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

China 85 India 1 United States 7 Global 93

Shanghai Taibao Pharmaceutical Technology Co., Ltd.

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Suzhou MgPlus Pharmtech Co., Ltd.

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Shanghai Boyle Chemical Co., Ltd.

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Haoyuan Chemexpress Co., Ltd.

Tel: 021-58950125
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Email: info@chemexpress.com
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Shanghai Aladdin Bio-Chem Technology Co.,LTD

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ShangHai Caerulum Pharma Discovery Co., Ltd.

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DKMbiochem.Co. Ltd

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Email: sales@DKMbiochem.com
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LETOPHARM LIMITED

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Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
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Shanghai Synchem Pharma Co., ltd

Tel: 21-619849051-1 18521059765
Email: synchempharma@aliyun.com
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1290543-63-3, PF-3084014Related Search:

PF-06700841 tosylate PF-06650833 PF-05089771 (tosylate) PF-06424439 PF-06447475 PF 3644022 PF 04995274 PF 573228 PF-06882961 PF-5190457 PF-05212384 [(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate PF-04691502 1H-Indole-2-carboxamide, 4-methoxy-N-[(1S)-3-methyl-1-[[[(1S)-2-oxo-1-[[(3S)-2-oxo-3-pyrrolidinyl]methyl]-3-(phosphonooxy)propyl]amino]carbonyl]butyl]- PF 477736

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

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