CAS 1290543-63-3; pf-03084014 hydrobromide

CAS:

1290543-63-3

分子式:

C₂₇H₄₁F₂N₅O

分子量:

489.64

英文名称:

pf-03084014 hydrobromide

(2S)-2-[[(2S)-6,8-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]amino]-n-[1-[2-[(2,2-dimethylpropyl)amino]-1,1-dimethylethyl]-1h-imidazol-4-yl]-pentanamide hydrobromide

pf 3084014 hydrobromide

nirogacestat

pf 03084014 hydrobromide

pf-3084014 hydrobromide

用途:

Nirogacestat (PF-03084014, PF-3084014) 是一种选择性gamma-secretase抑制剂，在无细胞试验中IC50为6.2 nM。Phase 2。PF-03084014 inhibits Notch receptor cleavage in cellular assays using HPB-ALL cells that harbor mutations in both the heterodimerization and PEST domains in Notch1with IC50 of 13.3 nM. PF-03084014 downregulates Notch target genes Hes-1, and cMyc expression in HPB-ALL cells with IC50 of <1 nM and 10 nM, respectively. PF-03084014 inhibits cell growth of a subset of human T-ALL cell lines (HPB-ALL, DND-41, TALL-1,and Sup-T1) through induction of cell cycle arrest and apoptosis with IC50s of 30-100 nM. [1]PF-03084014 reduces proliferation of HUVECs with IC50 of 0.5 μM, and decreases the lumen formation with an IC50 value of 50 nM. PF-03084014 (1 μM) has no antiproliferative effect in MX1 cells; however, it inhibits migration by 95%. [2]

推荐供应商

货号

品牌

产品名称

规格

包装、参考价格

N792411

MACKLIN

Nirogacestat (PF-03084014, PF-3084014)

10mM in DMSO

648元/1ml;

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储存：-20°C

N873140

MACKLIN

Nirogacestat (PF-03084014, PF-3084014)

≥99%

546元/5mg; 962元/10mg; 2001元/25mg; 3261元/50mg; 5865元/100mg;

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储存：-20℃
状态：白色到黄色固体

PZ0298

Sigma-Aldrich

PF-03084014 hydrobromide

≥98% (HPLC)

1396.09元/5 MG; 4498.97元/25 MG;

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产品说明

包装

5, 25 mg in glass bottle

生化/生理作用

PF-03084014 inhibits the Notch signalling pathway. It contributes totumor suppression in breast, pancreatic carcinoma, hepatocellular carcinoma and progressive desmoid tumors. PF-03084014 in combination with dexamethasone elicits antileukemic effects in T-cell acute lymphoblastic leukemias (T-ALL).
PF-03084014 is a highly potent γ-secretase inhibitor that reduces Aβ production in vitro. PF-03084014 does not show a paradoxical increase in plasma Aβ at low concentrations in both preclinical species and humans.

其他说明

This compound was developed by Pfizer for Neuroscience research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.

To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

法律信息

Sold for research purposes under agreement from Pfizer Inc.
Pfizer is a registered trademark of Pfizer, Inc.

基本信息

经验(实验)分子式	C₂₇H₄₁F₂N₅O · HBr
分子量	570.56
PubChem化学物质编号	329823821
NACRES	NA.77

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
manufacturer/tradename	Pfizer^®
颜色	white to beige
溶解性	H₂O: 1 mg/mL, clear
创始人	Pfizer
储存温度	room temp
SMILES string	FC1=C2C(CC[C@H](N[C@@H](CCC)C(NC3=CN(C(C)(C)CNCC(C)(C)C)C=N3)=O)C2)=CC(F)=C1.C
InChI	1S/C27H41F2N5O.CH4/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);1H4/t20-,23-;/m0./s1
InChI key	GLEYBLZDOTUZJH-WCRWPNQISA-N

安全信息

象形图
警示用语：	Warning
危险声明	H315 - H319 - H335
预防措施声明	P280 - P304 + P340 + P312 - P305 + P351 + P338 - P337 + P313
危险分类	Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官	Respiratory system
储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable