PHT-427
- Product Name
- PHT-427
- CAS No.
- 1191951-57-1
- Chemical Name
- PHT-427
- Synonyms
- CS-303;CS-0223;PHT-427;PHT-427, >=98%;PHT-427 ，S1556;PHT-427;PHT 427;PHT-427 USP/EP/BP;PHT-427 (CS-0223);Akt Inhibitor XIV;PHT-427, 10 mM in DMSO
- CBNumber
- CB62561491
- Molecular Formula
- C20H31N3O2S2
- Formula Weight
- 409.61
- MOL File
- 1191951-57-1.mol
PHT-427 Property
- Melting point:
- 126-127 °C(Solv: hexane (110-54-3); ethyl acetate (141-78-6))
- Boiling point:
- 535.0±43.0 °C(Predicted)
- Density
- 1.162
- storage temp.
- +2C to +8C
- solubility
- Chloroform, Methanol (Slightly)
- form
- White solid
- pka
- 6.03±0.40(Predicted)
- color
- White to Off-White
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H320Causes eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 124032
- Product name
- Akt Inhibitor XIV - CAS 1191951-57-1 - Calbiochem
- Packaging
- 10mg
- Price
- $154
- Updated
- 2023/06/20
- Product number
- 24188
- Product name
- PHT-427
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $38
- Updated
- 2024/03/01
- Product number
- 24188
- Product name
- PHT-427
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $71
- Updated
- 2024/03/01
- Product number
- 24188
- Product name
- PHT-427
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $166
- Updated
- 2024/03/01
- Product number
- 24188
- Product name
- PHT-427
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $311
- Updated
- 2024/03/01
PHT-427 Chemical Properties,Usage,Production
Uses
PHT-427 is a dual Akt and PDPK1 inhibitor with Ki of 2.7 μM and 5.2 μM, respectively.
Uses
PHT-427 is a pleckstrin homology domain inhibitor to Akt and PKB Kinase (PDPK1). It can also be used for therapeutic use and biological study of mathematical modeling and parametric analysis of nanoparticle encapsulation and controlled release of a hydrophobic kinase inhibitor PHT-427.
Biological Activity
pht-427 is an inhibitor of akt and pdpk1 (ki =2.7 μm and 5.2 μm, respectively).akt is a serine/threonine-specific protein kinase that plays a vital role in multiple cellular processes including glucose metabolism, apoptosis, cell proliferation, transcription and cell migration etc.in bxpc-3 cells, pht-427 showed inhibition upon akt function with ic50 value of 8.6±0.8 μm and for its downstream substrates. pht-427 reduced the akt phosphorylation on ser473 residue and did not decrease total akt protein level. pht-427 also inhibited p70s6k and gsk3β in a dose-dependent manner. [1][2]in scid (severe combined immunodeficiency) mice of bxpc-3 pancreatic cancer xenografts, administration of pht-427 exerted prominent antitumor activity that halted tumor growth. pht-427 in combination with erlotinib exhibited greater than additive antitumor activity in nsc lung cancer and with paclitaxel in breast cancer. [1][2]
in vivo
Mice with BxPC-3 pancreatic, MCF-7 breast or A-549 NSCL cancer xenografts are administered PHT-427, or its analogs with a C-4, C-6 or C-8 alkyl chain by oral gavage twice a day for 10 days. The results show that PHT-427 has the greatest antitumor activity with the C-8 chain analog having less activity, and analogs with a C-4 or C-6 chain very little activity. All further antitumor studies are conducted using compound PHT-427. Plasma levels of PHT-427 following oral administration to mice of a dose of 200 mg/kg show rapid absorption, without a lag phase, Cmax is 8.2 μg/mL 1 hr following dosing, and the elimination half-life is 1.4 hr with a terminal PHT-427 concentration of 0.1 μg/mL 10 hr after dosing. The plasma concentration of PH-427 is above the level which gave inhibition of Akt and PDPK1 signaling in cells of 10 μM (4 μg/mL) for at least 3 hr[1].
Enzyme inhibitor
This orally bioavailable, dual Akt/PDPK1 inhibitor (F.Wt. = 409.61; CAS 1191951-57-1 and 1178893-77-0; Solubility (25°C): 80 mg/mL DMSO, <1 mg/mL Water), known systematically as 4-dodecyl-N-(1,3,4-thiadiazol-2- yl)benzenesulfonamide, targets Akt (also known as Protein Kinase B, or PKB) and 3-phosphoinositide-dependent protein kinase-1, with Ki of 2.7 μM and 5.2 μM, respectively. PHT-427 was designed to bind to the pleckstrin homology (PH) auto-inhibitory domains of the signal cascade protein kinase Akt.
IC 50
PDPK1: 5.2 μM (Ki)
storage
-20°C
References
1. meuillet ej, zuohe s, lemos r et al. molecular pharmacology and antitumor activity of pht-427, a novel akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor. mol cancer ther. 2010 mar;9(3):706-17.2. moses sa, ali ma, zuohe s et al. in vitro and in vivo activity of novel small-molecule inhibitors targeting the pleckstrin homology domain of protein kinase b/akt. cancer res. 2009 jun 15;69(12):5073-81.
PHT-427 Preparation Products And Raw materials
Raw materials
Preparation Products
PHT-427 Suppliers
- Tel
- Fax
- 86-21-57758967
- sales@boylechem.com
- Country
- China
- ProdList
- 2922
- Advantage
- 55
- Tel
- +86-21-20908456
- Fax
- 021-58180499
- sales@BioChemBest.com
- Country
- China
- ProdList
- 6003
- Advantage
- 61
- Tel
- 0531-88811783
- Fax
- +86 (531) 55696010 QQ 1762738062
- sales@trio-pharmatech.com
- Country
- China
- ProdList
- 1856
- Advantage
- 62
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Country
- China
- ProdList
- 4747
- Advantage
- 58
- Tel
- 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
- Fax
- +86-27-87599188
- Country
- China
- ProdList
- 1493
- Advantage
- 55
- Tel
- +86 21 61551611
- Fax
- +86 21 50676805
- Country
- China
- ProdList
- 9891
- Advantage
- 58
- Tel
- 021-58950125
- Fax
- (86) 21-58955996
- info@chemexpress.com
- Country
- China
- ProdList
- 7552
- Advantage
- 61
- Tel
- 400-6206333 13167063860
- Fax
- 021-50323701
- anhua.mao@aladdin-e.com
- Country
- China
- ProdList
- 25003
- Advantage
- 65
- Tel
- +86-18068513926
- Fax
- 0086-519-85153711
- Country
- China
- ProdList
- 1277
- Advantage
- 55
- Tel
- 020-39119399 18927568969
- Fax
- 020-39119999
- isunpharm@qq.com
- Country
- China
- ProdList
- 4720
- Advantage
- 55
- Tel
- 0086-571-86217390
- Fax
- 0086-571-86217391
- Sales@gihichem.com
- Country
- China
- ProdList
- 860
- Advantage
- 58
- Tel
- 0512-87182056 18013166090
- Fax
- 0512-87182056
- lingling.qi@yacoo.com.cn
- Country
- China
- ProdList
- 6295
- Advantage
- 60
- Tel
- 021-61478794
- Fax
- 021-61478794
- sales@hcshhai.com
- Country
- China
- ProdList
- 9793
- Advantage
- 50
- Tel
- 025-58849295 18951903616;
- Fax
- 025-68650336
- info@adooq.cn
- Country
- China
- ProdList
- 2990
- Advantage
- 60
- Tel
- +86 (21) 61124340
- Fax
- +86 (21) 6129-4103
- Country
- China
- ProdList
- 9756
- Advantage
- 58
- Tel
- 027-59599241 18871490274
- Fax
- 027-59599241
- 1400878000@qq.com
- Country
- China
- ProdList
- 9858
- 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
- 4769
- Advantage
- 55
- Tel
- 0512-63009836 18994340901
- Fax
- 0512-63006936
- helen@struchem.com
- Country
- China
- ProdList
- 3981
- Advantage
- 60
- Tel
- 18607101326 15172504745
- Fax
- +86-27-84254680
- aileen@chemfaces.com
- Country
- China
- ProdList
- 6905
- Advantage
- 55
- Tel
- Fax
- -
- eric_feng1954@126.com
- Country
- China
- ProdList
- 9248
- Advantage
- 55
- Tel
- 0371-53765687 18937137882
- Fax
- QQ:2885373884
- 2853979813@qq.com
- Country
- China
- ProdList
- 7991
- Advantage
- 55
- Tel
- 18620099427
- Fax
- +86-20-62619665
- amy@howeipharm.com
- Country
- China
- ProdList
- 6687
- Advantage
- 55
- Tel
- +86-400-851-9921
- Fax
- +86-10-82826195
- sales@pharmacodia.com
- Country
- China
- ProdList
- 2317
- Advantage
- 55
- Tel
- 020-61288194 61288195
- Fax
- 020-61288700
- 505721671@qq.com
- Country
- China
- ProdList
- 3866
- Advantage
- 58
- Tel
- 021-61312847; 18021002903
- Fax
- QQ:3008007432
- 3008007409@qq.com
- Country
- China
- ProdList
- 71826
- Advantage
- 60
- Tel
- 0519-85528066 13775048983
- Fax
- 0519-85528066
- sales@hopschem.com
- Country
- China
- ProdList
- 31553
- Advantage
- 55
- Tel
- 86-21-50817262
- Fax
- 86-21-57712035
- sales@lancrix.com
- Country
- China
- ProdList
- 1502
- Advantage
- 55
- Tel
- sales@njromanme.com
- Country
- China
- ProdList
- 4529
- Advantage
- 58
- Tel
- 400-1166-196 15982826727
- Fax
- QQ：800101999
- cdhxsj@163.com
- Country
- China
- ProdList
- 14603
- Advantage
- 60
- Tel
- 021-31433387 15618786686
- Fax
- QQ:1369748377
- sales@rechemscience.com
- Country
- China
- ProdList
- 2991
- Advantage
- 58
- Tel
- 021-QQ：65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 9125
- Advantage
- 58
- Tel
- 010-50973130 18101056239
- 3193328036@qq.com
- Country
- China
- ProdList
- 29760
- Advantage
- 68
- Tel
- 571-89925085
- Fax
- 0086-571-89925065
- sales@amadischem.com
- Country
- China
- ProdList
- 131957
- Advantage
- 58
- Tel
- 0519-83246372 13585352506
- Fax
- 0519-83246372
- Country
- China
- ProdList
- 1844
- Advantage
- 58
- Tel
- 0550-5196001 15000891977
- Fax
- 0550-5196001
- wj520wjxby@126.com
- Country
- China
- ProdList
- 1944
- Advantage
- 55
- Tel
- 86-(0)29-85992781 17792393971
- info@lynnchem.com
- Country
- China
- ProdList
- 4587
- Advantage
- 58
- Tel
- 13127280945
- 285424065@qq.com
- Country
- China
- ProdList
- 9976
- Advantage
- 55
- Tel
- 0512-56316828
- Fax
- 0512-56316826
- info@amateksci.com
- Country
- China
- ProdList
- 28785
- Advantage
- 58
- Tel
- 021-37581181
- Fax
- 021-57456066
- sales@chem-mall.com
- Country
- China
- ProdList
- 10330
- Advantage
- 58
- Tel
- 021-16621358918; 18516310516
- Fax
- 13045646768
- zhenlipharma888@163.com
- Country
- China
- ProdList
- 19035
- Advantage
- 58
- Tel
- 027-87466105 15377573527
- 2678564200@qq.com
- Country
- China
- ProdList
- 17987
- Advantage
- 58
- Tel
- 021-61350663 15502154572
- Fax
- -
- 1639466865@qq.com
- Country
- China
- ProdList
- 497
- Advantage
- 58
- Tel
- 15589964716
- Fax
- qq：3360232875
- 15253102672@163.com
- Country
- China
- ProdList
- 211
- Advantage
- 58
- Tel
- 17317130613
- Fax
- QQ3358272972
- 3358272972@qq.com
- Country
- China
- ProdList
- 3277
- Advantage
- 58
- Tel
- 4009004166/18616739031 18616739031
- 3007523370@qq.com
- Country
- China
- ProdList
- 52687
- Advantage
- 58
- Tel
- 025-025-51191215 18013836722
- Fax
- 025-51191215
- 2399235533@qq.com
- Country
- China
- ProdList
- 4933
- Advantage
- 58
- Tel
- 15911056312
- liming@bio-fount.com
- Country
- China
- ProdList
- 9729
- Advantage
- 58
- Tel
- 020-31155029 18902330969
- Fax
- 020-31155029
- sales@tomums.cn
- Country
- China
- ProdList
- 4696
- Advantage
- 58
- Tel
- +1-2135480471
- sales@sarms4muscle.com
- Country
- China
- ProdList
- 10473
- Advantage
- 58
View Lastest Price from PHT-427 manufacturers
- Product
- PHT-427 1191951-57-1
- Price
- US $60.00-600.00/kg
- Min. Order
- 10kg
- Purity
- 0.99
- Supply Ability
- 20tons
- Release date
- 2023-11-10
- Product
- PHT-427 1191951-57-1
- Price
- US $1000.00-950.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2018-08-04