVUSU6JRWK=
697 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm[yTWM2OD1{OT6wNlM2KM7:TR?= NFLUTI9USU6JRWK=
LU-139 NUjFT5pLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorsTWM2OD1{OT6zO|Q5KM7:TR?= M2D6PXNCVkeHUh?=
EW-13 M3HqWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:2XWJJUUN3ME2yPU4{QDF2IN88US=> NFvaUGFUSU6JRWK=
MOLT-13 NYTCfol6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHsV3RnUUN3ME2yPU4{QDF2IN88US=> MUfTRW5ITVJ?
L-363 NFfPcnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmmxTWM2OD1{OT60O|k5KM7:TR?= MUjTRW5ITVJ?
EM-2 M3TUPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTJ7LkS5NFEh|ryP MmXNV2FPT0WU
RS4-11 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LtTGlEPTB;M{CuOFI1OSEQvF2= M3nLPHNCVkeHUh?=
A2780 MoHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjRVJY3UUN3ME2zNE44PDV5IN88US=> NWrLU4t5W0GQR1XS
KU812 NUHn[ZFRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTN{LkO2OFIh|ryP NI\GZYZUSU6JRWK=
COLO-684 MonlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXzT242UUN3ME2zN{4{PTl7IN88US=> NUi5TFVtW0GQR1XS
MFE-280 M3zVR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTN|LkO4PFkh|ryP NYn4c2lHW0GQR1XS
KG-1 MkDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnmNWVYUUN3ME2zN{43ODBzIN88US=> M1rmT3NCVkeHUh?=
JVM-3 NVP0VnpFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkmzTWM2OD1|NT61PFY5KM7:TR?= NGHBdJZUSU6JRWK=
MV-4-11 NVvveFlOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGD1[ZZKSzVyPUO1Mlg1QTlizszN M2jhXnNCVkeHUh?=
LAMA-84 NHPjUoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTN4LkezOFUh|ryP M1fCfnNCVkeHUh?=
MOLT-16 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTN4Lkm1NkDPxE1? NGG1ZlhUSU6JRWK=
H4 M2DmS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILPV|JKSzVyPUO3MlU3PyEQvF2= NX;Ie45zW0GQR1XS
T47D NWi5TWh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL1TWM2OD1|Nz63NFE5KM7:TR?= MlzPV2FPT0WU
CAL-54 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTN5Lkm2OkDPxE1? MX;TRW5ITVJ?
SW982 M1PPWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTN6LkC5PVgh|ryP MUXTRW5ITVJ?
IGROV-1 NG\FT29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLabW5RUUN3ME2zPU4{OzB2IN88US=> NHTofZFUSU6JRWK=
NB14 NV7Xc4YzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HkSGlEPTB;NECuO|A{OSEQvF2= NFfxcVRUSU6JRWK=
HCC1187 NHrCZWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnsc45EUUN3ME20NU4zPzdzIN88US=> MUfTRW5ITVJ?
SBC-1 NI\YW3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;3SIFKSzVyPUSxMlMxPjNizszN NGK3NnlUSU6JRWK=
KARPAS-45 M3mweWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;FZ2o5UUN3ME20NU41QDF6IN88US=> M2HyNHNCVkeHUh?=
MOLT-4 MmS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mof0TWM2OD12Mj6yOVM5KM7:TR?= M3LQVHNCVkeHUh?=
JVM-2 NVzqN2xvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWqwc2VuUUN3ME20Nk46OjB5IN88US=> MljVV2FPT0WU
A4-Fuk NVfQfohxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLDTWM2OD12Mz61OlkyKM7:TR?= M1nRfHNCVkeHUh?=
MDA-MB-361 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTkdFZKSzVyPUSzMlg1OTRizszN M1LjWHNCVkeHUh?=
BALL-1 NFrkWo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTR|Lkm1N|Ih|ryP M3u2VnNCVkeHUh?=
T98G MonqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnexTWM2OD12ND64OVE4KM7:TR?= M{\4R3NCVkeHUh?=
Mo-T MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIT5XpNKSzVyPUS1MlY{QDlizszN MYXTRW5ITVJ?
MHH-PREB-1 NYXRSmx1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nJNGlEPTB;NEWuO|U5PSEQvF2= NYflOYJtW0GQR1XS
ALL-PO Moq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGK1dFdKSzVyPUS3MlM4QTFizszN NIPFTVhUSU6JRWK=
NCI-H510A NWixUlQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLxWo45UUN3ME20O{46ODN2IN88US=> MXrTRW5ITVJ?
ML-2 NFP2PJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DyZWlEPTB;NEmuO|g2PiEQvF2= MV;TRW5ITVJ?

... 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:
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
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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PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID