Veliparib (ABT-888) 化学構造
分子量: 244.29

高品質保証

文献中の引用(39)

カスタマーフィードバック(9)

MSDS

製品説明

  • Compare PARP Inhibitors
    PARP製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • Veliparib (ABT-888)のメカニズム

製品の説明

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。
ターゲット

PARP1

PARP2

IC50

5.2 nM (Ki)

2.9 nM (Ki) [1]

In vitro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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
C41 M3nEZWtqdmG|ZTDBd5NigQ>? NF3wW5E{OCCvaX6= MYLJcohq[mm2aX;uJI9nKFCDUmCxJJdqfGhiRVO1NEBw\iByLkCwNkDPxE1? M4\Se|E6QDh6N{[w
Jurkat Mlz0T4lv[XOnIFHzd4F6 MlvkPVYhcA>? MVXEUXNQ NWji[HkyUW6qaXLpeIlwdiCxZjDQRXJROSCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4Yh[2WubDD2bYFjcWyrdImge4l1cCCHQ{WwJI9nKDNizszN NFq3NJMzOzh3MEG5PS=>
Capan1 M2DyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3K2dlczKGh? NF;G[lJFVVOR MnjMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDCVmNCOiCpZX7lJI12fGG2ZXSgbJVu[W5iQ3HwZY4yKGOnbHzzJJdqfGhiSVO1NEBw\iB|OT63JO69VQ>? MVyyOFM6QDN6Mx?=
DT40 Mk[3R5l1d3SxeHnjJGF{e2G7 NFXGSo44OiCq MnXDSG1UVw>? MVjDfZRwfG:6aXPpeJkh[WejaX7zeEBkcGmla3XuJGJTS0F{LXTl[olkcWWwdDDEWFQxKGOnbHzz MVmyOFkzOjV6Nx?=
ML-1 M2DUUWFxd3C2b4TpZ{BCe3OjeR?= NHXUeXkzNjVizszN MlPSNlQhcA>? M3jCPGROW09? MV\TfY5memerc4TpZ4FtdHliZX7oZY5k\XNiVGLBTWwucW6mdXPl[EBieG:ydH;zbZMhcW5iTVytNUBk\Wyucx?= MWKyOFg6PTF|NR?=
HCT-116 Mk\pT4lv[XOnIFHzd4F6 NEPzPXQxNjVizszN NXvWO2JbOjRiaB?= NUTpfFNKWEGUUDDhZ5Rqfmm2eTDk[YNz\WG|ZYO= NFHYeZEzOzB3NEKxNy=>
UM-SCC1 MXrDfZRwfG:6aXOgRZN{[Xl? NVPZR4JyOTBizszN MYOyOEBp NWe5Z214WmWmdXPld{B1cGViY3XscEB3cWGkaXzpeJk> MkizNlE6OTJ4MkC=
FaDu MVPDfZRwfG:6aXOgRZN{[Xl? NWfLS2FiOTBizszN MnjGNlQhcA>? MYjS[YR2[2W|IITo[UBk\WyuII\pZYJqdGm2eR?= NYT4OVZiOjF7MUK2NlA>
PC-3 MnvjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHLc3dCOTBizszN MmTZTY5lfWOnczDhJJNq\26rZnnjZY51KGmwaHnibZRqd25iaX6gZ49td267IH\vdo1ifGmxbtMg M1n5e|IyPTdzOUGy
EoL-1-cell M1THfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Pp[2lEPTB;MT6wO|k5KM7:TR?= MlPnV2FPT0WU
NCI-SNU-5 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfvSGlZUUN3ME2zMlEzQDRzIN88US=> NV7EPIk2W0GQR1XS
BV-173 NGr2PWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTVwNEW0NFkh|ryP NYKxO5BoW0GQR1XS
HCC1806 MmrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTVwN{WxO|Mh|ryP MVzTRW5ITVJ?
COLO-680 NHTxSoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LieWlEPTB;Nj6yNVQxPiEQvF2= Mm[5V2FPT0WU
HCC2218 NFHqW5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTMWVlKSzVyPUeuO|k4ODRizszN NWLPbVZDW0GQR1XS
SK-MEL-24 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nhc2lEPTB;Nz64NVkzPCEQvF2= M4W2cHNCVkeHUh?=
NCI-H720 NUnhd4RFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXwb45KSzVyPUiuOFM3ODNizszN MYTTRW5ITVJ?
KASUMI-1 NI\QUZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPXTWM2OD16Lki5NlY3KM7:TR?= M1X2cHNCVkeHUh?=
HAL-01 NX3Id2tOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\kTIZKSzVyPUmuPFg3OiEQvF2= NXXHcmZFW0GQR1XS
CAL-33 NXGxT29PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTFyLkSzOEDPxE1? M1m2NnNCVkeHUh?=
SK-MEL-1 NV7FUXdMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rNS2lEPTB;MUKuOFY3OyEQvF2= NED5UohUSU6JRWK=
Ramos-2G6-4C10 MnX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XIUWlEPTB;MUKuOFc2OiEQvF2= NIHQfoFUSU6JRWK=
KY821 NVHMT4ZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3ywWmlEPTB;MUKuOFg2KM7:TR?= M{XXWXNCVkeHUh?=
