Rucaparib (AG-014699,PF-01367338) phosphate

目录号:S1098

Rucaparib (AG-014699,PF-01367338) phosphate Chemical Structure

Molecular Weight(MW): 421.36

Rucaparib (AG-014699,PF-01367338)是一种PARP抑制剂,无细胞试验中作用于PARP1的Ki为1.4 nM,对其余8个PARP位点也有结合亲和力。Phase 3。

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产品安全说明书

PARP抑制剂选择性比较

生物活性

产品描述 Rucaparib (AG-014699,PF-01367338)是一种PARP抑制剂,无细胞试验中作用于PARP1的Ki为1.4 nM,对其余8个PARP位点也有结合亲和力。Phase 3。
特性 AG-014699是第一个用于人类癌症疗法的PARP 抑制剂。
靶点
PARP [1]
(Cell-free assay)
1.4 nM(Ki)
体外研究

AG-014699有效抑制纯化的全长人类PARP-1,作用于LoVo和SW620细胞显示出强PARP抑制效果。AG-014699是AG14447的磷酸盐形式,且是第一个和temozolomide联用用于临床实验的PARP抑制剂。[1] AG-014699的辐射增敏性是由于下游NF-κB激活的抑制,及SSB修复抑制。AG-014699可以作用于DNA损伤激活的NF-κB,且克服传统NF-κB抑制剂的毒性,不会损害其他重要的炎症反应。[2]1μM AG-014699作用于D283Med细胞时抑制PARP-1活性达97.1%。[3]在NB-1691, SH-SY-5Y, 和SKNBE(2c)细胞中AG-014699明显增强Topotecan和Temozolomide的细胞毒性。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT-474 M4npVGZ2dmO2aX;uJGF{e2G7 MoLxNE4yNzFxNUCwM|ExODBibl2= MlHQbY5pcWKrdIOgVGFTWCCjY4Tpeol1gSCjdDDzeIFzfGmwZzDjc45k\XKwdILheIlwdiCxZjC1NFAhdk1? MYWyOVEzQDR3NR?=
BT474 NVXrW3B2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{ToW|UxOCCwTR?= NUHPN|Q4OTEkgKOxOeKh\A>? NUDL[ohXemWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>? MlHjNlUyOjh2NUW=
SKBR3 NEDucFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPIOVAxKG6P NFW0TnkyOOLCk{G1xsBl NX;RUpNHemWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>? M1TnTFI2OTJ6NEW1
AU565 NYe0W3V3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUKxXHpxPTByIH7N NF;zSIoyOOLCk{G1xsBl NUfPfodEemWmdXPld{Bk\WyuIHfyc5d1cCCrbjD0bIUh\m:3cjDsbY5meyCjbnSgd4lodmmoaXPhcpRtgQ>? NWLmZ4FyOjVzMki0OVU>
EFM192A NY\MbZY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3O5SVUxOCCwTR?= MmPTNVDjiJNzNdMg[C=> NF3hcFlz\WS3Y3XzJINmdGxiZ4Lve5RpKGmwIITo[UBnd3W{IHzpcoV{KGGwZDDzbYdvcW[rY3HueIx6 M4fNN|I2OTJ6NEW1
MDA-MB-231 MmC1SpVv[3Srb36gRZN{[Xl? NWL2Um5LOTBxMkCvOFAh|ryP NIjnfoczPCCq MUHpcoNz\WG|ZYOgdE1CU1RibHX2[Yx{KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXHtUWpEOjR2MkCxOVI>
MDA-MB-231 MkDzR4VtdCCYaXHibYxqfHliQYPzZZk> MYmwMlEuPDBizszN M{DiVFI1KGh? MYLJR|Ux6oDLPfMAjVE4Njd5wrFOwG0> M17BUlI1PDJyMUWy
MDA-MB-231 MVHBdI9xfG:|aYOgRZN{[Xl? MnTuNVAwOjBxNECg{txO NYX6bJdyOjRiaB?= Mlv3bY5lfWOnczDhdI9xfG:|aYOg[I9{\SCmZYDlcoRmdnSueR?= Mlu4NlQ1OjBzNUK=
MDA-MB-231 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TLfVExNzJyL{SwJO69VQ>? MWeyOEBp NF\IOIpjdG:la4OgZ4VtdCCleXPs[UBxem:pcnXzd4lwdiCrbjDHNk9OKHCqYYPl MkjrNlQ1OjBzNUK=
H460 NEfaRlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3GySlQxOCCwTR?= NIfBUYszPMLiaB?= MUjpcoNz\WG|ZYOgZ4VtdHWuYYKgdoFlcW:|ZX7zbZRqfmm2eR?= NGPwWGYzPDRzMU[xNS=>
A549  MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrnOFAxKG6P MlnuNlTDqGh? NH;qVoRqdmO{ZXHz[ZMh[2WubIXsZZIhemGmaX;z[Y5{cXSrdnn0fS=> M1LVV|I1PDFzNkGx
DT40 NE\HfIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTJzIH7N M{LlSFI1OzV4OEGz
DU145 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\jXHZGUUN3ME2xPEBvVQ>? NGrsSlMzPDN3NkixNy=>
COLO704 NXXucFNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHqTWM2OD1{LkWyJOKyKDBwNkeg{txO M4jSTVI{PzJ7NECy
OVMANAb NYfPS4RIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTJwNUigxtEhOC5|ODFOwG0> NIq3eZgzOzd{OUSwNi=>
OV177 NVHafY9vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTJwN{igxtEhOC55MTFOwG0> M4Ho[lI{PzJ7NECy
OAW28 NFTsfZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTNwNkGgxtEhOC5{ODFOwG0> MY[yN|czQTRyMh?=
OVSAHO NYnzXJJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LZbmlEPTB;Mz62OEDDuSByLkOzJO69VQ>? NVXteox4OjN5Mkm0NFI>
OVKATE MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLQTWM2OD1|Lk[0JOKyKDFwN{mg{txO M2TFNFI{PzJ7NECy
OVCAR3 NV7HSIoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTNwN{SgxtEhOC52MDFOwG0> MVGyN|czQTRyMh?=
PEO14 MnzsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHj[FhKSzVyPUOuPFQhyrFiMD63OkDPxE1? NUDlbpNSOjN5Mkm0NFI>
A2780 NX[5dlZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULF[FQyUUN3ME2zMlk1KMLzIECuNlUh|ryP MV6yN|czQTRyMh?=
OVTOKO MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXO0XlRtUUN3ME20MlE1KMLzIEGuOVMh|ryP M3nvU|I{PzJ7NECy
KURAMOCHIb M3vzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDncWlKSzVyPUSuN|QhyrFiMD6yPUDPxE1? NIfOOFczOzd{OUSwNi=>
TOV21G NUnucHlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3R[o4xUUN3ME21MlA4KMLzIEGuN|Ah|ryP NU[wVGo{OjN5Mkm0NFI>
OVISE MmTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnr6TWM2OD13Lk[4JOKyKDBwMkOg{txO M1S2PVI{PzJ7NECy
KK MknMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlm4TWM2OD14LkG1JOKyKDFwNEKg{txO MWCyN|czQTRyMh?=
RMUGS NHj6SIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vTUWlEPTB;Nz6wN{DDuSBzLkizJO69VQ>? MViyN|czQTRyMh?=
PEO6 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HPXWlEPTB;Nz6wOkDDuSByLke0JO69VQ>? MonwNlM4Ojl2MEK=
OVCA429 M1LZ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nhW2lEPTB;OD6yPUDDuSBzLk[0JO69VQ>? NIT6T2UzOzd{OUSwNi=>
OV167 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXWeZlKSzVyPUiuN|MhyrFiMT6xPEDPxE1? MnfoNlM4Ojl2MEK=
RMG1 MoLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTlwM{KgxtEhOi5|NjFOwG0> MYSyN|czQTRyMh?=
OVCAR5 NEDoS|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjVTWM2OD17LkWwJOKyKDJwNUmg{txO NV31RZhIOjN5Mkm0NFI>
EFO21 M3\2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTlwOUKgxtEhOS56NzFOwG0> NY\SO2l4OjN5Mkm0NFI>
ES2 MofWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MluwTWM2OD1zMD6xNkDDuSBzLkKzJO69VQ>? MmDjNlM4Ojl2MEK=
Tyk-nu M3HZN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDzS5JbUUN3ME2xNE4zOCEEsTCxMlEzKM7:TR?= Ml7BNlM4Ojl2MEK=
CAOV3 NX3yOolLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3X5PWlEPTB;MUCuN|chyrFiMD64O{DPxE1? MUWyN|czQTRyMh?=
OV207 MnXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rHXGlEPTB;MUKuNlchyrFiMD6zNkDPxE1? M{G0PFI{PzJ7NECy
HEY MlzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jxT2lEPTB;MUOuNFEhyrFiMD63OUDPxE1? NYrwSFV4OjN5Mkm0NFI>
DOV13 NI\CfnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHzTWM2OD5zNTFOwG0> MnPTNlM4Ojl2MEK=
EFO27 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFiydZZKSzVyPkG1JO69VQ>? NX\0SZpJOjN5Mkm0NFI>
HEY C2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFH6d3lKSzVyPkG1JO69VQ>? M4DC[FI{PzJ7NECy
KOC-7cc MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HRZWlEPTB-MUWg{txO NUGxVY9zOjN5Mkm0NFI>
MCASb NIHZO3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInLcm9KSzVyPkG1JO69VQ>? M2DnflI{PzJ7NECy
OAW42 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPDTWM2OD5zNTFOwG0> MY[yN|czQTRyMh?=
OV2008 M2jWNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRjF3IN88US=> MX:yN|czQTRyMh?=
OV90 MmLBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRjF3IN88US=> NW\BdFFXOjN5Mkm0NFI>
OVCA420b MnnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrpWIxKSzVyPkG1JO69VQ>? M1[wW|I{PzJ7NECy
OVCA432 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHUcYlpUUN3ME6xOUDPxE1? M1\5PVI{PzJ7NECy
PEA2 NVeyN|NrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfaR5VKSzVyPkG1JO69VQ>? NWG4SlZ3OjN5Mkm0NFI>
SKOV3 NWfCbldIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRjF3IN88US=> NWrS[4lEOjN5Mkm0NFI>
TOV112D MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFyyOHYxNTNizszN MXnJR|UxRjF3IN88US=> NEDW[nMzOzd{OUSwNi=>
C4-2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDYSo1uOC1|IN88US=> NWnue5BOOTRiZB?= NI\rZm5FVVOR NV7SSolF\GWlcnXhd4V{KGOxbH;ufUBvfW2kZYKg[I9{\SCmZYDlcoRmdnSueR?= NXnqOZI3OjN3NkWyOFQ>
PC3 NES1[IFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmniNE0{KM7:TR?= M4XqZ|E1KGR? NVLFNFNWTE2VTx?= M1TZTYRm[3KnYYPld{Bkd2yxbomgcpVu[mW{IHTvd4Uh\GWyZX7k[Y51dHl? MWCyN|U3PTJ2NB?=
DU145 M4P5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfxcFcxNTNizszN M4nHe|E1KGR? NXfWZoR4TE2VTx?= NHvafmRl\WO{ZXHz[ZMh[2:ub375JI52dWKncjDkc5NmKGSncHXu[IVvfGy7 NITTOYozOzV4NUK0OC=>
VCaP  MkP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Hy[VAuOyEQvF2= MWexOEBl NWfYO5ROTE2VTx?= MX;k[YNz\WG|ZYOgZ49td267IH71cYJmeiCmb4PlJIRmeGWwZHXueIx6 NWexfnA1OjN3NkWyOFQ>
LNCaP  NWm5[lRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqwMVMh|ryP NEHzUngyPCCm MVnEUXNQ M1nNe4Rm[3KnYYPld{Bkd2yxbomgcpVu[mW{IHTvd4Uh\GWyZX7k[Y51dHl? MoPMNlM2PjV{NES=
MDA-MB-468 M{LVOmNmdGxiVnnhZoltcXS7IFHzd4F6 MYjJR|UxRTlwNzFOwG0> NYC2Zmt7OjJ4N{ixOlE>
MDA-MB-231 M4\NSmNmdGxiVnnhZoltcXS7IFHzd4F6 MnHKTWM2OD1zMzFOwG0> M1\FdVIzPjd6MU[x
Cal-51 MYDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkHOTWM2OD16Lk[g{txO NFj1eWMzOjZ5OEG2NS=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PAR; 

