产品名称

英文名称：PF-3084014

同义词

Nirogacestat、1290543-63-3、PF-03084014、PF-3084014、865773-15-5、PF 3084014、Nirogacestat [USAN]、PF 03084014、(S)-2-(((S)-6,8-Difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)amino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide、PF3084014

产品性质

CAS编号：1290543-63-3

分子式：C27H41F2N5O

分子量：489.64

PubChem编号：46224413

英文别名：Nirogacestat|1290543-63-3|PF-03084014|PF-3084014|865773-15-5|PF 3084014|Nirogacestat [USAN]|PF 03084014|(S)-2-(((S)-6,8-Difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)amino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide|PF3084014|

规格或纯度：≥98%

英文名称：PF-3084014

生化机理：DescriptionIC50 Value 1.2 nM (whole-cell assay);6.2 nM (cell-free assay) [1]PF-03084014 is a novel gamma-secretase inhibitor that reduces amyloid-beta (Abeta) production with an in vitro IC(50) of 1.2 nM (whole-cell assay) to 6.2 nM (cell-free assay).in vitro PF-03084014 inhibits Notch-related T- and B-cell maturation in an in vitro thymocyte assay with an EC(50) of 2.1 microM. A single acute dose showed dose-dependent reduction in brain, cerebrospinal fluid (CSF), and plasma Abeta in Tg2576 mice as measured by enzyme-linked immunosorbent assay and immunoprecipitation (IP)/mass spectrometry (MS) [1]. The ability of PF-03084014 to inhibit gamma-secretase activity was shown by the reduction of endogenous NICD levels and by the downregulation of Notch target genes Hes-1 and cMyc in the T-cell acute lymphoblastic leukemia (T-ALL) cell line HPB-ALL. PF-03084014 caused cell growth inhibition of several T-ALL cell lines via cell cycle arrest and induction

储存温度：-20°C储存

运输条件：超低温冰袋运输

IUPAC Name：(2S)-2-[[(2S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]amino]-N-[1-[1-(2,2-dimethylpropylamino)-2-methylpropan-2-yl]imidazol-4-yl]pentanamide

INCHI：InChI=1S/C27H41F2N5O/c1-7-8-23(32-20-10-9-18-11-19(28)12-22(29)21(18)13-20)25(35)33-24-14-34(17-31-24)27(5,6)16-30-15-26(2,3)4/h11-12,14,17,20,23,30,32H,7-10,13,15-16H2,1-6H3,(H,33,35)/t20-,23-/m0/s1

InChi Key：VFCRKLWBYMDAED-REWPJTCUSA-N

Canonical SMILES：CCCC(C(=O)NC1=CN(C=N1)C(C)(C)CNCC(C)(C)C)NC2CCC3=C(C2)C(=CC(=C3)F)F

Isomeric SMILES：CCC[C@@H](C(=O)NC1=CN(C=N1)C(C)(C)CNCC(C)(C)C)N[C@H]2CCC3=C(C2)C(=CC(=C3)F)F

关联CAS：1962925-29-6

PubChem CID：46224413

ChEMBL Ligand：CHEMBL1770916

CAS Registry No.：1290543-63-3

溶解性：DMSO ≥ 50 mg/mL (102.12 mM);H2O < 0.1 mg/mL (insoluble)

产品包装