HEC-1 MmnKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnVWolKSzVyPUGyMlkyQTZizszN NXLTN5JzW0GQR1XS
SK-NEP-1 M4rkUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnI[oVoUUN3ME2xN{4yPjZizszN M3LQRnNCVkeHUh?=
MN-60 MmnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTaTWM2OD1zMz61N|g6KM7:TR?= NFXEdnhUSU6JRWK=
DU-145 NV\2PGROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTF|LkmwOVMh|ryP Ml;RV2FPT0WU
EW-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7UN5FJUUN3ME2xOE42PTZ3IN88US=> MmT0V2FPT0WU
OS-RC-2 NWOyW5FNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4H5TWlEPTB;MUWuPVU5QSEQvF2= NHPIdJdUSU6JRWK=
RPMI-8226 NHHEbVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7pNGpKSzVyPUG2MlIxPDJizszN MVvTRW5ITVJ?
ChaGo-K-1 M1TTRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVyyWJM4UUN3ME2xOk42OzJ3IN88US=> NWDZUXMxW0GQR1XS
DEL NXThco95T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnHTWM2OD1zNj62O|E4KM7:TR?= NFPaUHBUSU6JRWK=
GP5d MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjITWM2OD1zNz6wOVMh|ryP M1vnZXNCVkeHUh?=
COLO-668 NGPPdpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LDNWlEPTB;MUeuOlI6PCEQvF2= MkPnV2FPT0WU
H9 Mln5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjhe5RPUUN3ME2xPE4zQDN|IN88US=> M{ezVnNCVkeHUh?=
NKM-1 NVy5TlFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TiZ2lEPTB;MUiuOVEyQSEQvF2= NWPlUXV3W0GQR1XS
KYSE-150 MlT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrmRoFKSzVyPUG4Mlk6QDZizszN MYLTRW5ITVJ?
Daoy MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mke4TWM2OD1zOT61OlQ6KM7:TR?= MliyV2FPT0WU
ECC10 M3vwUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmj3TWM2OD1{MD63OFU2KM7:TR?= MXnTRW5ITVJ?
A388 NEm2SHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHqySGJKSzVyPUKxMlkxQTFizszN MWPTRW5ITVJ?
MHH-NB-11 NGnVUYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTKTWM2OD1{Mz6xN|Y{KM7:TR?= NF70V5lUSU6JRWK=
HCC1937 NFjNb29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7GTWM2OD1{ND63OFYh|ryP M1KwUHNCVkeHUh?=
TGBC11TKB MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDoc|dlUUN3ME2yOU43QDZ|IN88US=> M3LkUnNCVkeHUh?=
CTV-1 MnTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfMbY9pUUN3ME2yOU45QTZ7IN88US=> NH64SnVUSU6JRWK=
NCI-H2029 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PxTWlEPTB;Mk[uOFI{QCEQvF2= M33ycHNCVkeHUh?=
HLE Moj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF2wbWhKSzVyPUK3MlA2PCEQvF2= MoDYV2FPT0WU
NCI-H1693 NVvrUGFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDtbIhKSzVyPUK3MlI5QThizszN MV\TRW5ITVJ?
HCC70 M4nybGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXONJVKSzVyPUK3MlczPDZizszN MUTTRW5ITVJ?
BEN MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLQV5dUUUN3ME2yO{46PTZ4IN88US=> M3zBbnNCVkeHUh?=
LB771 M4rrVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3y0NGlEPTB;MkiuPFM4OyEQvF2= MmPYV2FPT0WU
697 MoLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHO1[nRKSzVyPUK5MlAzOzVizszN MmDUV2FPT0WU
LU-139 NVTwNlFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\0TGlKSzVyPUK5MlM4PDhizszN Mof5V2FPT0WU
EW-13 M4HZWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfae5A3UUN3ME2yPU4{QDF2IN88US=> MV\TRW5ITVJ?
MOLT-13 M4XH[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDaeGhOUUN3ME2yPU4{QDF2IN88US=> NVS2WnlGW0GQR1XS
