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PF-3084014, γ-分泌酶抑制剂

规格或纯度: ≥98%
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货号 (SKU) 包装规格 是否现货 价格 数量
P127448-5mg
 5mg 现货 Stock Image
P127448-10mg
 10mg 现货 Stock Image
P127448-25mg
 25mg 现货 Stock Image
P127448-50mg
 50mg 现货 Stock Image
P127448-100mg
 100mg 现货 Stock Image
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基本描述

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

Description:
IC50 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

名称和标识符

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
分子量 489.64

化学和物理性质

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

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参考文献

1. Wei P, Walls M, Qiu M, Ding R, Denlinger RH, Wong A, Tsaparikos K, Jani JP, Hosea N, Sands M et al..  (2010)  Evaluation of selective gamma-secretase inhibitor PF-03084014 for its antitumor efficacy and gastrointestinal safety to guide optimal clinical trial design..  Mol Cancer Ther,  9  (6):  (1618-28).  [PMID:20530712]
2. Brodney MA, Auperin DD, Becker SL, Bronk BS, Brown TM, Coffman KJ, Finley JE, Hicks CD, Karmilowicz MJ, Lanz TA et al..  (2011)  Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: discovery of PF-3084014..  Bioorg Med Chem Lett,  21  (9):  (2637-40).  [PMID:21269827]
3. López-Guerra M, Xargay-Torrent S, Rosich L, Montraveta A, Roldán J, Matas-Céspedes A, Villamor N, Aymerich M, López-Otín C, Pérez-Galán P et al..  (2015)  The γ-secretase inhibitor PF-03084014 combined with fludarabine antagonizes migration, invasion and angiogenesis in NOTCH1-mutated CLL cells..  Leukemia,  29  (1):  (96-106).  [PMID:24781018]
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