Veliparib (ABT-888)

製品コードS1004 別名:NSC 737664

Veliparib (ABT-888)化学構造

分子量(MW):244.29

Veliparib (ABT-888) は一種の有効なPARP1とPARP2阻害剤で、無細胞試験でKi値が5.2 nM と2.9 nMに分かれて、SIRT2に活性を表しません。臨床3期。

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文献中の引用(40)

カスタマーフィードバック(9)

  • (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.

製品安全説明書

PARP阻害剤の選択性比較

生物活性

製品説明 Veliparib (ABT-888) は一種の有効なPARP1とPARP2阻害剤で、無細胞試験でKi値が5.2 nM と2.9 nMに分かれて、SIRT2に活性を表しません。臨床3期。
特性 Increases the efficacy of common cancer therapies such as radiation and alkylating agents.
ターゲット
PARP2 [1]
(Cell-free assay)
PARP1 [1]
(Cell-free assay)
2.9 nM(Ki) 5.2 nM(Ki)
体外試験

ABT-888 is inactive to SIRT2 (>5 μM). [1] ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells. [2] ABT-888 could decrease the PAR levels in both irradiated and nonirradiated H460 cells. ABT-888 also reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. ABT-888 increases apoptosis and autophagy in H460 cells when combination with radiation. [3] ABT-888 also inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. ABT-888 (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. ABT-888 shows effective radiosensitivity in oxic H1299 cells. Furthermore, ABT-888 could attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1. [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C41 NWrZbYFzU2mwYYPlJGF{e2G7 NWC4b4JzOzBibXnu MV7Jcohq[mm2aX;uJI9nKFCDUmCxJJdqfGhiRVO1NEBw\iByLkCwNkDPxE1? NX\oSmFwOTl6OEi3OlA>
Jurkat M{TNWWtqdmG|ZTDBd5NigQ>? M1HwWFk3KGh? NULOcY12TE2VTx?= Mk\uTY5pcWKrdHnvckBw\iCSQWLQNUBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gZ4VtdCC4aXHibYxqfHlid3n0bEBGSzVyIH;mJFMh|ryP NGD2VpgzOzh3MEG5PS=>
Capan1 NVr6O3RFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXBPHF3PzJiaB?= NIfpfnRFVVOR M1u4U2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRnJESTJiZ3Xu[UBufXSjdHXkJIh2dWGwIFPhdIFvOSClZXzsd{B4cXSqIFnDOVAhd2ZiM{muO{DPxE1? MkL3NlQ{QTh|OEO=
DT40 NHrCS2hEgXSxdH;4bYMhSXO|YYm= NEnjZYM4OiCq MWDEUXNQ MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBkcGmla3XuJGJTS0F{LXTl[olkcWWwdDDEWFQxKGOnbHzz NHLGVpczPDl{MkW4Oy=>
ML-1 MmO2RZBweHSxdHnjJGF{e2G7 MlHXNk42KM7:TR?= MU[yOEBp NV;BVXB[TE2VTx?= MmHRV5lv\XKpaYP0bYNidGy7IHXubIFv[2W|IGTSRWlNNWmwZIXj[YQh[XCxcITvd4l{KGmwIF3MMVEh[2WubIO= MXiyOFg6PTF|NR?=
HCT-116 NHnJXWJMcW6jc3WgRZN{[Xl? NX[3ZlVHOC53IN88US=> M{DEV|I1KGh? M2K0eXBCWlBiYXP0bZZqfHliZHXjdoVie2W| NVHrc5lKOjNyNUSyNVM>
UM-SCC1 Mlr5R5l1d3SxeHnjJGF{e2G7 MUixNEDPxE1? MmnNNlQhcA>? M{TL[3Jm\HWlZYOgeIhmKGOnbHygeoli[mmuaYT5 NUn6RXZLOjF7MUK2NlA>
FaDu MUPDfZRwfG:6aXOgRZN{[Xl? NITtN5cyOCEQvF2= M1e0dFI1KGh? NV32T5VwWmWmdXPld{B1cGViY3XscEB3cWGkaXzpeJk> MWSyNVkyOjZ{MB?=
PC-3 NXj0eY1GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXTNVAh|ryP MXrJcoR2[2W|IHGgd4lodmmoaXPhcpQhcW6qaXLpeIlwdiCrbjDjc4xwdnliZn;ycYF1cW:wwrC= M1O5TFIyPTdzOUGy
EoL-1-cell MkfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DXemlEPTB;MT6wO|k5KM7:TR?= M2L0R3NCVkeHUh?=
NCI-SNU-5 NUjr[olST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjZTWM2OD1|LkGyPFQyKM7:TR?= M4SyV3NCVkeHUh?=
BV-173 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfNTWM2OD13LkS1OFA6KM7:TR?= MVnTRW5ITVJ?
HCC1806 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrmOZhkUUN3ME21Mlc2OTd|IN88US=> MkXvV2FPT0WU
COLO-680 MojxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;EWllKSzVyPU[uNlE1ODZizszN MlqxV2FPT0WU
HCC2218 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojvTWM2OD15Lke5O|A1KM7:TR?= NH7yOXBUSU6JRWK=
SK-MEL-24 MljSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PRNGlEPTB;Nz64NVkzPCEQvF2= MXnTRW5ITVJ?
NCI-H720 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\GO2lEPTB;OD60N|YxOyEQvF2= MXLTRW5ITVJ?
KASUMI-1 NF7EcY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\WdpNKSzVyPUiuPFkzPjZizszN MXfTRW5ITVJ?
HAL-01 MkT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLBTWM2OD17Lki4OlIh|ryP M3m4cHNCVkeHUh?=
CAL-33 Mof5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\HfGlEPTB;MUCuOFM1KM7:TR?= NHuwTVFUSU6JRWK=
SK-MEL-1 M3Ho[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTF{LkS2OlMh|ryP MVLTRW5ITVJ?
Ramos-2G6-4C10 NVrqUG14T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\ZZmlEPTB;MUKuOFc2OiEQvF2= M3PrenNCVkeHUh?=
KY821 M1;TPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33aXWlEPTB;MUKuOFg2KM7:TR?= M1fZ[XNCVkeHUh?=
HEC-1 Mn\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;Fd|lGUUN3ME2xNk46OTl4IN88US=> NFzQXYFUSU6JRWK=
SK-NEP-1 M3;ySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[0UXIxUUN3ME2xN{4yPjZizszN NEGye2ZUSU6JRWK=
MN-60 NXfESHNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrCTWM2OD1zMz61N|g6KM7:TR?= MXHTRW5ITVJ?
DU-145 Mn;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPwTWM2OD1zMz65NFU{KM7:TR?= MWTTRW5ITVJ?
EW-3 M1G3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV2w[Ws4UUN3ME2xOE42PTZ3IN88US=> M4K5TXNCVkeHUh?=
OS-RC-2 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fNUGlEPTB;MUWuPVU5QSEQvF2= M37jfXNCVkeHUh?=
RPMI-8226 NHraWWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfkTlNKSzVyPUG2MlIxPDJizszN M3vqeHNCVkeHUh?=
ChaGo-K-1 MliyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWL5PHhTUUN3ME2xOk42OzJ3IN88US=> NGnxPHJUSU6JRWK=
DEL NVzVbm92T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTF4Lk[3NVch|ryP NHu2RmZUSU6JRWK=
GP5d MlraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mli5TWM2OD1zNz6wOVMh|ryP NWTrWWg1W0GQR1XS
COLO-668 M4LQOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;RNHBKSzVyPUG3MlYzQTRizszN MYrTRW5ITVJ?
H9 NFfYZ4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVizV4szUUN3ME2xPE4zQDN|IN88US=> NGHsbYhUSU6JRWK=
NKM-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTF6LkWxNVkh|ryP NGrrdZlUSU6JRWK=
KYSE-150 NFnHRYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLZToVKSzVyPUG4Mlk6QDZizszN MkThV2FPT0WU
Daoy Mo\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTF7LkW2OFkh|ryP M{K0S3NCVkeHUh?=
ECC10 MlrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTJyLke0OVUh|ryP NGnBfYdUSU6JRWK=
A388 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\HU4RKSzVyPUKxMlkxQTFizszN MYnTRW5ITVJ?
MHH-NB-11 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\QTWlEPTB;MkOuNVM3OyEQvF2= NF3sNG5USU6JRWK=
HCC1937 NVjVUG12T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml24TWM2OD1{ND63OFYh|ryP MWPTRW5ITVJ?
TGBC11TKB M3\0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfuc5hLUUN3ME2yOU43QDZ|IN88US=> MX\TRW5ITVJ?
CTV-1 M{ixT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\TNIxKSzVyPUK1Mlg6PjlizszN NVjXR3VZW0GQR1XS
NCI-H2029 M2jaVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIKx[WZKSzVyPUK2MlQzOzhizszN NEX5[XhUSU6JRWK=
HLE MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4q0[2lEPTB;MkeuNFU1KM7:TR?= NFfGd2hUSU6JRWK=
NCI-H1693 M1T0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTJ5LkK4PVgh|ryP Mki5V2FPT0WU
HCC70 MkXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1znb2lEPTB;MkeuO|I1PiEQvF2= MkDkV2FPT0WU
BEN Mn3lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTJ5Lkm1OlYh|ryP NHrSbopUSU6JRWK=
LB771 NY\0VFZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17UZmlEPTB;MkiuPFM4OyEQvF2= MorQV2FPT0WU
697 MoK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHqfXZKSzVyPUK5MlAzOzVizszN M2i5bnNCVkeHUh?=
LU-139 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrSTWM2OD1{OT6zO|Q5KM7:TR?= MlvFV2FPT0WU
EW-13 Ml;3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjWVVFKSzVyPUK5MlM5OTRizszN MYjTRW5ITVJ?
MOLT-13 NF;mdGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzrVWlIUUN3ME2yPU4{QDF2IN88US=> NW\RUZZLW0GQR1XS
L-363 NI\ZWIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUG3RoFKUUN3ME2yPU41Pzl6IN88US=> NVTjO45{W0GQR1XS
EM-2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnsNFRCUUN3ME2yPU41QTBzIN88US=> NXuwdXRIW0GQR1XS
RS4-11 NG\TZ|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{H4bWlEPTB;M{CuOFI1OSEQvF2= MVvTRW5ITVJ?
A2780 M3G1[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTNTWM2OD1|MD63OFU4KM7:TR?= M2HrbHNCVkeHUh?=
KU812 NGHadXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzlTWM2OD1|Mj6zOlQzKM7:TR?= MkXJV2FPT0WU
COLO-684 NH22WpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTN|LkO1PVkh|ryP NGjJR5BUSU6JRWK=
MFE-280 MknQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPhTWM2OD1|Mz6zPFg6KM7:TR?= NHGyZZhUSU6JRWK=
KG-1 Ml;MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jkVGlEPTB;M{OuOlAxOSEQvF2= MYLTRW5ITVJ?
JVM-3 NGP0U|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXmydYc5UUN3ME2zOU42QDZ6IN88US=> M4TRTXNCVkeHUh?=
MV-4-11 NHv6RnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTN3Lki0PVkh|ryP M3LvO3NCVkeHUh?=
LAMA-84 M3fNdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTpUIpFUUN3ME2zOk44OzR3IN88US=> NEDac3JUSU6JRWK=
MOLT-16 NEWzdopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHiTWM2OD1|Nj65OVIh|ryP M{TRWHNCVkeHUh?=
H4 MkX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTiZWhKSzVyPUO3MlU3PyEQvF2= M1v2e3NCVkeHUh?=
T47D NXf0Xoo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TzdWlEPTB;M{euO|AyQCEQvF2= MoPXV2FPT0WU
CAL-54 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DqTGlEPTB;M{euPVY3KM7:TR?= NVH5[mhLW0GQR1XS
SW982 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rMZ2lEPTB;M{iuNFk6QCEQvF2= MWLTRW5ITVJ?
IGROV-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLHTWM2OD1|OT6zN|A1KM7:TR?= NGPOS|JUSU6JRWK=
NB14 MoDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\OSWlEPTB;NECuO|A{OSEQvF2= M3fzenNCVkeHUh?=
HCC1187 M1;qeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL6WGszUUN3ME20NU4zPzdzIN88US=> NEjiUJdUSU6JRWK=
SBC-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUCzSWlzUUN3ME20NU4{ODZ|IN88US=> M1rOTHNCVkeHUh?=
KARPAS-45 M{PyZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTRzLkS4NVgh|ryP NEX0SnRUSU6JRWK=
MOLT-4 NYKxRo51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnaSFlIUUN3ME20Nk4zPTN6IN88US=> MkTBV2FPT0WU
JVM-2 NHmycIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULZSJBlUUN3ME20Nk46OjB5IN88US=> NHjZN2tUSU6JRWK=
A4-Fuk MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\te2lEPTB;NEOuOVY6OSEQvF2= MkO3V2FPT0WU
MDA-MB-361 NHHtd5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2T3cGlEPTB;NEOuPFQyPCEQvF2= NGDlZZRUSU6JRWK=
BALL-1 M4\SW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2e3e2lEPTB;NEOuPVU{OiEQvF2= Ml;6V2FPT0WU
T98G NEjxSphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnjRmNsUUN3ME20OE45PTF5IN88US=> NHu1[G9USU6JRWK=
Mo-T MmPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTXNmR1UUN3ME20OU43Ozh7IN88US=> MlT6V2FPT0WU
MHH-PREB-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTR3Lke1PFUh|ryP NV\ZPXJuW0GQR1XS
ALL-PO NYjnc4xHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\pTWM2OD12Nz6zO|kyKM7:TR?= M2DuSXNCVkeHUh?=
NCI-H510A Mmm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4L2XGlEPTB;NEeuPVA{PCEQvF2= MWfTRW5ITVJ?
ML-2 NFfIT4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\PVnkyUUN3ME20PU44QDV4IN88US=> NXfIWpVQW0GQR1XS

多くの細胞株試験データを見る場合、クリックしてください

体内試験 The oral bioavailability of ABT-888 is 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys after oral administration. [1] ABT-888 (25 mg/kg i.p.) could improve tumor growth delay in a NCI-H460 xenograft model with well tolerated. Combination with radiation, ABT-888 decreases the tumor vessel formation. [3] ABT-888 reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg in A375 and Colo829 xenograft models and the suppression could be maintained over time. [4]

お薦めの試験操作(参考用のみ)

動物試験:

[1]

+ 展開
  • 動物モデル: NCI-H460, H460, B16F10 and 9L xenografts in C57BL/6 mice
  • 製剤: Formulated in solution containing 0.9% NaCl adjusted to pH 4.0
  • 投薬量: ~25 mg/kg
  • 投与方法: Orally administered
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 17 mg/mL (69.58 mM)
Water slightly soluble or insoluble
Ethanol slightly soluble or insoluble
体内 順序で溶剤を入れること:
0.5% methylcellulose+0.2% Tween 80
5 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 244.29
化学式

C13H16N4O

CAS No. 912444-00-9
保管
in solvent
別名 NSC 737664

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID