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 NX;Qfo1iU2mwYYPlJGF{e2G7 NFfUeJU{OCCvaX6= MYPJcohq[mm2aX;uJI9nKFCDUmCxJJdqfGhiRVO1NEBw\iByLkCwNkDPxE1? MmPVNVk5QDh5NkC=
Jurkat NX;6ZpBrU2mwYYPlJGF{e2G7 M3n4NVk3KGh? M4fjdmROW09? NEXXdY9KdmirYnn0bY9vKG:oIGDBVnAyKGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBk\WyuII\pZYJqdGm2eTD3bZRpKEWFNUCgc4YhOyEQvF2= NVnqcWpbOjN6NUCxPVk>
Capan1 NX\NZXcxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmn6O|IhcA>? M3TUSWROW09? NF\IdZFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGJTS0F{IHflcoUhdXW2YYTl[EBpfW2jbjDDZZBidjFiY3XscJMhf2m2aDDJR|UxKG:oIEO5Mlch|ryP M174W|I1Ozl6M{iz
DT40 MYjDfZRwfG:6aXOgRZN{[Xl? NH3K[oU4OiCq NUfDdoRwTE2VTx?= MlWxR5l1d3SxeHnjbZR6KGGpYXnud5Qh[2irY3vlckBDWkODMj3k[YZq[2mnboSgSHQ1OCClZXzsdy=> M4Dqe|I1QTJ{NUi3
ML-1 M175N2Fxd3C2b4TpZ{BCe3OjeR?= MkPmNk42KM7:TR?= MoXqNlQhcA>? MX\EUXNQ MnnWV5lv\XKpaYP0bYNidGy7IHXubIFv[2W|IGTSRWlNNWmwZIXj[YQh[XCxcITvd4l{KGmwIF3MMVEh[2WubIO= NWjZSW5nOjR6OUWxN|U>
HCT-116 M4[yZ2tqdmG|ZTDBd5NigQ>? M{PwN|AvPSEQvF2= M{G3cFI1KGh? NW\mbnY{WEGUUDDhZ5Rqfmm2eTDk[YNz\WG|ZYO= NIfWZZczOzB3NEKxNy=>
UM-SCC1 M2qzSWN6fG:2b4jpZ{BCe3OjeR?= NWj3dFIyOTBizszN MYWyOEBp NXLEWZkxWmWmdXPld{B1cGViY3XscEB3cWGkaXzpeJk> MnHENlE6OTJ4MkC=
FaDu NF3FeJpEgXSxdH;4bYMhSXO|YYm= NFSz[WQyOCEQvF2= MoL4NlQhcA>? NEPPNm5T\WS3Y3XzJJRp\SClZXzsJJZq[WKrbHn0fS=> NUfl[49IOjF7MUK2NlA>
PC-3 NVjjWJRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIryWHAyOCEQvF2= M1HMdmlv\HWlZYOgZUB{cWewaX\pZ4FvfCCrbnjpZol1cW:wIHnuJINwdG:weTDmc5Ju[XSrb39CpC=> NIXoVJczOTV5MUmxNi=>
EoL-1-cell M2j2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHGTWM2OD1zLkC3PVgh|ryP M1foOHNCVkeHUh?=
NCI-SNU-5 NWP3PW1mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTNwMUK4OFEh|ryP MorCV2FPT0WU
BV-173 NFLEPZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXruT|Y{UUN3ME21MlQ2PDB7IN88US=> MVzTRW5ITVJ?
HCC1806 M4rU[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\6SFR1UUN3ME21Mlc2OTd|IN88US=> NX30NmN1W0GQR1XS
COLO-680 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTZwMkG0NFYh|ryP MnzqV2FPT0WU
HCC2218 M{LHUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XFS2lEPTB;Nz63PVcxPCEQvF2= NHP1RpBUSU6JRWK=
SK-MEL-24 Mkf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTdwOEG5NlQh|ryP NF7zOo9USU6JRWK=
NCI-H720 NYHB[|J3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTGe5lKSzVyPUiuOFM3ODNizszN NFrYdFVUSU6JRWK=
KASUMI-1 NFGyW2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7jSIxVUUN3ME24Mlg6OjZ4IN88US=> NU\lVFlHW0GQR1XS
HAL-01 MmXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HNemlEPTB;OT64PFYzKM7:TR?= NX7pPHUzW0GQR1XS
CAL-33 NVXYeHd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\afGlEPTB;MUCuOFM1KM7:TR?= NW\FSpV5W0GQR1XS
SK-MEL-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLUdJNKSzVyPUGyMlQ3PjNizszN NYfhTHdpW0GQR1XS
Ramos-2G6-4C10 M2\YW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkO3TWM2OD1zMj60O|UzKM7:TR?= NYO3NY1VW0GQR1XS
KY821 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3xTWM2OD1zMj60PFUh|ryP MX3TRW5ITVJ?
