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 Mlr6T4lv[XOnIFHzd4F6 NYW5SWFoOzBibXnu MkCwTY5pcWKrdHnvckBw\iCSQWLQNUB4cXSqIFXDOVAhd2ZiMD6wNFIh|ryP M1HW[|E6QDh6N{[w
Jurkat MVPLbY5ie2ViQYPzZZk> MUG5OkBp M{HwTmROW09? NIW1T4hKdmirYnn0bY9vKG:oIGDBVnAyKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBk\WyuII\pZYJqdGm2eTD3bZRpKEWFNUCgc4YhOyEQvF2= MlPBNlM5PTBzOUm=
Capan1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXi3NkBp MU\EUXNQ M1m4VmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRnJESTJiZ3Xu[UBufXSjdHXkJIh2dWGwIFPhdIFvOSClZXzsd{B4cXSqIFnDOVAhd2ZiM{muO{DPxE1? NELqXpgzPDN7OEO4Ny=>
DT40 NGXkSo5EgXSxdH;4bYMhSXO|YYm= Mme5O|IhcA>? M4PuSWROW09? NWrJWJpjS3m2b4TvfIlkcXS7IHHnZYlve3RiY3jpZ4tmdiCEUlPBNk1l\W[rY3nlcpQhTFR2MDDj[Yxtew>? M4DSXVI1QTJ{NUi3
ML-1 NU\CcWZwSXCxcITveIlkKEG|c3H5 MWiyMlUh|ryP MoDNNlQhcA>? NXrMcIFyTE2VTx?= NET5e|RUgW6ncnfpd5Rq[2GubImg[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXNiaX6gUWwuOSClZXzsdy=> MWWyOFg6PTF|NR?=
HCT-116 MU\LbY5ie2ViQYPzZZk> MlK5NE42KM7:TR?= NUTGTHpZOjRiaB?= MXXQRXJRKGGldHn2bZR6KGSnY4LlZZNmew>? M2jMXlI{ODV2MkGz
UM-SCC1 NUnvZYM4S3m2b4TvfIlkKEG|c3H5 MXWxNEDPxE1? M1r6[lI1KGh? NHvERVdT\WS3Y3XzJJRp\SClZXzsJJZq[WKrbHn0fS=> NIfzOVUzOTlzMk[yNC=>
FaDu NV7qU3NnS3m2b4TvfIlkKEG|c3H5 MYixNEDPxE1? MV[yOEBp NFiyUnpT\WS3Y3XzJJRp\SClZXzsJJZq[WKrbHn0fS=> M2qxWVIyQTF{NkKw
PC-3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\mVlZGOTBizszN MnjITY5lfWOnczDhJJNq\26rZnnjZY51KGmwaHnibZRqd25iaX6gZ49td267IH\vdo1ifGmxbtMg NV\aeXUyOjF3N{G5NVI>
EoL-1-cell NFfJfI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPCTWM2OD1zLkC3PVgh|ryP MWrTRW5ITVJ?
NCI-SNU-5 M1faOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPFTWM2OD1|LkGyPFQyKM7:TR?= MXrTRW5ITVJ?
BV-173 NX3FOIZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTVwNEW0NFkh|ryP NIXGXopUSU6JRWK=
HCC1806 NXvSVnZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTVdXBKSzVyPUWuO|UyPzNizszN MXnTRW5ITVJ?
COLO-680 M1O3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTZwMkG0NFYh|ryP NFn5SZdUSU6JRWK=
HCC2218 NFLXSJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vZVWlEPTB;Nz63PVcxPCEQvF2= NEnncGpUSU6JRWK=
SK-MEL-24 MojUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTdwOEG5NlQh|ryP Ml\UV2FPT0WU
NCI-H720 M{\xeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfQTWM2OD16LkSzOlA{KM7:TR?= MWrTRW5ITVJ?