PubMed: 27960087     


MCF-7 cells were pretreated ± Rucaparib (15 µM, 2 hr), then ± Rucaparib (15 µM) or two different doses of β-lap (2.0 or 5.0 µM) for 2 hr. Levels of PAR (PARP hyperactivation) formation were assessed with α-tubulin as loading controls.

BRCA1; 

PubMed: 24085845     


MCF7 cells, MDA-MB-436 parental cells and resistant clones RR-1, RR-5, and RR-6 were treated with DMSO (−) or 1 µM rucaparib (+) for 24 h, and BRCA1 protein levels were assessed by using BRCA1 N- or C-terminal-specific antibodies by Western blot. 

27960087 24085845
Growth inhibition assay
Cell viability; 

PubMed: 31119062     


The effect of rucaparib on proliferation of keloid fibroblasts. (A) Keloid cell growth following treatment with rucaparib at various concentration (0, 2, 10, 20 μM) was evaluated by MTT assays. Data are expression as mean standard deviation of percent changes of triplicate optical densities. (B) Rucaparib (20 μM) significantly decreased proliferation of keloid fibroblasts. The combination of rucaparib (20 μM) and triamcinolone (50 μM) showed additive suppressive effect on keloid fibroblasts as compared with rucaparib single therapy. Data are expression as mean standard deviation of percent changes of triplicate optical densities. MTT, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide.

31119062
Immunofluorescence
α-tubulin; 

PubMed: 30589644     


Representative immunofluorescence images of DMSO-, rucaparib- (Ruca-), and Ola-exposed A549-ERCC1(WT/WT) and A549-ERCC1(–/–) cells. Cells were exposed to 15 μM Ruca or 40 μM Ola during 72 hours. White arrows, CCFs; yellow arrows, micronuclei. Scale bar: 20 μm. 

