性能参数

产品名称

Niraparib R-enantiomer (MK 4827 (R-enantiomer))

规格

10mM*1mLinDMSO2mg 5mg 10mg 50mg

货号

GOY-Y3822

 含量

>98.00%

CAS

1038915-58-0

别名

N/A

化学名

N/A

分子式

C19H20N4O

分子量

分子量 320.39

溶解度

DMSO : ≥ 32 mg/mL (99.88 mM)

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM.

Niraparib R-enantiomer (MK-4827 R-enantiomer) resolution of Niraparib R-enantiomer give compounds Niraparib R-enantiomer and Niraparib S-enantiomer, both showing excellent inhibition of PARP-1. Niraparib R-enantiomer has somewhat lower in vitro metabolic clearance than the Niraparib S-enantiomer in rat liver microsomes, but Niraparib S-enantiomer is more potent in cell based assays (PARylation EC50, Niraparib R-enantiomer=30 nM, Niraparib S-enantiomer=4.0 nM; BRCA1-HeLa CC50, Niraparib R-enantiomer=470, Niraparib S-enantiomer=34 nM). Given this improved potency and similar in vitro turnover in human liver microsomes (HLM Clint, Niraparib R-enantiomer=4, Niraparib S-enantiomer=3 μL/min/mgP), Niraparib S-enantiomer (Niraparib) is focused on[1].

[1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.

氨甲基膦酸  1066-51-9  吲哚-7-甲醛  1074-88-0

5-氨基-4-氯-2-氟苯甲酸盐酸盐  957120-34-2  3,5-二溴苄腈  97165-77-0

2-氨基-4-硝基苯甲醚  99-59-2  离子交换树酯  9002-26-0

3-氨基-5-(4-氯苯基)噻吩-2-羧酸甲酯  91076-93-6  双(4-氯苄基)偶氮二甲酸酯  916320-82-6

乙?；芬严?/span>  932-66-1  苯甲醛肟  932-90-1

对甲基苯甲酸乙酯  34552  4-氯间二甲苯,

3,5-二溴-4-羟基苯...3,5-Dibromo-4-hydroxybenzaldehyde,98%2973-77-55G

香芹酮L-Carvone,99%6485-40-125G

乙基香兰素Ethyl vanillin,≥98%121-32-425G

2-己烯醛trans-2-Hexen-1-al,98%6728-26-325ML

2,6-二甲基-5-庚烯醛2,6-Dimethyl-5-heptenal,97%106-72-925ML

反,反-2,4-壬二烯醛trans,trans-2,4-Nonadienal,≥89%5910-87-25ML