Veliparib (ABT-888) 化学構造
分子量: 244.29

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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 MWTLbY5ie2ViQYPzZZk> M2L6eFMxKG2rbh?= MU\Jcohq[mm2aX;uJI9nKFCDUmCxJJdqfGhiRVO1NEBw\iByLkCwNkDPxE1? M4roUFE6QDh6N{[w
Jurkat NF:2XWxMcW6jc3WgRZN{[Xl? NFuyOIk6PiCq NWTWeFJqTE2VTx?= MXTJcohq[mm2aX;uJI9nKFCDUmCxJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDj[YxtKH[rYXLpcIl1gSC5aYToJGVEPTBib3[gN{DPxE1? M2TTbVI{QDVyMUm5
Capan1 MlfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXW3NkBp M1HQOWROW09? NGDZN5FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGJTS0F{IHflcoUhdXW2YYTl[EBpfW2jbjDDZZBidjFiY3XscJMhf2m2aDDJR|UxKG:oIEO5Mlch|ryP NHvrRYEzPDN7OEO4Ny=>
DT40 MlLOR5l1d3SxeHnjJGF{e2G7 NGGyZYc4OiCq NEL3c4hFVVOR NH\yflhEgXSxdH;4bYNqfHliYXfhbY5{fCClaHnjb4VvKEKUQ1GyMYRm\mmlaXXueEBFXDRyIHPlcIx{ NUHlV3RyOjR7MkK1PFc>
ML-1 MlLjRZBweHSxdHnjJGF{e2G7 NWLmNVBDOi53IN88US=> MnXINlQhcA>? M4jBcWROW09? NIXiVIxUgW6ncnfpd5Rq[2GubImg[Y5p[W6lZYOgWHJCUUxvaX7keYNm\CCjcH;weI9{cXNiaX6gUWwuOSClZXzsdy=> NWnWOWZtOjR6OUWxN|U>
HCT-116 MVLLbY5ie2ViQYPzZZk> MYWwMlUh|ryP MlrPNlQhcA>? NYnDPHl4WEGUUDDhZ5Rqfmm2eTDk[YNz\WG|ZYO= MYOyN|A2PDJzMx?=
UM-SCC1 MoDDR5l1d3SxeHnjJGF{e2G7 NITPU4syOCEQvF2= Ml\0NlQhcA>? MY\S[YR2[2W|IITo[UBk\WyuII\pZYJqdGm2eR?= M3nCV|IyQTF{NkKw
FaDu M3XCO2N6fG:2b4jpZ{BCe3OjeR?= NXvzXG17OTBizszN MkGzNlQhcA>? NF3KVGZT\WS3Y3XzJJRp\SClZXzsJJZq[WKrbHn0fS=> NIfrZVczOTlzMk[yNC=>
PC-3 NGS0dHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUexNEDPxE1? MYDJcoR2[2W|IHGgd4lodmmoaXPhcpQhcW6qaXLpeIlwdiCrbjDjc4xwdnliZn;ycYF1cW:wwrC= NFn5dmszOTV5MUmxNi=>
EoL-1-cell NVfnW4JtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTFwMEe5PEDPxE1? MUXTRW5ITVJ?
NCI-SNU-5 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTNwMUK4OFEh|ryP M1yxdHNCVkeHUh?=
BV-173 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LZdGlEPTB;NT60OVQxQSEQvF2= Mn7KV2FPT0WU
HCC1806 M13rW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTVwN{WxO|Mh|ryP NGDNZnlUSU6JRWK=
COLO-680 MnPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jmUGlEPTB;Nj6yNVQxPiEQvF2= NYLJZ41XW0GQR1XS
HCC2218 NVXtXlVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[3TlR5UUN3ME23Mlc6PzB2IN88US=> NWnafY51W0GQR1XS
SK-MEL-24 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;BTJpSUUN3ME23MlgyQTJ2IN88US=> MUjTRW5ITVJ?
NCI-H720 M324Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3L4W2lEPTB;OD60N|YxOyEQvF2= MX3TRW5ITVJ?
