Niraparib (MK-4827)

For research use only. Not for use in humans.

目录号:S2741 中文名称:尼拉帕尼

Niraparib (MK-4827) Chemical Structure

CAS No. 1038915-60-4

Niraparib (MK4827)是一种口服有效的选择性PARP-1PARP-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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1392.3 现货
RMB 1419.74 现货
RMB 7933.56 现货
RMB 20229.3 现货
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客户使用Selleck生产的Niraparib (MK-4827)发表文献54篇:

产品安全说明书

PARP抑制剂选择性比较

生物活性

产品描述 Niraparib (MK4827)是一种口服有效的选择性PARP-1PARP-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
PARP2 [1]
(Cell-free assay)
PARP1 [1]
(Cell-free assay)
2.1 nM 3.8 nM
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells MYLGeY5kfGmxbjDhd5NigQ>? NWfjSZB5UW6qaXLpeIlwdiCxZjDQRXJRKGmwIHj5[JJw\2WwIIDldo95cWSnLXnu[JVk\WRiaIXtZY4hUGWOYTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJGRPSS2mYX3h[4UucW6mdXPl[EBRSVK7bHH0bY9vNCCHQ{WwQVAvODB2IN88US=> NEfQd5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi3N|k5OSd-MUm4O|M6QDF:L3G+
A549 cells NYLKeIpQS3m2b4TvfIlkcXS7IHHzd4F6 NIDWTJY2NTdiZHH5dy=> NGDTT2xEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSlKFQUKgd4hTVkFiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPSC2bzC3JIRigXNiYomgR4VtdFSrdHXyMWJtfWViYYPzZZktKEOFNUC9NE4xOTFizszN MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
MDA-MB-436 cells M4\nfHBzd2yrZnXyZZRqd25iYYPzZZk> NV:3UlZFPiCmYYnz M1zuN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR|NjDj[YxteyCneIDy[ZN{cW6pIFLSR2EyKDV|OU[gL{AyTz6DIH31eIFvfCCjZoTldkA3KGSjeYOgZpkh[2WubDD0bZRmei2kbIXlJIF{e2G7LDDDR|UxRTF6IH7N MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh5M{m4NUc,OTl6N{O5PFE9N2F-
SUM1315MO2 cells MnjyR5l1d3SxeHnjbZR6KGG|c3H5 MV:xNkBl[Xm| MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTWW0yOzF3TV:yJINmdGy|IHPhdpJ6cW6pIFLSR2EyKG23dHHueEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjCxNkBl[Xm|IHL5JGNmdGyWaYTldk1DdHWnIHHzd4F6NCCFQ{WwQVAvODJizszN Mmf3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
DoTc2-4510 cells M1\yeGN6fG:2b4jpZ4l1gSCjc4PhfS=> MoHCOU04KGSjeYO= MlHZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSI9V[zJvNEWxNEBk\WyuczDjZZJzgWmwZzDCVmNCOiCvdYThcpQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgOUB1dyB5IHThfZMh[nliQ3XscHRqfGW{LVLseYUh[XO|YYmsJGNEPTB;MD6wNlMh|ryP MknDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
SUM149PT cells Mm\vR5l1d3SxeHnjbZR6KGG|c3H5 MWO1MVch\GG7cx?= MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTWW0yPDmSVDDj[YxteyClYYLyfYlv\yCEUlPBNUBufXSjboSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiNTD0c{A4KGSjeYOgZpkhS2WubGTpeIVzNUKudXWgZZN{[XluIFPDOVA:OC5yMkSg{txO MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
UWB1.289 cells NIjSZ5hEgXSxdH;4bYNqfHliYYPzZZk> M4PON|UuPyCmYYnz MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVW2IyNjJ6OTDj[YxteyClYYLyfYlv\yCEUlPBNUBufXSjboSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiNTD0c{A4KGSjeYOgZpkhS2WubGTpeIVzNUKudXWgZZN{[XluIFPDOVA:OC5yNU[g{txO MkTaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Capan1 cells MmfMR5l1d3SxeHnjbZR6KGG|c3H5 Ml3vR5l1d3SxeHnjbZR6KGGpYXnud5QhSlKFQUKt[IVncWOrZX70JIh2dWGwIFPhdIFvOSClZXzsd{whS0N3ME2wMlA6KM7:TR?= NYLOb4xiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