HEC-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HGUWlEPTB;MUKuPVE6PiEQvF2= NHLjN|JUSU6JRWK=
SK-NEP-1 MoThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTF|LkG2OkDPxE1? MkjVV2FPT0WU
MN-60 M2rGWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrtSWxKSzVyPUGzMlU{QDlizszN NVLFVYpWW0GQR1XS
DU-145 M2rNTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEKz[o9KSzVyPUGzMlkxPTNizszN NGjCOIFUSU6JRWK=
EW-3 NWm1RldJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXsVG1KSzVyPUG0MlU2PjVizszN MYnTRW5ITVJ?
OS-RC-2 MkHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Xk[mlEPTB;MUWuPVU5QSEQvF2= NIDKPW1USU6JRWK=
RPMI-8226 NHG1fnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTpVY1KSzVyPUG2MlIxPDJizszN M2HteXNCVkeHUh?=
ChaGo-K-1 M1HUbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2DHOmlEPTB;MU[uOVMzPSEQvF2= MknuV2FPT0WU
DEL MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTF4Lk[3NVch|ryP NHXsUXdUSU6JRWK=
GP5d MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PmSWlEPTB;MUeuNFU{KM7:TR?= NUn1TZVnW0GQR1XS
COLO-668 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTVVYlKSzVyPUG3MlYzQTRizszN MX7TRW5ITVJ?
H9 MlfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3ESFNKSzVyPUG4MlI5OzNizszN NGjDN4VUSU6JRWK=
NKM-1 M1nKfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTF6LkWxNVkh|ryP Mm\yV2FPT0WU
KYSE-150 M2Gw[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrmTWM2OD1zOD65PVg3KM7:TR?= MlLJV2FPT0WU
Daoy MlTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTF7LkW2OFkh|ryP NE\QUmRUSU6JRWK=
ECC10 NImzZ4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLKTWM2OD1{MD63OFU2KM7:TR?= NIH0PZpUSU6JRWK=
A388 NWLiboFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfGXHJKSzVyPUKxMlkxQTFizszN M4LCdXNCVkeHUh?=
MHH-NB-11 NH\sVYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH33NVlKSzVyPUKzMlE{PjNizszN M4jSenNCVkeHUh?=
HCC1937 NUPWPZM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\JTWM2OD1{ND63OFYh|ryP NU[xWlVRW0GQR1XS
TGBC11TKB MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTJ3Lk[4OlMh|ryP NWXBN281W0GQR1XS
CTV-1 MoWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTJ3Lki5Olkh|ryP NHnlfIFUSU6JRWK=
NCI-H2029 NWX4[JV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnONJQ3UUN3ME2yOk41OjN6IN88US=> NFP4RZZUSU6JRWK=
HLE MorsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVf1W|ROUUN3ME2yO{4xPTRizszN MUfTRW5ITVJ?
NCI-H1693 MlTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfiboxVUUN3ME2yO{4zQDl6IN88US=> NHnzSHdUSU6JRWK=
HCC70 NYjZ[WdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fzeWlEPTB;MkeuO|I1PiEQvF2= MXTTRW5ITVJ?
BEN MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4T2TWlEPTB;MkeuPVU3PiEQvF2= M1\pfHNCVkeHUh?=
LB771 MnjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXmxPGZOUUN3ME2yPE45Ozd|IN88US=> M{[zXXNCVkeHUh?=
697 MmnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\VTWM2OD1{OT6wNlM2KM7:TR?= NH:5e|dUSU6JRWK=
LU-139 MmW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPL[VFKSzVyPUK5MlM4PDhizszN NFXHSVNUSU6JRWK=
EW-13 NHvW[YtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjFTWM2OD1{OT6zPFE1KM7:TR?= MoXlV2FPT0WU
MOLT-13 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTpTWM2OD1{OT6zPFE1KM7:TR?= M2HHbXNCVkeHUh?=
L-363 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1THVGlEPTB;MkmuOFc6QCEQvF2= MVjTRW5ITVJ?
EM-2 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXiOFlIUUN3ME2yPU41QTBzIN88US=> MYPTRW5ITVJ?
RS4-11 MnnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HkO2lEPTB;M{CuOFI1OSEQvF2= M3fpS3NCVkeHUh?=
A2780 NXKyUoFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDSVYZKSzVyPUOwMlc1PTdizszN MofsV2FPT0WU
KU812 M17pVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPBTWM2OD1|Mj6zOlQzKM7:TR?= NXTpO4diW0GQR1XS
COLO-684 M4THfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVS5SXVkUUN3ME2zN{4{PTl7IN88US=> MYHTRW5ITVJ?
MFE-280 M13lN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3X4PWlEPTB;M{OuN|g5QSEQvF2= NHXFR5ZUSU6JRWK=
KG-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrUe3RKSzVyPUOzMlYxODFizszN NFHkPXhUSU6JRWK=
JVM-3 Ml\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LjOmlEPTB;M{WuOVg3QCEQvF2= M33N[XNCVkeHUh?=
MV-4-11 MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDNbXRJUUN3ME2zOU45PDl7IN88US=> M1PyfXNCVkeHUh?=
LAMA-84 NXXFVI52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTN4LkezOFUh|ryP M4W2dHNCVkeHUh?=
MOLT-16 NETFe4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjVSHlHUUN3ME2zOk46PTJizszN M{TEXXNCVkeHUh?=
H4 NGLDb|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\H[WlEPTB;M{euOVY4KM7:TR?= M176XXNCVkeHUh?=
T47D Mmj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjQTWM2OD1|Nz63NFE5KM7:TR?= MlqwV2FPT0WU
CAL-54 M2SwSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLudm9uUUN3ME2zO{46PjZizszN M{nodnNCVkeHUh?=
SW982 M3\IcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4juNmlEPTB;M{iuNFk6QCEQvF2= MYLTRW5ITVJ?
IGROV-1 NFLINmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTN7LkOzNFQh|ryP NF7MSZJUSU6JRWK=
NB14 NGK4eIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTRyLkewN|Eh|ryP NEfXVYFUSU6JRWK=
HCC1187 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3m3S2lEPTB;NEGuNlc4OSEQvF2= NIPi[WRUSU6JRWK=
SBC-1 NYTCVpV6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHxTWM2OD12MT6zNFY{KM7:TR?= M3TwcnNCVkeHUh?=
KARPAS-45 NWHtSHRbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjDR5dKSzVyPUSxMlQ5OThizszN M{DLU3NCVkeHUh?=
MOLT-4 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTR{LkK1N|gh|ryP M3LrO3NCVkeHUh?=
JVM-2 NUXySYYyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\GXGlEPTB;NEKuPVIxPyEQvF2= MlryV2FPT0WU
A4-Fuk M2HaZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTR|LkW2PVEh|ryP NWrBU3lZW0GQR1XS
MDA-MB-361 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\iSFI6UUN3ME20N{45PDF2IN88US=> NH31e5dUSU6JRWK=
BALL-1 MnXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfyd2g2UUN3ME20N{46PTN{IN88US=> MlzyV2FPT0WU
T98G NV6zZ|hQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnWOJBKSzVyPUS0Mlg2OTdizszN MmfJV2FPT0WU
Mo-T M3vuXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fvZWlEPTB;NEWuOlM5QSEQvF2= M{mwU3NCVkeHUh?=
MHH-PREB-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlWwTWM2OD12NT63OVg2KM7:TR?= MWjTRW5ITVJ?
ALL-PO NVTJNWR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XSO2lEPTB;NEeuN|c6OSEQvF2= NFjzW2NUSU6JRWK=
NCI-H510A MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTR5LkmwN|Qh|ryP M3yyUXNCVkeHUh?=
ML-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnKN2N5UUN3ME20PU44QDV4IN88US=> MojSV2FPT0WU

... 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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