KASUMI-1 NIf5NGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRThwOEmyOlYh|ryP M{DTVnNCVkeHUh?=
HAL-01 NX22RlhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrCVIdKSzVyPUmuPFg3OiEQvF2= M3zEenNCVkeHUh?=
CAL-33 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTFyLkSzOEDPxE1? M13pOXNCVkeHUh?=
SK-MEL-1 NULCfFZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrlSmRKSzVyPUGyMlQ3PjNizszN MkHrV2FPT0WU
Ramos-2G6-4C10 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVKwWI91UUN3ME2xNk41PzV{IN88US=> NYS4fnFIW0GQR1XS
KY821 M2SzdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4r4S2lEPTB;MUKuOFg2KM7:TR?= NWWzWJRnW0GQR1XS
HEC-1 Mni1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXRO5F{UUN3ME2xNk46OTl4IN88US=> M3zKSXNCVkeHUh?=
SK-NEP-1 MoXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTF|LkG2OkDPxE1? M2PnRnNCVkeHUh?=
MN-60 NIXnNHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\wTWM2OD1zMz61N|g6KM7:TR?= NHLXPGxUSU6JRWK=
DU-145 M{i5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVq2R5Z{UUN3ME2xN{46ODV|IN88US=> NUniNZNrW0GQR1XS
EW-3 NWLER5F1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTF2LkW1OlUh|ryP M3XjbnNCVkeHUh?=
OS-RC-2 NHzodWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTF3Lkm1PFkh|ryP NFSxPFhUSU6JRWK=
RPMI-8226 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETmNIxKSzVyPUG2MlIxPDJizszN MXXTRW5ITVJ?
ChaGo-K-1 MnHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrrS4ZKSzVyPUG2MlU{OjVizszN M3fCdnNCVkeHUh?=
DEL MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1mx[GlEPTB;MU[uOlcyPyEQvF2= NYHwfJNVW0GQR1XS
GP5d MmHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLaTWM2OD1zNz6wOVMh|ryP Mn23V2FPT0WU
COLO-668 NGDaS|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTzTWM2OD1zNz62Nlk1KM7:TR?= M{XuN3NCVkeHUh?=
H9 NXuxZpZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLqTWM2OD1zOD6yPFM{KM7:TR?= Mn\rV2FPT0WU
NKM-1 NFq3[4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTF6LkWxNVkh|ryP NI\MRotUSU6JRWK=
KYSE-150 Mn;MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrDTWM2OD1zOD65PVg3KM7:TR?= M1LOSnNCVkeHUh?=
Daoy MorOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PuNmlEPTB;MUmuOVY1QSEQvF2= MW\TRW5ITVJ?
ECC10 M1vCR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUK4TFZQUUN3ME2yNE44PDV3IN88US=> Mom1V2FPT0WU
A388 NHq3cJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{K1eGlEPTB;MkGuPVA6OSEQvF2= M37T[nNCVkeHUh?=
MHH-NB-11 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHEW5BKSzVyPUKzMlE{PjNizszN M1nHbHNCVkeHUh?=
HCC1937 NUnEOnQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zUXmlEPTB;MkSuO|Q3KM7:TR?= MXTTRW5ITVJ?
TGBC11TKB MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTJ3Lk[4OlMh|ryP NUi5UFZbW0GQR1XS
CTV-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfjZVRTUUN3ME2yOU45QTZ7IN88US=> NH7JVG1USU6JRWK=
NCI-H2029 M2HY[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTJ4LkSyN|gh|ryP M2D0WXNCVkeHUh?=
HLE M13TWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHLdHRKSzVyPUK3MlA2PCEQvF2= NYXISlZnW0GQR1XS
NCI-H1693 MnvBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fXPGlEPTB;MkeuNlg6QCEQvF2= MVfTRW5ITVJ?
HCC70 NXnrUW8{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DiTGlEPTB;MkeuO|I1PiEQvF2= NGD6[XJUSU6JRWK=
BEN MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTJ5Lkm1OlYh|ryP NVfWVJY3W0GQR1XS
LB771 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTJ6LkizO|Mh|ryP MW\TRW5ITVJ?
697 MnT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTJ7LkCyN|Uh|ryP NHz2SlhUSU6JRWK=
LU-139 M{\YVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTJ7LkO3OFgh|ryP NGXYS5ZUSU6JRWK=
EW-13 MmnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELW[3VKSzVyPUK5MlM5OTRizszN NV\yN|lHW0GQR1XS
MOLT-13 Mm\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfzZ41SUUN3ME2yPU4{QDF2IN88US=> NUPv[3BSW0GQR1XS
L-363 NHjMXldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH31dlFKSzVyPUK5MlQ4QThizszN MXzTRW5ITVJ?