Jurkat cells MVTGeY5kfGmxbjDhd5NigQ>? M1vvWWlvcGmkaYTpc44hd2ZiUFHSVFEhcW5iaIXtZY4hUnW{a3H0JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iClZXzsJJZq[WKrbHn0fUBi\nSncjC5OkBpenNiYomgUXRUKGG|c3H5JIlvKHC{ZYPlcoNmKG:oIEGwNEB2VSCxZjD0[Y1wgm:ub33p[IUtKEWFNUC9NE4zKM7:TR?= NVKzPHppRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OVAyQTlpPkKzPFUxOTl7PD;hQi=>
BT20 cells NHfKXZlEgXSxdH;4bYNqfHliYYPzZZk> NIS5V3Q2NTdiZHH5dy=> NW\SU3Z1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSlR{MDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA2KHSxIEeg[IF6eyCkeTDD[YxtXGm2ZYKtRox2\SCjc4PhfUwhS0N3ME2yMlIh|ryP NV\0RllLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
Antiproliferative assay MoDtTIVN[Q>? NUG1bVNsPyCmYYnz MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFLSR2EyKGSnZnnjbYVvfCCqdX3hckBJ\UyjIHPlcIx{KGGodHXyJFch\GG7czDifUBk\WyuIITpeIVzNWKudXWgZZN{[XluIFPDOVAhRSByLkCzN{DPxE1w NYjxU4NbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4O|M6QDFpPkG5PFc{QThzPD;hQi=>
Function assay NGfTN5BJ\Uyj MoLITY5pcWKrdHnvckBw\iCSQWLQJIlvKGi7ZILv[4VvKHCncn;4bYRmNWmwZIXj[YQhcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIFTORU1l[W2jZ3WtbY5lfWOnZDDQRXJ6dGG2aX;uMEBGSzlyIE2gNE4xPDVizszNMi=> NFLa[YE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUi3N|k5OSd-MUm4O|M6QDF:L3G+
Antiproliferative assay NEHCNG1E[XCjbkG= NFTPZ3gyOyCmYYnz MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOjcHHuNUBk\WyuczDlfJBz\XO|aX7nJGJTS0F{IE[xO|Rl\WyWIH31eIF1cW:wIHHu[EBtd3O|IH;mJJdqdGRvdInw[UBidGynbHWgZYZ1\XJiMUOg[IF6eyCkeTDj[YxtKHSrdHXyMYJtfWViYYPzZZktKEOFNUCgQUAxNjB7IN88UU4> MnfpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6N{O5PFEoRjF7OEezPVgyRC:jPh?=
Antiproliferative assay NG\uV4JJ\Uyj MmPtO{Bl[Xm| NGSzOYdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOg[ZhxemW|c3nu[{B4cWymIIT5dIUhSlKFQUGgZYZ1\XJiNzDkZZl{KGK7IHPlcIwhfGm2ZYKtZox2\SCjc4PhfUwhS0N3MDC9JFAvQDZizszNMi=> Mmr1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6N{O5PFEoRjF7OEezPVgyRC:jPh?=
Function assay MkXxTpVzc2G2 NXLtcYtuQTZiaILz MV;Jcohq[mm2aX;uJI9nKFCDUmCxJIlvKGi3bXHuJGp2emujdDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4Yh[2WubDD2bYFjcWyrdImgZYZ1\XJiOU[gbJJ{KGK7IF3UV{Bie3OjeTygSWM2OCB;IEOxJO69VS5? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3MEG5PUc,OjN6NUCxPVk9N2F-
Function assay NF7CcGRESVCDTj2x MnGzTY5pcWKrdHnvckBw\iCSQWLQJIlvKEKUQ1GyMYRm\mmlaXXueEBpfW2jbjDDRXBCVi1zIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhcHmmcn;n[Y4heGW{b4jp[IUucW6mdXPl[EBRSVK7bHH0bY9vKGK7IHPlcIwu[mG|ZXSgZZN{[XluIFnDOVAhRSByLkCwN|Uh|ryPLh?= NV;he4Q1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
Function assay M{LaVWhmVGF? MmX6TY5pcWKrdHnvckBw\iCSQWLQJIlvKGi3bXHuJGhmVGFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgWS{b3flckBx\XKxeHnk[U1qdmS3Y3XkJHBCWnmuYYTpc44h[nliY3XscE1j[XOnZDDhd5NigSxiRVO1NEA:KDBwMEC0JO69VS5? NVTVfGNLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
Function assay NYfUR5FVSTJ5OEC= MYLJcohq[mm2aX;uJI9nKFCDUmCgbY4hcHWvYX6gRVI4QDBiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgWS{b3flckBx\XKxeHnk[U1qdmS3Y3XkJHBCWnmuYYTpc44h[nliY3XscE1j[XOnZDDhd5NigSxiSVO1NEA:KDBwMEC0JO69VS5? NWH0T2dNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
