产品名称

英文名称：MK-4827 (Niraparib)

同义词

2-(4-(3S)-3-piperidinylphenyl)-2H-indazole-7-carboxamide 、 1038915-60-4 、 STL556264 、 LABETALOL [WHO-DD] 、 DTXCID8068620 、 BCP9000940 、 DB11793 、 MK 4827 、 s2741 、 AKOS016004869 、 BCP0726000077 、 MK-4827/MK4827 、 NIRAPARIB [INN] 、 C19H20N4O 、 MK-4827(Nira

产品性质

CAS编号：1038915-60-4

分子式：C19H20N4O

分子量：320.39

PubChem编号：24958200

英文别名：2-(4-(3S)-3-piperidinylphenyl)-2H-indazole-7-carboxamide | 1038915-60-4 | STL556264 | LABETALOL [WHO-DD] | DTXCID8068620 | BCP9000940 | DB11793 | MK 4827 | s2741 | AKOS016004869 | BCP0726000077 | MK-4827/MK4827 | NIRAPARIB [INN] | C19H20N4O | MK-4827(Nira

规格或纯度：98%

英文名称：MK-4827 (Niraparib)

生化机理：MK-4827 is a potent, selective, PARP 1/2 inhibitor with IC50 of 3.8 and 2.1 nM for PARP1 and 2, respectively. MK-4827 possesses potential antineoplastic activity. In a whole cell assay, MK-4827 prevented PARP activity with an EC50 of 4 nM, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. MK-4827 induces selective synthetic lethality in homologous recombination (HR) repair deficient tumors with BRCA1/2 loss and tumor cell lines with non-BRCA-related HR defects, supporting clinical utility in sporadic tumors. MK-4827 reveals good pharmacokinetic properties and is currently in phase I clin. trials. The phase I clinical trials for MK-4827 is ongoing in the treatment of solid tumors.

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：50mg卖完停产，不再备货

产品介绍：MK-4827(Niraparib)是高活性PARP1/PARP2抑制剂，IC50分别为3.8 nM/2.1 nM，在BRCA-1和BRCA-2突变型肿瘤细胞中具有很好的活性，比对PARP3，V-PARP和Tank1的抑制性高330倍以上。MK-4827(Niraparib) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM;with great activity in cancer cells with mutant BRCA-1 and BRCA-2;>330-fold selective against PARP3,V-PARP and Tank1.

ALogP：2.2

PubChem SID：488200727

PubChem SID url：https//pubchem.ncbi.nlm.nih.gov/substance/488200727

IUPAC Name：2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide

INCHI：InChI=1S/C19H20N4O/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24)/t14-/m1/s1

InChi Key：PCHKPVIQAHNQLW-CQSZACIVSA-N

Canonical SMILES：C1CC(CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N

Isomeric SMILES：C1C[C@H](CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N

PubChem CID：24958200

ChEMBL Ligand：CHEMBL1094636

CAS Registry No.：1038915-60-4

RCSB PDB Ligand：3JD

DrugCentral Ligand：5222

溶解性：DMSO

象形图：

信号词：Danger

危险声明：H373 Causes damage to organs through prolonged or repeated exposureH302 Harmful if swallowedH340 May cause genetic defectsH361 Suspected of damaging fertility or the unborn child

预防措施声明：P280,P405,P501,P264,P260,P281,P270,P330,P203,P301+P317,P318,P319

产品包装