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PF-3084014

Product Name
PF-3084014
CAS No.
1290543-63-3
Chemical Name
PF-3084014
Synonyms
Nirogacestat;CS-2699;PF-3084014;PF-03084014 (PF-3084014);Nirogacestat (PF-03084014;PF-03084014 (Nirogacestat);PF03084014;PF 03084014;PF-03084014;Nirogacestat(PF-03084014,PF-3084014);Nirogacestat,γ-secretase,Gamma secretase,cancer,inhibit,PF 3084014,gastrointestinal,toxicity,Inhibitor,Notch,PF3084014,Apoptosis;(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
CBNumber
CB42628246
Molecular Formula
C27H41F2N5O
Formula Weight
489.64
MOL File
1290543-63-3.mol
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PF-3084014 Property

Boiling point:
651.3±55.0 °C(Predicted)
Density 
1.16±0.1 g/cm3(Predicted)
storage temp. 
room temp
solubility 
Water:1.0(Max Conc. mg/mL);2.04(Max Conc. mM)
form 
powder
pka
13.27±0.70(Predicted)
color 
white to beige
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Safety

HS Code 
29332900
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PZ0298
Product name
PF-03084014 hydrobromide
Purity
≥98% (HPLC)
Packaging
5MG
Price
$115
Updated
2023/06/20
Sigma-Aldrich
Product number
PZ0298
Product name
PF-03084014 hydrobromide
Purity
≥98% (HPLC)
Packaging
25MG
Price
$451
Updated
2023/06/20
Cayman Chemical
Product number
27061
Product name
PF-3084014
Packaging
5mg
Price
$109
Updated
2024/03/01
Cayman Chemical
Product number
27061
Product name
PF-3084014
Packaging
25mg
Price
$420
Updated
2024/03/01
Cayman Chemical
Product number
27061
Product name
PF-3084014
Packaging
1mg
Price
$32
Updated
2024/03/01
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PF-3084014 Chemical Properties,Usage,Production

Biochem/physiol Actions

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).

Enzyme inhibitor

This novelγ-secretase inhibitor (FW = 489.66 g/mol; CAS 1290543-63-3; soluble in DMSO), also code-named HY-15185 and systematically named [(S)-2-((S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-3-ylamino)-N-(1-(2- methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide], inhibitsγ-secretase reversibly, noncompetitively, and selectively, thereby reducing amyloid-b (Ab) production, with an in vitro IC50 of 1.2 nM in a whole-cell assay and 6.2 nM in cell-free assay. PF-03084014 inhibits Notch-related T- and B-cell maturation in an in vitro thymocyte assay with an EC50 of 2.1 μM. PF-3084014 had an IC50 on B- and T-cell reductions of 1.3 to 3 μM with a mean EC50 of 2.1 μM. This represents >300-fold separation from the broken-cell Aβ IC50 and >1500x separation from the whole-cell IC50. A single acute dose showed dose-dependent reduction in brain, cerebrospinal fluid (CSF), and plasma Ab . When dosed with PF- 3084014 for 5 days using an osmotic minipump (0.03 to 3 mg/kg/day), Guinea pigs exhibited dose-dependent Ab reduction in brain, CSF, and plasma. While otherγ-secretase inhibitors show high potency at elevating Ab in the conditioned media of whole cells and the plasma of multiple animal models and humans, such potentiation is not observed with PF- 3084014. By evoking antitumor and antimetastatic properties via pleiotropic mechanisms, experiments with PF-03084014 offer hope that Notch pathway downstream genes may be used to predict the antitumor activity of PF-03084014 in breast cancer patients.

PF-3084014 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF-3084014 Suppliers

BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
ProdList
9923
Advantage
65
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
Advantage
58
Aladdin Scientific
Tel
+1-+1(833)-552-7181
Email
sales@aladdinsci.com
Country
United States
ProdList
57505
Advantage
58
TargetMol Chemicals Inc.
Tel
Email
support@targetmol.com
Country
United States
ProdList
38632
Advantage
58
Cayman Chemical Company
Tel
--
Fax
--
Email
cayman@caymanchem.com
Country
United States
ProdList
6213
Advantage
81

1290543-63-3, PF-3084014Related Search:


  • PF-3084014
  • (S)-2-((S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-ylamino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide Molecular Weight: 489.64
  • PF-03084014 (PF-3084014)
  • (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
  • Nirogacestat
  • PF03084014;PF 03084014;PF-03084014
  • CS-2699
  • PF-03084014 (Nirogacestat)
  • Nirogacestat(PF-03084014,PF-3084014)
  • Pentanamide, 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]-, (2S)-
  • Nirogacestat (PF-03084014
  • Nirogacestat,γ-secretase,Gamma secretase,cancer,inhibit,PF 3084014,gastrointestinal,toxicity,Inhibitor,Notch,PF3084014,Apoptosis
  • 1290543-63-3
  • api