Cytotoxicity assay MXXNSGEuVUJvNEO2 MkHMR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDjZZJzgWmwZzDCVmNCOSCvdYThcpQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44tKEOFNUCgQUAxNjBzODFOwG0v M1vj[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Cytotoxicity assay MnrjTIVN[Q>? NXzJfWRrPSC2bzC3JIRigXN? NIrEXoFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\UyjIHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghSlKFQUGgd4hTVkFiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGOnbHygeoli[mmuaYT5JIFnfGW{IEWgeI8hPyCmYYnzJIJ6KEOnbHzUbZRmei2EbIXlJIF{e2G7LDDDR|UxKD1iMD6wN|Qh|ryPLh?= M3;RbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Function assay NVXEdGFiUGWOYR?= Mn;qTY5pcWKrdHnvckBw\iCSQWLQJIlvKGi3bXHuJGhmVGFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBpgWS{b3flckBx\XKxeHnk[U1qdmS3Y3XkJHBCWnmuYYTpc44h[nliY3XscE1j[XOnZDDhd5NigSxiSVO5NEA:KDBwMES2JO69VS5? MkTMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Function assay Ml64R2FRSU5vMR?= Ml;wTY5pcWKrdHnvckBw\iCSQWLQJIlvKEKUQ1GyMYRm\mmlaXXueEBpfW2jbjDDRXBCVi1zIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhcHmmcn;n[Y4heGW{b4jp[IUucW6mdXPl[EBRSVK7bHH0bY9vKGK7IHPlcIwu[mG|ZXSgZZN{[XluIFnDPVAhRSByLkC1JO69VS5? NUHCPFc5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OlExQTZpPkK1O|YyODl4PD;hQi=>
Function assay M3LpZmEzPzhy NFTOcWVKdmirYnn0bY9vKG:oIGDBVnAhcW5iaIXtZY4hSTJ5OECgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCqeXTyc4dmdiCyZYLvfIll\S2rbnT1Z4VlKFCDUonsZZRqd25iYomgZ4VtdC2kYYPl[EBie3OjeTygTWM6OCB;IECuNFUzKM7:TT6= NHLGSGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Cytotoxicity assay MVvI[Wxi MkPTOUB1dyB5IHThfZM> NVjIXGViS3m2b4TvfIlkcXS7IHHnZYlve3Rid3ns[EB1gXCnIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPSC2bzC3JIRigXNiYomgR4VtdFSrdHXyMWJtfWViYYPzZZktKEOFNUCgQUAxNjh3MjFOwG0v M2KxbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{[xNFk3Lz5{NUe2NVA6PjxxYU6=
Cytotoxicity assay NXPqXmtxXVeEMT6yPFk> M4\0OlUhfG9iNzDkZZl{ MoLGR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWXdDOS5{OEmgZ4VtdHNiZYjwdoV{e2mwZzDCVmNCOSCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA2KHSxIEeg[IF6eyCkeTDD[YxtXGm2ZYKtRox2\SCjc4PhfUwhS0N3MDC9JFAvQTd3IN88UU4> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Cytotoxicity assay Ml7WRVU1QQ>? M1PnUFUhfG9iNzDkZZl{ NHPHd3hEgXSxdH;4bYNqfHliYXfhbY5{fCC5aXzkJJR6eGViaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA2KHSxIEeg[IF6eyCkeTDD[YxtXGm2ZYKtRox2\SCjc4PhfUwhS0N3MDC9JFEvPzZizszNMi=> NEK3XnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe2NVA6Pid-MkW3OlExQTZ:L3G+
Cytotoxicity assay MmXiR4Fx[W5z NFW1NllEgXSxdH;4bYNqfHliYXfhbY5{fCCEUlPBNk1l\W[rY3nlcpQhcHWvYX6gR4Fx[W5zIHPlcIx{NCCHQ{WwJF0hOC54NTFOwG0v NX7wZXliRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI4OTdpPkK2OlUzPzF5PD;hQi=>
Antitumor assay MWrNSGEuVUJvNEO2 MoT1OVAhdWdxa3e= MVOzN{Bl[Xm| M1nybWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{[gZ4VtdHNiZYjwdoV{e2mwZzDCVmNCOSB3M{m2JEshOUd-QTDteZRidnRieHXuc4dz[W[2ZXSgbY4hS0RzIH3veZNmKGG|c3Xzd4VlKGG|IIT1cY9zKHKnZ4Lld5Nqd25iYYSgOVAhdWdxa3esJJBwKGKrZDDmc5IhOzNiZHH5dy=> M2LhN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEezPVgyLz5zOUi3N|k5OTxxYU6=
Antitumor assay NUG0eWhyVUSDLV3CMVQ{Pg>? MWSxNFAhdWdxa3e= NHLFRmU{OyCmYYnz NYrKO5BoSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOkBk\WyuczDlfJBz\XO|aX7nJGJTS0FzIEWzPVYhMyBzR{7BJI12fGGwdDD4[Y5w\3KjZoTl[EBqdiCFREGgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JicnXndoV{e2mxbjDheEAyODBibXevb4ctKHCxIIHkJIZweiB|MzDkZZl{ MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh5M{m4NUc,OTl6N{O5PFE9N2F-
Antitumor assay NHHrNXZOTEFvTVKtOFM3 NHzDOpI5OCCvZz;r[y=> NYjNU5FoOSC2bzCyJJdm\Wu| MWHBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN4IHPlcIx{KGijcnLvdolv\yCEUlPBNUBufXSjboSgfIVvd2e{YX\0[YQhcW5iaX3teY5w[2:vcILvcYl{\WRibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[XRiOECgcYcwc2duIIDvJJFlKG[xcjCxJJRwKDJid3Xlb5M> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Antitumor assay NEHmWGJOTEFvTVKtOFM3 M4LzWFgxKG2pL3vn M4\FPFQhf2Wna4O= MUfBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN4IHPlcIx{KGijcnLvdolv\yCEUlPBNUBufXSjboSgfIVvd2e{YX\0[YQhcW5iaX3teY5w[2:vcILvcYl{\WRibX;1d4Uh[XO|ZYPz[YQh[XNiY3;tdIxmfGViYX7kJJN2e3SjaX7l[EB1fW2xcjDy[Ydz\XO|aX;uJIF1KDhyIH3nM4toNCCybzDx[EBnd3JiNDD3[YVsew>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd4MUC5Okc,OjV5NkGwPVY9N2F-
Antitumor assay MVTNSGEuVUJvNEO2 MVK1NEBu\y:tZx?= M2PPPGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{[gZ4VtdHNiaHHyZo9zcW6pIFLSR2EyKG23dHHueEB5\W6xZ4Lh[pRm\CCrbjDpcY12dm:lb33wdo9ucXOnZDDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiCpcn;3eIghcW6qaXLpeIlwdiCjdDC1NEBu\y:tZzygdI8h[WSvaX7pd5RmemWmIHThbYx6 MmjHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
Antitumor assay NVnyfFhPVUSDLV3CMVQ{Pg>? MlKwPFAhdWdxa3e= M4PIe|Mhf2Wna4O= NH\ITVdCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO2JINmdGy|IHjhdoJwemmwZzDCVmNCOSCvdYThcpQhgGWwb3fyZYZ1\WRiaX6gbY1ufW6xY3;tdJJwdWm|ZXSgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3Jic3jybY5s[WenIHH0JFgxKG2pL3vnMEBxdyCzZDDmc5IhOyC5ZXXrdy=> MmDkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NkGwPVYoRjJ3N{[xNFk3RC:jPh?=
qHTS assay NHXPfGpVSzN{ MXTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? MoW0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
qHTS assay M2[xTWE3PzN? MnPXdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay M4P6Um5DOTZ2Mx?= MmnUdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= M3jqU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay M{O3cGE3PzN? NHHYVIdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBCPjd|IHPlcIx{MQ>? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay NGjnZWhDXC1|Nx?= M1LmUZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGJVNTN5IHPlcIx{ M4jUT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay M36zUHNMNU5vTVO= NILNVpRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> NWC4cpZmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
qHTS assay M{PGcW5DNUWEY{G= NYrsSWxWeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
qHTS assay MY\MRW4uPQ>? M1\Ne5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= NGfxNGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
qHTS assay M2TndXNMNU5vTVO= MlfhdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2PQzDj[Yxtew>? M3X4RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
qHTS assay NITGN4lVSzN{ MmTKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWGM{OiClZXzsdy=> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
c-PARP /c-caspase 3 / γ-H2AX; 