PAR; 

PubMed: 27515310     


Cells were treated with 20 mM hydrogen peroxide (H2O2) in order to stimulate PARP-1 activity in the presence or absence of the PARP-1 inhibitors rucaparib and olaparib. Poly(ADP-ribose) (PAR) chain synthesis was detected using an anti-PAR monoclonal Alexa Fluor 488-conjugated antibody (green). The nucleus was visualised using the nuclear counterstain DAPI (blue). Representative images obtained from the analysis of anti-PAR staining of SK-N-BE(2c) cells are shown.

γH2AX; 

PubMed: 23565244     


γH2AX foci was determined by immunofluoresecence microscopy at 24 h following combined treatment with radiation and rucaparib in PC3 and LNCaP cells. 

53BP1; 

PubMed: 23565244     


53BP1 foci was determined by immunofluoresecence microscopy at 24 h following combined treatment with radiation and rucaparib in PC3 and LNCaP cells.

30589644 27515310 23565244
体内研究 AG-014699无毒,明显增强D384Med移植瘤DNA修复功能蛋白中temozolomide诱导的TGD。药物动力学研究显示在脑组织中也检测到AG-014699,说明AG-014699用于治疗颅内恶性肿瘤具有潜在可能。[3]活体模型(NB1691和SHSY5Y移植瘤)研究显示AG-014699增强temozolomide的抗癌活性,产生彻底且持久的肿瘤衰退现象。[4]

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)

激酶实验:[3]
+ 展开

激酶实验:

不同浓度(0到1μ)AG-014699作用于5×103D283Med 细胞,与只用DMSO处理5×103D283Med细胞相比,来测定PARP活性抑制率。参考GCLP验证试验的PAR标准曲线,在和NAD+及寡核苷酸(底物和激活剂)温育的6分钟期间,使用10H PAR抗体,通过PAR形成量的免疫检测,在细胞样本中测量最大程度刺激的PARP活性。
细胞实验: [3]
+ 展开
  • Cell lines: D425Med, D283Med和D384Med细胞
  • Concentrations: 0.4 μM
  • Incubation Time: 3或5天
  • Method: 髓母细胞瘤细胞系包含D425Med, D283Med,和D384Med细胞,分别按1×103, 3×103,和3×103密度接种在96孔板上。接种24小时(D384Med细胞)或48小时(D283Med和D425Med细胞)后,细胞用不同浓度temozolomide处理。培养3天(D425Med和D384Med细胞)或5天(D283Med细胞)后,通过XTT细胞增殖检测试剂盒检测细胞活力。用DMSO处理的对照组和0.4μ AG-014699处理的实验组的百分比表示细胞生长。计算temozolomide单独使用或者和AG-014699联用时的GI50值。Temozolomide单独使用时的GI50值和与AG-014699联用时的GI50值之比就是趋化因子50(PF50)值。
    (Only for Reference)
动物实验:[3]
+ 展开
  • Animal Models: 携带D283Med移植瘤的CD-1裸鼠
  • Formulation: 盐水溶液
  • Dosages: 1 mg/kg
  • Administration: 腹腔注射,每天1次或4次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 84 mg/mL (199.35 mM)
Water Insoluble
Ethanol Insoluble
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):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
10mg/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 421.36
化学式

C19H18FN3O.H3PO4

CAS号 459868-92-9
稳定性 powder
in solvent
别名 N/A

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 (g) = 浓度 (mol/L) x 体积 (L) 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、MSDS / 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、MSDS / 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03694262 Not yet recruiting Endometrial Cancer Medical College of Wisconsin April 1 2019 Phase 2
NCT03694262 Not yet recruiting Endometrial Cancer Medical College of Wisconsin April 1 2019 Phase 2
NCT03840200 Not yet recruiting Breast Cancer|Prostate Cancer|Ovarian Cancer Hoffmann-La Roche March 22 2019 Phase 1|Phase 2
NCT03795272 Not yet recruiting Cervical Cancer Nordic Society for Gynaecologic Oncology|Institute of Cancer Research United Kingdom|Central and Eastern European Oncology Group|North Eastern Germany Society of Gynaecologic Oncology|Belgian Gynaecological Oncology Group|Princess Margaret Hospital Canada|PGOG (Polish Gynaecologic Oncology Group)|GSO Global Clinical Research BV|GCP-enhederne March 1 2019 Phase 2
NCT03639935 Recruiting Biliary Tract Cancer University of Michigan Rogel Cancer Center|Dana-Farber Cancer Institute|Vanderbilt University Medical Center March 2019 Phase 2
NCT03617679 Recruiting Metastatic Endometrial Cancer University of Colorado Denver|Clovis Oncology Inc.|National Cancer Institute (NCI) March 6 2019 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID