- PHT-427
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- $79.00 / 25mg
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2025-09-22
- CAS:1191951-57-1
- Min. Order:
- Purity: 98.00%
- Supply Ability: 10g
- PHT-427
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- $60.00 / 1kg
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2025-06-03
- CAS:1191951-57-1
- Min. Order: 10kg
- Purity: 0.99
- Supply Ability: 20tons
- PHT-427
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- $1000.00 / 1KG
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2019-07-06
- CAS:1191951-57-1
- Min. Order: 1KG
- Purity: 99%
- Supply Ability: 100kg
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| | PHT-427 Basic information |
| Product Name: | PHT-427 | | Synonyms: | PHT-427;4-Dodecyl-N-1,3,4-thiadiazol-2-ylbenzenesulfonamide;CS-0223;4-Dodecyl-N-1,3,4-thiadiazol-2-ylbenzenesulfonamide PHT 427;PHT-427
4-Dodecyl-N-1,3,4-thiadiazol-2-ylbenzenesulfonamide;PHT-427;PHT 427;PHT-427, >=98%;PHT-427 (CS-0223) | | CAS: | 1191951-57-1 | | MF: | C20H31N3O2S2 | | MW: | 409.61 | | EINECS: | | | Product Categories: | PI3K/Akt/mTOR;Akt;mTOR;PI3K;Inhibitors | | Mol File: | 1191951-57-1.mol |  |
| | PHT-427 Chemical Properties |
| 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 |
| | PHT-427 Usage And Synthesis |
| 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. | | Uses | PHT-427 is a dual Akt and PDPK1 inhibitor with Ki of 2.7 μM and 5.2 μM, respectively. | | 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 |
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