EM-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorDTWM2OD1{OT60PVAyKM7:TR?= MUDTRW5ITVJ?
RS4-11 NGPSXnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXMTWM2OD1|MD60NlQyKM7:TR?= NV7DcoxrW0GQR1XS
A2780 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PzfWlEPTB;M{CuO|Q2PyEQvF2= NX7udo5MW0GQR1XS
KU812 MlvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnZO4JTUUN3ME2zNk4{PjR{IN88US=> MUHTRW5ITVJ?
COLO-684 NYLrWphJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XWTmlEPTB;M{OuN|U6QSEQvF2= MUfTRW5ITVJ?
MFE-280 M2W3OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzQVmJnUUN3ME2zN{4{QDh7IN88US=> NVPPfo02W0GQR1XS
KG-1 M3fQUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDl[YxKSzVyPUOzMlYxODFizszN NYjRPI9jW0GQR1XS
JVM-3 MmC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHMOW1KSzVyPUO1MlU5PjhizszN MVfTRW5ITVJ?
MV-4-11 NGHZdWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTN3Lki0PVkh|ryP M1q3UnNCVkeHUh?=
LAMA-84 NGDBNJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLUe4dyUUN3ME2zOk44OzR3IN88US=> M1TDNnNCVkeHUh?=
MOLT-16 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHK4fJVKSzVyPUO2Mlk2OiEQvF2= M37NRnNCVkeHUh?=
H4 NF7BRmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7QO4N{UUN3ME2zO{42PjdizszN MmTHV2FPT0WU
T47D NFTl[2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEK4WXBKSzVyPUO3MlcxOThizszN MnjnV2FPT0WU
CAL-54 MlW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnPRolKSzVyPUO3Mlk3PiEQvF2= NUO5cGhTW0GQR1XS
SW982 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTN6LkC5PVgh|ryP MkWyV2FPT0WU
IGROV-1 M1PCdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfxellKSzVyPUO5MlM{ODRizszN Ml7YV2FPT0WU
NB14 M4\zTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4roSWlEPTB;NECuO|A{OSEQvF2= M2LLTnNCVkeHUh?=
HCC1187 MnPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTRzLkK3O|Eh|ryP NHrtWG5USU6JRWK=
SBC-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfUNZRKSzVyPUSxMlMxPjNizszN NVnPNHpNW0GQR1XS
KARPAS-45 NWDmWmVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmryTWM2OD12MT60PFE5KM7:TR?= NYTTUGlrW0GQR1XS
MOLT-4 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEj6ZpNKSzVyPUSyMlI2OzhizszN NWHHfo9JW0GQR1XS
JVM-2 NUHIPYk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1y1fmlEPTB;NEKuPVIxPyEQvF2= M37HbnNCVkeHUh?=
A4-Fuk M4Lw[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYC4OJNWUUN3ME20N{42PjlzIN88US=> M2X6T3NCVkeHUh?=
MDA-MB-361 NYHGeWFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTR|Lki0NVQh|ryP NHzZRXFUSU6JRWK=
BALL-1 NFzob4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XHeGlEPTB;NEOuPVU{OiEQvF2= NGLPSIpUSU6JRWK=
T98G M33qW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLjO2RKSzVyPUS0Mlg2OTdizszN Ml;3V2FPT0WU
Mo-T MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\KTWM2OD12NT62N|g6KM7:TR?= MU\TRW5ITVJ?
MHH-PREB-1 NF22d5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj2XJlrUUN3ME20OU44PTh3IN88US=> MUfTRW5ITVJ?
ALL-PO NEXNcnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTR5LkO3PVEh|ryP NFSzPJVUSU6JRWK=
NCI-H510A MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUP4PIpYUUN3ME20O{46ODN2IN88US=> NETWb2lUSU6JRWK=
ML-2 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfXTWM2OD12OT63PFU3KM7:TR?= NFHRWZNUSU6JRWK=

... 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 (40)

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    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).

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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