KASUMI-1 M2DD[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn6wTWM2OD16Lki5NlY3KM7:TR?= Mn3jV2FPT0WU
HAL-01 NXHibnhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTlwOEi2NkDPxE1? NF20XnZUSU6JRWK=
CAL-33 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlKzTWM2OD1zMD60N|Qh|ryP M4rYTnNCVkeHUh?=
SK-MEL-1 NH7hUm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXjflBKSzVyPUGyMlQ3PjNizszN NVXP[osxW0GQR1XS
Ramos-2G6-4C10 M3fZcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTF{LkS3OVIh|ryP M1y4dHNCVkeHUh?=
KY821 M3vzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTF{LkS4OUDPxE1? NFL3W2ZUSU6JRWK=
HEC-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDleHRSUUN3ME2xNk46OTl4IN88US=> MUjTRW5ITVJ?
SK-NEP-1 MkX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjE[YFKSzVyPUGzMlE3PiEQvF2= MVXTRW5ITVJ?
MN-60 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moe4TWM2OD1zMz61N|g6KM7:TR?= NWr4bY1LW0GQR1XS
DU-145 MoXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHh[YdKSzVyPUGzMlkxPTNizszN Ml\QV2FPT0WU
EW-3 M3HMbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:0O2lEPTB;MUSuOVU3PSEQvF2= M1G4bHNCVkeHUh?=
OS-RC-2 NGmzcXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTPTWM2OD1zNT65OVg6KM7:TR?= NIrEZ3ZUSU6JRWK=
RPMI-8226 NGXTVI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{[4OWlEPTB;MU[uNlA1OiEQvF2= NWHvcodNW0GQR1XS
ChaGo-K-1 MkeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPaTWM2OD1zNj61N|I2KM7:TR?= NXTzcJlmW0GQR1XS
DEL M3q0VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPuXVNPUUN3ME2xOk43PzF5IN88US=> NIHWXJRUSU6JRWK=
GP5d MljzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M374RmlEPTB;MUeuNFU{KM7:TR?= MVPTRW5ITVJ?
COLO-668 M3XRSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTF5Lk[yPVQh|ryP MVvTRW5ITVJ?
H9 NVPhe4w2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknBTWM2OD1zOD6yPFM{KM7:TR?= M37IVXNCVkeHUh?=
NKM-1 M1zhfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnRTWM2OD1zOD61NVE6KM7:TR?= NUTURXFPW0GQR1XS
KYSE-150 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrLeWhKSzVyPUG4Mlk6QDZizszN NGHvS49USU6JRWK=
Daoy MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\1TWFKSzVyPUG5MlU3PDlizszN NFPpOFZUSU6JRWK=
ECC10 NEnXbGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTJyLke0OVUh|ryP MXLTRW5ITVJ?
A388 NHTpcmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLBOGRKSzVyPUKxMlkxQTFizszN NIryOGRUSU6JRWK=
MHH-NB-11 MmnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnFWJlKSzVyPUKzMlE{PjNizszN MXLTRW5ITVJ?
HCC1937 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M160V2lEPTB;MkSuO|Q3KM7:TR?= M13PTXNCVkeHUh?=
TGBC11TKB MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTJ3Lk[4OlMh|ryP MlLqV2FPT0WU
CTV-1 M3rnbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rwc2lEPTB;MkWuPFk3QSEQvF2= NY\NT2VRW0GQR1XS
NCI-H2029 M3PQSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTJ4LkSyN|gh|ryP M1jJcHNCVkeHUh?=
HLE NYLNRpBNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILSW3RKSzVyPUK3MlA2PCEQvF2= NFrsVHpUSU6JRWK=
NCI-H1693 NYfndIJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYC1SVZ1UUN3ME2yO{4zQDl6IN88US=> MnfGV2FPT0WU
HCC70 M{HMemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33aSGlEPTB;MkeuO|I1PiEQvF2= M3v2cnNCVkeHUh?=
BEN M4P4V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTJ5Lkm1OlYh|ryP M2nvWHNCVkeHUh?=
LB771 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTJ6LkizO|Mh|ryP MWjTRW5ITVJ?
