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
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
Safety
- HS Code
- 29332900
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.
N-Bromosuccinimide Price
- Product number
- PZ0298
- Product name
- PF-03084014 hydrobromide
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $115
- Updated
- 2023/06/20
- Product number
- PZ0298
- Product name
- PF-03084014 hydrobromide
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $451
- Updated
- 2023/06/20
- Product number
- 27061
- Product name
- PF-3084014
- Packaging
- 5mg
- Price
- $109
- Updated
- 2024/03/01
- Product number
- 27061
- Product name
- PF-3084014
- Packaging
- 25mg
- Price
- $420
- Updated
- 2024/03/01
- Product number
- 27061
- Product name
- PF-3084014
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
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
PF-3084014 Suppliers
- Tel
- 13816752554
- 1745533547@qq.com
- Country
- China
- ProdList
- 129
- Advantage
- 58
- Tel
- 0512-66727658 18115508618
- phoenix888.ok@163.com
- Country
- China
- ProdList
- 968
- Advantage
- 58
- Tel
- Fax
- 86-21-57758967
- sales@boylechem.com
- Country
- China
- ProdList
- 2922
- Advantage
- 55
- Tel
- 021-58950125
- Fax
- (86) 21-58955996
- info@chemexpress.com
- Country
- China
- ProdList
- 7552
- Advantage
- 61
- Tel
- 400-400-6206333 18521732826
- Fax
- 021-50323701
- market@aladdin-e.com
- Country
- China
- ProdList
- 25003
- Advantage
- 65
- Tel
- 18149758185 18149758185
- sales-cpd@caerulumpharma.com
- Country
- China
- ProdList
- 3466
- Advantage
- 58
- Tel
- 15901859516
- Fax
- 15901859516
- sales@DKMbiochem.com
- Country
- China
- ProdList
- 344
- Advantage
- 58
- Tel
- +86-21-5821 5861
- Fax
- +86-21-5106 2861
- sales@letopharm.com
- Country
- China
- ProdList
- 2384
- Advantage
- 58
- Tel
- 021-52996696，15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4512
- Advantage
- 55
- Tel
- 21-619849051-1 18521059765
- synchempharma@aliyun.com
- Country
- China
- ProdList
- 6463
- Advantage
- 55
- Tel
- Fax
- -
- eric_feng1954@126.com
- Country
- China
- ProdList
- 9248
- Advantage
- 55
- Tel
- 18620099427
- Fax
- +86-20-62619665
- amy@howeipharm.com
- Country
- China
- ProdList
- 17687
- Advantage
- 55
- Tel
- 020-61288194 61288195
- Fax
- 020-61288700
- 505721671@qq.com
- Country
- China
- ProdList
- 3866
- Advantage
- 58
- Tel
- 0317-5296180 15533709196
- Fax
- 0317-5106596
- sale@enkepharma.com
- Country
- China
- ProdList
- 1898
- Advantage
- 55
- Tel
- 400-1166-196 18502815961
- Fax
- QQ：800101999
- cdhxsj@163.com
- Country
- China
- ProdList
- 14603
- Advantage
- 60
- Tel
- 028-83379370 13880556291
- Fax
- 028-87747383
- tcy@tcypharm.com
- Country
- China
- ProdList
- 6268
- Advantage
- 58
- Tel
- Fax
- -
- 13006575422@163.com
- Country
- China
- ProdList
- 6355
- Advantage
- 58
- Tel
- 010-50973130 4009686088
- 3193328036@qq.com
- Country
- China
- ProdList
- 29785
- Advantage
- 68
- Tel
- 571-89925085
- Fax
- 0086-571-89925065
- sales@amadischem.com
- Country
- China
- ProdList
- 131957
- Advantage
- 58
- Tel
- 010-88886666-01 13112345678
- Fax
- CDXH21@126.com
- loyson@tcypharm.com
- Country
- China
- ProdList
- 595
- Advantage
- 55
- Tel
- 0755-0755-85201366 18938635012
- Fax
- 0755-85201366
- sales@regentsciences.com
- Country
- China
- ProdList
- 9355
- Advantage
- 58
- Tel
- 13917627064
- Fax
- -qq：56229367
- 56229367@qq.com
- Country
- China
- ProdList
- 577
- Advantage
- 58
- Tel
- 4009004166/18616739031 18616739031
- 3007523370@qq.com
- Country
- China
- ProdList
- 52693
- Advantage
- 58
- Tel
- 020-31155029 18902330969
- Fax
- 020-31155029
- sales@tomums.cn
- Country
- China
- ProdList
- 4696
- Advantage
- 58
- Tel
- 0571-85361029
- Fax
- 0571-85361029
- synstar518@163.com
- Country
- China
- ProdList
- 1990
- Advantage
- 58
- Tel
- 86-571-88216897,88216896 13588875226
- Fax
- 86-571-88216895
- sales@hzclap.com
- Country
- CHINA
- ProdList
- 6312
- Advantage
- 58
- Tel
- 021-58447131 13564518121
- sales@dcchemicals.com
- Country
- China
- ProdList
- 9409
- Advantage
- 58
- Tel
- 0519-85788828 13775037613
- sales@chemrenpharm.com
- Country
- China
- ProdList
- 3600
- Advantage
- 58
- Tel
- 021-54156369 16621315851
- yhsuyiming@126.com
- Country
- China
- ProdList
- 310
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- sales@chemegen.com
- Country
- China
- ProdList
- 11217
- Advantage
- 58
- Tel
- 020-82000279 18988968278
- Fax
- QQ：3283937693
- sales@ubiochem.com
- Country
- China
- ProdList
- 4297
- Advantage
- 58
- Tel
- 021-38015121 15000105423
- wulan@absin.cn
- Country
- China
- ProdList
- 24731
- Advantage
- 58
- Tel
- 88888888888
- hongquchem@qq.com
- Country
- China
- ProdList
- 5132
- Advantage
- 58
- Tel
- 021-51111890 15317326293
- sales@molnova.com
- Country
- China
- ProdList
- 4195
- Advantage
- 58
- Tel
- 15869524721
- 3525679403@qq.com
- Country
- China
- ProdList
- 3991
- Advantage
- 58
- Tel
- 15342225168
- yutianchun2007@126.com
- Country
- China
- ProdList
- 10002
- Advantage
- 58
- Tel
- 021-58432009 400-005-6266
- Fax
- 021-58436166
- marketing1@energy-chemical.com
- Country
- China
- ProdList
- 44808
- Advantage
- 58
- Tel
- 1701086315
- Fax
- 1701086315@qq.com
- dexuanpharma@126.com
- Country
- China
- ProdList
- 9475
- Advantage
- 58
- Tel
- +86-02787215551 +86-19945035818
- Fax
- 027-87215551
- 2936752263@qq.com
- Country
- China
- ProdList
- 7973
- Advantage
- 58
- Tel
- 13348960310 13348960310
- 3003867561@qq.com
- Country
- China
- ProdList
- 10002
- Advantage
- 58
- Tel
- 021-50967598 02150967598
- sales@abmole.cn
- Country
- China
- ProdList
- 4494
- Advantage
- 58
- Tel
- 18051384581
- sales@chemhifuture.com
- Country
- China
- ProdList
- 3056
- Advantage
- 58
- Tel
- 14793566
- info@cenpharm.com
- Country
- China
- ProdList
- 696
- Advantage
- 58
- Tel
- 15995756885
- Fax
- QQ:273525849
- 15995756885@139.com
- Country
- China
- ProdList
- 45
- Advantage
- 58
- Tel
- 027-59101668 19945030958
- Fax
- 027-59101668
- 2881924765@qq.com
- Country
- China
- ProdList
- 8140
- Advantage
- 58
- Tel
- 400-1647117 13681763483
- product02@bidepharm.com
- Country
- China
- ProdList
- 62163
- Advantage
- 58
- Tel
- 13549236410
- sales@invivochem.cn
- Country
- China
- ProdList
- 6753
- Advantage
- 58
- Tel
- +86-027-59232304 15387063101
- 2881924050@qq.com
- Country
- China
- ProdList
- 9951
- Advantage
- 58
- Tel
- 4008200310
- marketing@tsbiochem.com
- Country
- China
- ProdList
- 24647
- Advantage
- 58
- Tel
- 0371-53370800 18037197114
- 2853031799@qq.com
- Country
- China
- ProdList
- 10007
- Advantage
- 58