PubMed: 29158830     


Western Blot data testing protein expression after treatment with Olaparib, Niraparib, and Talazoparib on Brca1-deficient cell line in W0069 cells.

29158830
Immunofluorescence
Rad51 / Geminin; 

PubMed: 27614696     


Immunofluorescence microscopy of niraparib-treated PDX cells (PH039) and irradiated cells showing RAD51 foci (arrow) within geminin positive cells and lack of RAD51 foci formation in control cells. 

27614696
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[2]
- 合并
  • Cell lines: BRCA1基因沉默的Hela细胞
  • Concentrations: 系列稀释浓度
  • Incubation Time: 7天
  • Method: 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。
    (Only for Reference)
动物实验:[1]
- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 64 mg/mL warmed (199.75 mM)
Water Insoluble
Ethanol '64 mg/mL
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+40% PEG 300+5% Tween 80+ 50% ddH2O
2.5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 320.39
化学式

C19H20N4O

CAS号 1038915-60-4
储存条件 粉状
溶于溶剂
别名

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04149145 Not yet recruiting Drug: M4344+Niraparib Ovarian Cancer Recurrent University of Alabama at Birmingham December 2021 Phase 1
NCT04986371 Not yet recruiting Drug: Niraparib Epithelial Ovarian Cancer Ling-Ying Wu|Chinese Academy of Medical Sciences August 10 2021 --
NCT04972110 Recruiting Drug: RP-3500 Advanced Solid Tumor Adult Repare Therapeutics July 21 2021 Phase 1|Phase 2
NCT04655183 Withdrawn Drug: Niraparib|Drug: M4344 Advanced Solid Tumor|Breast Cancer EMD Serono Research & Development Institute Inc.|Merck KGaA Darmstadt Germany|EMD Serono December 1 2020 Phase 1|Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

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 Signaling Pathway Map

相关PARP产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID