Niraparib (MK-4827)
中文名称：尼拉帕尼
Niraparib (MK4827)是一种口服有效的选择性PARP-1和PARP-2抑制剂，可在有BRCA和PTEN功能缺陷的临床肿瘤模型中引起合成致死性。Niraparib 可形成PARP–DNA复合物并导致DNA损伤、凋亡和细胞死亡。Phase 3。
Niraparib (MK-4827) Chemical Structure
CAS: 1038915-60-4
相关PARP产品
客户使用Selleck的Niraparib (MK-4827)发表文献70篇：
产品质控
批次：
纯度：
99.97%
99.97
PARP抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HeLa cells | MmT4SpVv[3Srb36gZZN{[Xl? | NIrzOG5KdmirYnn0bY9vKG:oIGDBVnAhcW5iaInkdo9o\W5icHXyc5hq\GVvaX7keYNm\CCqdX3hckBJ\UyjIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gSG5CNWSjbXHn[U1qdmS3Y3XkJHBCWnmuYYTpc44tKEWFNUC9NE4xODRizszN | MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh5M{m4NUc,OTl6N{O5PFE9N2F- | ||
| A549 cells | NIW2cYJEgXSxdH;4bYNqfHliYYPzZZk> | NUnIbG53PS15IHThfZM> | NHGzdIlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSlKFQUKgd4hTVkFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPSC2bzC3JIRigXNiYomgR4VtdFSrdHXyMWJtfWViYYPzZZktKEOFNUC9NE4xOTFizszN | M{LmVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6= | |
| MDA-MB-436 cells | NEfTOYhRem:uaX\ldoF1cW:wIHHzd4F6 | MlzBOkBl[Xm| | MlnLRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN4IHPlcIx{KGW6cILld5NqdmdiQmLDRVEhPTN7NjCrJFFIRkFibYX0ZY51KGGodHXyJFYh\GG7czDifUBk\WyuIITpeIVzNWKudXWgZZN{[XluIFPDOVA:OThibl2= | NHH4VJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi3N|k5OSd-MUm4O|M6QDF:L3G+ | |
| SUM1315MO2 cells | NXTVcpNtS3m2b4TvfIlkcXS7IHHzd4F6 | MnTmNVIh\GG7cx?= | M2jUO2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNWVTF|MUXNU|Ih[2WubIOgZ4FzenmrbnegRnJESTFibYX0ZY51KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFEzKGSjeYOgZpkhS2WubGTpeIVzNUKudXWgZZN{[XluIFPDOVA:OC5yMjFOwG0> | Mn\ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?= | |
| DoTc2-4510 cells | NFXsV5pEgXSxdH;4bYNqfHliYYPzZZk> | NYizTHI4PS15IHThfZM> | NG\JT3NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFd1SlMj20OVExKGOnbHzzJINienK7aX7nJGJTS0F{IH31eIFvfCCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA2KHSxIEeg[IF6eyCkeTDD[YxtXGm2ZYKtRox2\SCjc4PhfUwhS0N3ME2wMlAzOyEQvF2= | M{\2bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6= | |
| SUM149PT cells | NUTQ[3N7S3m2b4TvfIlkcXS7IHHzd4F6 | Mn;aOU04KGSjeYO= | MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTWW0yPDmSVDDj[YxteyClYYLyfYlv\yCEUlPBNUBufXSjboSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiNTD0c{A4KGSjeYOgZpkhS2WubGTpeIVzNUKudXWgZZN{[XluIFPDOVA:OC5yMkSg{txO | MmnRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?= | |
| UWB1.289 cells | NUO5dFBDS3m2b4TvfIlkcXS7IHHzd4F6 | MWG1MVch\GG7cx?= | MljYR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWXdDOS5{OEmgZ4VtdHNiY3HydplqdmdiQmLDRVEhdXW2YX70JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEWgeI8hPyCmYYnzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDDR|UxRTBwMEW2JO69VQ>? | NG\QTWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+ | |
| Capan1 cells | NGPDfWVEgXSxdH;4bYNqfHliYYPzZZk> | MXPDfZRwfG:6aXPpeJkh[WejaX7zeEBDWkODMj3k[YZq[2mnboSgbJVu[W5iQ3HwZY4yKGOnbHzzMEBESzVyPUCuNFkh|ryP | MoDUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?= | ||
| Jurkat cells | MofUSpVv[3Srb36gZZN{[Xl? | M{\n[WlvcGmkaYTpc44hd2ZiUFHSVFEhcW5iaIXtZY4hUnW{a3H0JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iClZXzsJJZq[WKrbHn0fUBi\nSncjC5OkBpenNiYomgUXRUKGG|c3H5JIlvKHC{ZYPlcoNmKG:oIEGwNEB2VSCxZjD0[Y1wgm:ub33p[IUtKEWFNUC9NE4zKM7:TR?= | Mn6zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NUCxPVkoRjJ|OEWwNVk6RC:jPh?= | ||
| BT20 cells | MW\DfZRwfG:6aXPpeJkh[XO|YYm= | NIXFd|Y2NTdiZHH5dy=> | NIX4cVVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDXDJyIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFUhfG9iNzDkZZl{KGK7IFPlcIxVcXSncj3CcJVmKGG|c3H5MEBESzVyPUKuNkDPxE1? | MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F- | |
| Antiproliferative assay | Mlm4TIVN[Q>? | MVy3JIRigXN? | M13WRWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRnJESTFiZHXmbYNq\W62IHj1cYFvKEinTHGgZ4VtdHNiYX\0[ZIhPyCmYYnzJIJ6KGOnbHygeIl1\XJvYnz1[UBie3OjeTygR2M2OCB;IECuNFM{KM7:TT6= | NEPRRY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi3N|k5OSd-MUm4O|M6QDF:L3G+ | |
| Function assay | MlL5TIVN[Q>? | NX7nfnZSUW6qaXLpeIlwdiCxZjDQRXJRKGmwIHj5[JJw\2WwIIDldo95cWSnLXnu[JVk\WRiaIXtZY4hUGWOYTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJGRPSS2mYX3h[4UucW6mdXPl[EBRSVK7bHH0bY9vNCCHQ{mwJF0hOC5yNEWg{txONg>? | MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh5M{m4NUc,OTl6N{O5PFE9N2F- | ||
| Antiproliferative assay | MVjDZZBidjF? | MoPHNVMh\GG7cx?= | MnK3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFYYDhclEh[2WubIOg[ZhxemW|c3nu[{BDWkODMjC2NVc1\GWuVDDteZRifGmxbjDhcoQhdG:|czDv[kB4cWymLYT5dIUh[WyuZXzlJIFnfGW{IEGzJIRigXNiYomgZ4VtdCC2aYTldk1jdHWnIHHzd4F6NCCFQ{WwJF0hOC5yOTFOwG0v | MkGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6N{O5PFEoRjF7OEezPVgyRC:jPh?= | |
| Antiproliferative assay | Mle4TIVN[Q>? | NF7uOlc4KGSjeYO= | MljiRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZVzhJINmdGy|IHX4dJJme3Orbnege4lt\CC2eYDlJGJTS0FzIHHmeIVzKDdiZHH5d{BjgSClZXzsJJRqfGW{LXLseYUh[XO|YYmsJGNEPTBiPTCwMlg3KM7:TT6= | M{LZOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEezPVgyLz5zOUi3N|k5OTxxYU6= | |
| Function assay | M2\LZ2p2emujdB?= | NInMV2Y6PiCqcoO= | M1LBTGlvcGmkaYTpc44hd2ZiUFHSVFEhcW5iaIXtZY4hUnW{a3H0JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iClZXzsJJZq[WKrbHn0fUBi\nSncjC5OkBpenNiYomgUXRUKGG|c3H5MEBGSzVyIE2gN|Eh|ryPLh?= | MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3MEG5PUc,OjN6NUCxPVk9N2F- | |
| Function assay | M4GxOmNCWEGQLUG= | MWrJcohq[mm2aX;uJI9nKFCDUmCgbY4hSlKFQUKt[IVncWOrZX70JIh2dWGwIFPBVGFPNTFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgWS{b3flckBx\XKxeHnk[U1qdmS3Y3XkJHBCWnmuYYTpc44h[nliY3XscE1j[XOnZDDhd5NigSxiSVO1NEA:KDBwMECzOUDPxE1w | MnvIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?= | ||
| Function assay | MoPqTIVN[Q>? | MV\Jcohq[mm2aX;uJI9nKFCDUmCgbY4hcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIh6\HKxZ3XuJJBmem:6aXTlMYlv\HWlZXSgVGFTgWyjdHnvckBjgSClZXzsMYJie2WmIHHzd4F6NCCHQ{WwJF0hOC5yMESg{txONg>? | NH;scWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+ | ||
| Function assay | NWKxRVM1STJ5OEC= | MlvNTY5pcWKrdHnvckBw\iCSQWLQJIlvKGi3bXHuJGEzPzhyIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhcHmmcn;n[Y4heGW{b4jp[IUucW6mdXPl[EBRSVK7bHH0bY9vKGK7IHPlcIwu[mG|ZXSgZZN{[XluIFnDOVAhRSByLkCwOEDPxE1w | MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F- | ||
| Cytotoxicity assay | M4G1eG1FSS2PQj20N|Y> | MkLuR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDjZZJzgWmwZzDCVmNCOSCvdYThcpQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44tKEOFNUCgQUAxNjBzODFOwG0v | MofPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?= | ||
| Cytotoxicity assay | MlzmTIVN[Q>? | MmHZOUB1dyB5IHThfZM> | M3;IdmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmVGFiY3XscJMhfHKjboPm[YN1\WRid3n0bEBDWkODMTDzbHJPSSCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4Yh[2WubDD2bYFjcWyrdImgZYZ1\XJiNTD0c{A4KGSjeYOgZpkhS2WubGTpeIVzNUKudXWgZZN{[XluIFPDOVAhRSByLkCzOEDPxE1w | MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F- | |
| Function assay | NHH4dJFJ\Uyj | MVzJcohq[mm2aX;uJI9nKFCDUmCgbY4hcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIh6\HKxZ3XuJJBmem:6aXTlMYlv\HWlZXSgVGFTgWyjdHnvckBjgSClZXzsMYJie2WmIHHzd4F6NCCLQ{mwJF0hOC5yNE[g{txONg>? | M1;telxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6= | ||
| Function assay | MWLDRXBCVi1z | NUnj[GM2UW6qaXLpeIlwdiCxZjDQRXJRKGmwIFLSR2EzNWSnZnnjbYVvfCCqdX3hckBESVCDTj2xJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiaInkdo9o\W5icHXyc5hq\GVvaX7keYNm\CCSQWL5cIF1cW:wIHL5JINmdGxvYnHz[YQh[XO|YYmsJGlEQTBiPTCwMlA2KM7:TT6= | NXuwOI0{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=> | ||
| Function assay | M2n0UGEzPzhy | Mme5TY5pcWKrdHnvckBw\iCSQWLQJIlvKGi3bXHuJGEzPzhyIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhcHmmcn;n[Y4heGW{b4jp[IUucW6mdXPl[EBRSVK7bHH0bY9vKGK7IHPlcIwu[mG|ZXSgZZN{[XluIFnDPVAhRSByLkC1NkDPxE1w | NFL1VoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+ | ||
| Cytotoxicity assay | MVTI[Wxi | NUPnWpZwPSC2bzC3JIRigXN? | MW\DfZRwfG:6aXPpeJkh[WejaX7zeEB4cWymIIT5dIUhcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC1JJRwKDdiZHH5d{BjgSCFZXzsWIl1\XJvQnz1[UBie3OjeTygR2M2OCB;IECuPFUzKM7:TT6= | NYHKdWtpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=> | |
| Cytotoxicity assay | MoXzWXdDOS5{OEm= | NVvwTXhpPSC2bzC3JIRigXN? | NXezfZRXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXVeEMT6yPFkh[2WubIOg[ZhxemW|c3nu[{BDWkODMTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB3IITvJFch\GG7czDifUBE\WyuVHn0[ZIuSmy3ZTDhd5NigSxiQ1O1NEA:KDBwOUe1JO69VS5? | NIK2S|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+ | |
| Cytotoxicity assay | M2C5WWE2PDl? | MXS1JJRwKDdiZHH5dy=> | MknLR5l1d3SxeHnjbZR6KGGpYXnud5Qhf2muZDD0fZBmKGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgOUB1dyB5IHThfZMh[nliQ3XscHRqfGW{LVLseYUh[XO|YYmsJGNEPTBiPTCxMlc3KM7:TT6= | NHr6V5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+ | |
| Cytotoxicity assay | Mn3rR4Fx[W5z | NF3s[mREgXSxdH;4bYNqfHliYXfhbY5{fCCEUlPBNk1l\W[rY3nlcpQhcHWvYX6gR4Fx[W5zIHPlcIx{NCCHQ{WwJF0hOC54NTFOwG0v | Mo\kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK3NVcoRjJ4NkWyO|E4RC:jPh?= | ||
| Antitumor assay | NUPNU|ZVVUSDLV3CMVQ{Pg>? | NWT6VohyPTBibXevb4c> | MXWzN{Bl[Xm| | NYi0R3VoSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDlfJBz\XO|aX7nJGJTS0FzIEWzPVYhMyBzR{7BJI12fGGwdDD4[Y5w\3KjZoTl[EBqdiCFREGgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JicnXndoV{e2mxbjDheEA2OCCvZz;r[{wheG9iYnnkJIZweiB|MzDkZZl{ | M1HPNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEezPVgyLz5zOUi3N|k5OTxxYU6= |
| Antitumor assay | NF;CVZdOTEFvTVKtOFM3 | NFHpTW0yODBibXevb4c> | M2fpdlM{KGSjeYO= | M3TQPGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{[gZ4VtdHNiZYjwdoV{e2mwZzDCVmNCOSB3M{m2JEshOUd-QTDteZRidnRieHXuc4dz[W[2ZXSgbY4hS0RzIH3veZNmKGG|c3Xzd4VlKGG|IIT1cY9zKHKnZ4Lld5Nqd25iYYSgNVAxKG2pL3vnMEBxdyCzZDDmc5IhOzNiZHH5dy=> | MmPkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6N{O5PFEoRjF7OEezPVgyRC:jPh?= |
| Antitumor assay | M1npNm1FSS2PQj20N|Y> | Mn:xPFAhdWdxa3e= | NGTUcYIyKHSxIEKge4Vmc3N? | NIH3cW9CdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO2JINmdGy|IHjhdoJwemmwZzDCVmNCOSCvdYThcpQhgGWwb3fyZYZ1\WRiaX6gbY1ufW6xY3;tdJJwdWm|ZXSgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JiZ4Lve5RpKGmwaHnibZRqd25iYYSgPFAhdWdxa3esJJBwKHGmIH\vdkAyKHSxIEKge4Vmc3N? | NGK0e5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+ |
| Antitumor assay | MXPNSGEuVUJvNEO2 | NVXJV|JYQDBibXevb4c> | MXy0JJdm\Wu| | NXnwfFZ2SW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDoZZJjd3KrbnegRnJESTFibYX0ZY51KHinbn;ndoFnfGWmIHnuJIludXWwb3PvcZBzd22rc3XkJI1wfXOnIHHzd4V{e2WmIHHzJINwdXCuZYTlJIFv\CC|dYP0ZYlv\WRidIXtc5IhemWpcnXzd4lwdiCjdDC4NEBu\y:tZzygdI8heWRiZn;yJFQhf2Wna4O= | NXyxTJlsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=> |
| Antitumor assay | MnXHUWRCNU2ELUSzOi=> | MlfzOVAhdWdxa3e= | MWXBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN4IHPlcIx{KGijcnLvdolv\yCEUlPBNUBufXSjboSgfIVvd2e{YX\0[YQhcW5iaX3teY5w[2:vcILvcYl{\WRibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[XRiNUCgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCmYXnsfS=> | M2[4bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6= | |
| Antitumor assay | MX\NSGEuVUJvNEO2 | NWLZXW9nQDBibXevb4c> | MYezJJdm\Wu| | M{H4c2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{[gZ4VtdHNiaHHyZo9zcW6pIFLSR2EyKG23dHHueEB5\W6xZ4Lh[pRm\CCrbjDpcY12dm:lb33wdo9ucXOnZDDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiC|aILpcoti\2ViYYSgPFAhdWdxa3esJJBwKHGmIH\vdkA{KHenZXvz | M4C0TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6= |
| qHTS assay | M1LuU3REOzJ? | MlfjdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFSFM{KgZ4VtdHN? | M3T4[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6= | ||
| qHTS assay | MYfBOlc{ | M{HlZZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| | MkHhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?= | ||
| qHTS assay | M3vvSG5DOTZ2Mx?= | NV7XcpY4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> | MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F- | ||
| qHTS assay | MUHBOlc{ | M3fze5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGE3PzNiY3XscJMq | MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F- | ||
| qHTS assay | MUPCWE0{Pw>? | NXrj[oNneUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? | NEW1ZYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+ | ||
| qHTS assay | NXXUXFFNW0tvTj3NRy=> | NXrTbmJKeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> | Ml;XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?= | ||
| qHTS assay | NXPvRZVyVkJvRVLjNS=> | MYXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= | M2D2WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6= | ||
| qHTS assay | MnjlUGFPNTV? | NGDM[5RyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO= | MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F- | ||
| qHTS assay | MnzKV2suVi2PQx?= | MV7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNU2FIHPlcIx{ | MoLvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?= | ||
| qHTS assay | MXLUR|Mz | NIHOXFFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBVSzN{IHPlcIx{ | Mm\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?= | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Niraparib (MK4827)是一种口服有效的选择性PARP-1和PARP-2抑制剂，可在有BRCA和PTEN功能缺陷的临床肿瘤模型中引起合成致死性。Niraparib 可形成PARP–DNA复合物并导致DNA损伤、凋亡和细胞死亡。Phase 3。 | ||||
|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在完整细胞试验中，MK-4827抑制PARP的活性，EC50为4 nM，并抑制携带BRCA-1和BRCA-2突变的癌细胞的增殖，IC50为10-100 nM。它能有效地抑制PARP-1和PARP-2，IC分别为3.8 nM和2.1 nM。它对PARP-3, V-PARP和tankyrase-1的选择性低100倍以上，IC50分别为1300、330、570 nM。MK-4827能够抑制携带有天然BRCA-1和BRCA-2突变的癌细胞的增殖、通过RNA干扰抑制BRCA-1缺陷的Hela细胞的生长。在携带BRCA-1突变的MDA-MB-436人类乳腺腺癌的细胞中，MK-4827的CC50=18 nM；而在BRCA-2缺陷的CAPAN-1人胰腺癌细胞中，CC50=90 nM。而正常人类前列腺和乳腺上皮细胞对MK-4827具有耐药性，在微摩尔范围内具有抗凋亡作用，说明这些PARP抑制剂在具有BRCA-1和BRCA-2突变的癌细胞中具有选择性细胞毒性，对周围组织影响小[2]。 | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | BRCA1基因沉默的Hela细胞 | ||
| 浓度 | 系列稀释浓度 | |||
| 孵育时间 | 7天 | |||
| 方法 | 将细胞置于96孔黑色viewplates中，细胞密度为300/孔，每孔含190 μLDMEM培养基(含10%胎牛血清，0.1 mg/mL青-链霉素双抗，2 mM L-谷氨酰胺)，在37℃、5% CO2的细胞培养箱中培养4小时。将系列稀释的抑制剂加入其中，每孔10 μL，使化合物浓度达到工作浓度、DMSO为0.5%。然后在细胞在细胞培养箱中培养7天。7天后，测定细胞活力。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | c-PARP /c-caspase 3 / γ-H2AX |
|
29158830 | |
| Immunofluorescence | Rad51 / Geminin |
|
27614696 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | MK-4827能够显著增强辐射对人类肿瘤移植体（p53野生型或p53突变型）的效果[1]。在体内实验中，其耐受良好。单独使用时，在BRCA-1缺陷型移植瘤模型中具有一定功效[2]。 | |
|---|---|---|
| 动物实验 | Animal Models | 雌性裸鼠 |
| Dosages | 25 mg/kg每日两次或50 mg/kg每日一次 | |
| Administration | 口服 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05289648 | Not yet recruiting | Endometrial Cancer|Serous Adenocarcinoma|Uterine Neoplasm | Sir Mortimer B. Davis - Jewish General Hospital | May 1 2023 | Early Phase 1 |
| NCT04149145 | Not yet recruiting | Ovarian Cancer Recurrent | University of Alabama at Birmingham | December 2022 | Phase 1 |
| NCT05406700 | Recruiting | Low-grade Glioma|IDH2 Gene Mutation|Recurrent Glioma|IDH1 Mutation|Glioma Malignant | Massachusetts General Hospital|GlaxoSmithKline | November 2022 | Early Phase 1 |
| NCT05442749 | Recruiting | Metastatic Pancreatic Cancer | Centre Leon Berard|GlaxoSmithKline | October 28 2022 | Phase 2 |
| NCT05335993 | Recruiting | Recurrent Ovarian Cancer|Recurrent Epithelial Cancer of Ovary|Recurrent Epithelial Ovarian Cancer|Recurrent Fallopian Tube Cancer|Peritoneal Cancer|Recurrent Carcinoma of Ovary|Adenocarcinoma of Ovary | CanariaBio Inc.|Veristat LLC | July 25 2022 | Phase 2 |
化学信息&溶解度
| 分子量 | 320.39 | 分子式 | C19H20N4O |
| CAS号 | 1038915-60-4 | SDF | Download Niraparib (MK-4827) SDF |
| Smiles | C1CC(CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 64 mg/mL ( 199.75 mM； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 64 mg/mL Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
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点击购买：
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实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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如果有其他问题，请给我们留言。
* 必填项
常见问题及建议解决方法
问题 1:
How to reconstitute the compound for in vivo studies?
回答：
You can use the formulation 1% CMC-Na (suspension) for oral administration.
PARP相关信号通路图
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