L-363 NHjoZ|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEm2R5VKSzVyPUK5MlQ4QThizszN NILsRnNUSU6JRWK=
EM-2 NXXHVXNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\1b5RKSzVyPUK5MlQ6ODFizszN MUjTRW5ITVJ?
RS4-11 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3yxd2lEPTB;M{CuOFI1OSEQvF2= NFTmUGhUSU6JRWK=
A2780 NFTaVYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTNyLke0OVch|ryP NHL5T3dUSU6JRWK=
KU812 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrJN3lKUUN3ME2zNk4{PjR{IN88US=> Ml3WV2FPT0WU
COLO-684 NG\mbXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnFZoRKSzVyPUOzMlM2QTlizszN MWHTRW5ITVJ?
MFE-280 NIj4RWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHv0NWdKSzVyPUOzMlM5QDlizszN NF\qTnlUSU6JRWK=
KG-1 M2nzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXRPIVKSzVyPUOzMlYxODFizszN MXPTRW5ITVJ?
JVM-3 NH3LTXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrmeGVKSzVyPUO1MlU5PjhizszN MXHTRW5ITVJ?
MV-4-11 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjmTm5WUUN3ME2zOU45PDl7IN88US=> NUPON2xqW0GQR1XS
LAMA-84 NV3TUVQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vJemlEPTB;M{[uO|M1PSEQvF2= MVLTRW5ITVJ?
MOLT-16 MnnOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTN4Lkm1NkDPxE1? MlTiV2FPT0WU
H4 NXnROHZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTN5LkW2O{DPxE1? NGf0[2lUSU6JRWK=
T47D NHfZe4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjZUnZKSzVyPUO3MlcxOThizszN MoDOV2FPT0WU
CAL-54 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\vfWlEPTB;M{euPVY3KM7:TR?= M{HENHNCVkeHUh?=
SW982 M2TlVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTN6LkC5PVgh|ryP M1fDVnNCVkeHUh?=
IGROV-1 M1\SZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7DVWNKSzVyPUO5MlM{ODRizszN NH\VdZBUSU6JRWK=
NB14 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXVS|lKSzVyPUSwMlcxOzFizszN NXTLNmlmW0GQR1XS
HCC1187 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4mzcGlEPTB;NEGuNlc4OSEQvF2= M{DrbnNCVkeHUh?=
SBC-1 M4XBdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1q1bGlEPTB;NEGuN|A3OyEQvF2= NXztcZY4W0GQR1XS
KARPAS-45 NVLT[oZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTRzLkS4NVgh|ryP NIjRVGRUSU6JRWK=
MOLT-4 NWjLdIQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;VTWM2OD12Mj6yOVM5KM7:TR?= MUPTRW5ITVJ?
JVM-2 MlPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXO1cW9TUUN3ME20Nk46OjB5IN88US=> M3T3UHNCVkeHUh?=
A4-Fuk MkPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;RemRKSzVyPUSzMlU3QTFizszN NH;BUJhUSU6JRWK=
MDA-MB-361 NInlS|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTR|Lki0NVQh|ryP MmfNV2FPT0WU
BALL-1 M4nVSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXuTWM2OD12Mz65OVMzKM7:TR?= MX3TRW5ITVJ?
T98G M{f3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFWzfllKSzVyPUS0Mlg2OTdizszN NHm4R2JUSU6JRWK=
Mo-T NY[2OotzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHLU|BRUUN3ME20OU43Ozh7IN88US=> M2HxdHNCVkeHUh?=
MHH-PREB-1 MkPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljHTWM2OD12NT63OVg2KM7:TR?= MV\TRW5ITVJ?
ALL-PO MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV63dm4{UUN3ME20O{4{PzlzIN88US=> NXHQ[mtzW0GQR1XS
NCI-H510A NEHKVFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYC1dIc4UUN3ME20O{46ODN2IN88US=> MkXVV2FPT0WU
ML-2 MoPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\HTWM2OD12OT63PFU3KM7:TR?= NFPtUI9USU6JRWK=

... Click to View More Cell Line Experimental Data

In vivo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]
臨床試験 A Phase I study of evaluating the bioavailability and food effect of three formulations of ABT-888 on pharmacokinetics in subjects with solid tumors has been completed.
特集 Increases the efficacy of common cancer therapies such as radiation and alkylating agents.

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

In vitro PARP assays PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 μM [3H]NAD+ (1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Reactions are terminated with 1.5 mM benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter.

動物実験:

[1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Veliparib (ABT-888) SDF
分子量 244.29
化学式

C13H16N4O

CAS No. 912444-00-9
保管 3年-20℃
2年-80℃in solvent
別名 NSC 737664
溶解度 (25°C) * In vitro DMSO 17 mg/mL (69.58 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 0.5% methylcellulose+0.2% Tween 80 5 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 (R)-2-(2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-4-carboxamide

文献中の引用 (39)

技術サポート&よくある質問(FAQ)

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。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related PARP 阻害剤

  • G007-LK

    G007-LKは一種の有効的で、選択性タンキラーゼ(tankyrase)阻害剤で、TNKS1/2に作用する時のIC50値が46 nM と 25 nMに分かれます。

  • NU1025

    NU1025は一種の有効なPARP阻害剤で、このIC50値が 400 nMです。

  • SCR7

    SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ).

  • Blasticidin S HCl

    Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes, and acts as a DNA and protein synthesis inhibitor, used to select transfected cells carrying bsr or BSD resistance genes.

  • Olaparib (AZD2281, Ku-0059436)

    Olaparib (AZD2281, Ku-0059436)は一種の選択性PARP1/2阻害剤で、無細胞試験でIC50値が 5 nM/1 nMになって、PARP1/2に作用する効果は tankyrase-1に作用する効果が300倍が高くなります。臨床3期。

    Features:A potent PARP inhibitor (currently in late stage clinical trials).

  • Rucaparib (AG-014699,PF-01367338)

    Rucaparib (AG-014699, PF-01367338)は一種のPARP阻害剤で、無細胞試験でPARP1に作用する時のKi値が1.4 nMになって、残り8つPARPドメインにも結合親和力を表します。臨床3期。

    Features:The first PARP inhibitor used in clinical trials combined with temozolomide.

  • Talazoparib (BMN 673)

    Talazoparib (BMN 673)は一種の新たなPARP阻害剤で、無細胞試験でIC50値が0.58 nMになります。Talazoparib (BMN 673)も一種の有効なPARP-2阻害剤ですが、PARGを抑制しなくて、PTEN突然変異型に高度敏感をしています。臨床3期。

    Features:Most potent and selective PARPi reported thus far.

  • Iniparib (BSI-201)

    Iniparib (BSI-201)は一種のPARP1阻害剤で、三種陰性乳癌(TNBC)に作用効果を持っています。臨床3期。

  • PJ34 HCl

    PJ34 HClはPJ34の塩酸塩形式で、一種のPARP阻害剤です。PJ34 HClはEC50値が20 nMになって、 PARP1/2に同等有効に作用します。

    Features:Water-soluble PARP1/2 inhibitor with >10,000-fold potentcy vs. 3-aminobenzamide (prototypical PARP inhibitor). Potential uses in cardiovascular diseases (stroke, cerebral ischemia, & myocardial ischemia).

最近チェックしたアイテム

Tags: Veliparib (ABT-888)を買う | Veliparib (ABT-888)供給者 | Veliparib (ABT-888)を購入する | Veliparib (ABT-888)費用 | Veliparib (ABT-888)生産者 | オーダーVeliparib (ABT-888) | Veliparib (ABT-888)代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