697 MkjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjCTWM2OD1{OT6wNlM2KM7:TR?= MkDPV2FPT0WU
LU-139 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYH4bHhqUUN3ME2yPU4{PzR6IN88US=> M4LrbXNCVkeHUh?=
EW-13 M3\nZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1q5TmlEPTB;MkmuN|gyPCEQvF2= MmfOV2FPT0WU
MOLT-13 NX[4bWhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTJ7LkO4NVQh|ryP Mmm5V2FPT0WU
L-363 MonDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTJ7LkS3PVgh|ryP M2HXZXNCVkeHUh?=
EM-2 NEWyVGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\4dGlEPTB;MkmuOFkxOSEQvF2= NFu3T5ZUSU6JRWK=
RS4-11 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPoTpZKSzVyPUOwMlQzPDFizszN NYjV[oFxW0GQR1XS
A2780 MmTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\hTWM2OD1|MD63OFU4KM7:TR?= NGnGRWFUSU6JRWK=
KU812 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{L3RmlEPTB;M{KuN|Y1OiEQvF2= M{PQOnNCVkeHUh?=
COLO-684 Mo\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zuRWlEPTB;M{OuN|U6QSEQvF2= MYDTRW5ITVJ?
MFE-280 M1:2dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHYTWM2OD1|Mz6zPFg6KM7:TR?= MWLTRW5ITVJ?
KG-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTN|Lk[wNFEh|ryP NVG5SIRDW0GQR1XS
JVM-3 MlvRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVP3eVVHUUN3ME2zOU42QDZ6IN88US=> Mk\OV2FPT0WU
MV-4-11 NUXzN41HT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLXVXlSUUN3ME2zOU45PDl7IN88US=> NHfrNlNUSU6JRWK=
LAMA-84 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7jTWM2OD1|Nj63N|Q2KM7:TR?= NGXNbVdUSU6JRWK=
MOLT-16 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fBVGlEPTB;M{[uPVUzKM7:TR?= M361XXNCVkeHUh?=
H4 MojSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3IZ3BKSzVyPUO3MlU3PyEQvF2= M2HqU3NCVkeHUh?=
T47D M37LSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTN5LkewNVgh|ryP MYTTRW5ITVJ?
CAL-54 NVf2clZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfFUmliUUN3ME2zO{46PjZizszN Mm\vV2FPT0WU
SW982 NGjZ[ZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTN6LkC5PVgh|ryP Ml;RV2FPT0WU
IGROV-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\ldGlEPTB;M{muN|MxPCEQvF2= MoTIV2FPT0WU
NB14 NGDUWpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWG0PYttUUN3ME20NE44ODNzIN88US=> M2rUN3NCVkeHUh?=
HCC1187 MoXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nJUWlEPTB;NEGuNlc4OSEQvF2= M1LBbnNCVkeHUh?=
SBC-1 NUfhdlNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljuTWM2OD12MT6zNFY{KM7:TR?= NH\kUopUSU6JRWK=
KARPAS-45 MnzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHQW4U1UUN3ME20NU41QDF6IN88US=> MYfTRW5ITVJ?
MOLT-4 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPQTWM2OD12Mj6yOVM5KM7:TR?= M2nRenNCVkeHUh?=
JVM-2 M3vo[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTCc5ZiUUN3ME20Nk46OjB5IN88US=> M1jONHNCVkeHUh?=
A4-Fuk M3;qWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jyZmlEPTB;NEOuOVY6OSEQvF2= MUHTRW5ITVJ?
MDA-MB-361 NH3nUHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PxZWlEPTB;NEOuPFQyPCEQvF2= NWrWfFFZW0GQR1XS
BALL-1 NGn1PJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITpZXFKSzVyPUSzMlk2OzJizszN Mo\FV2FPT0WU
T98G NH;uc3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHQTWZKSzVyPUS0Mlg2OTdizszN NVz4SnBLW0GQR1XS
Mo-T NV\MSppMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LWfWlEPTB;NEWuOlM5QSEQvF2= M{DHOHNCVkeHUh?=
MHH-PREB-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjpNJNKSzVyPUS1Mlc2QDVizszN MoTVV2FPT0WU
ALL-PO M{DoXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknzTWM2OD12Nz6zO|kyKM7:TR?= MYTTRW5ITVJ?
NCI-H510A NInJeWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TPXWlEPTB;NEeuPVA{PCEQvF2= M2fRXXNCVkeHUh?=
ML-2 NXTjO3JsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\aOHJiUUN3ME20PU44QDV4IN88US=> NWj5RW1nW0GQR1XS

... 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 从左到右依次加入纯溶剂:
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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PARP Signaling Pathway Map

PARP Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID