PHT-427
PHT-427
CAS: 1191951-57-1
Molecular Formula: C20H31N3O2S2
PHT-427 - Names and Identifiers
PHT-427 - Physico-chemical Properties
| Molecular Formula | C20H31N3O2S2 |
| Molar Mass | 409.61 |
| Density | 1.162 |
| Melting Point | 126-127 °C(Solv: hexane (110-54-3); ethyl acetate (141-78-6)) |
| Boling Point | 535.0±43.0 °C(Predicted) |
| Solubility | Soluble in DMSO (82 mg/ml), water (< 1 mg/ml), and ethanol (60 mg/ml). |
| Appearance | White solid |
| Color | White to Off-White |
| pKa | 6.03±0.40(Predicted) |
| Storage Condition | +2C to +8C |
| MDL | MFCD18384970 |
| Use | A pleckstrin homology domain inhibitor to Akt and PKB Kinase (PDPK1). |
| In vitro study | PH-427 is a platelet leukocyte C kinase substrate homology (PH) domain inhibitor of Akt/pdpk1. 10 M PH-427 acts on PC-3 prostate cancer cells, significantly reduced by p-Ser241-PDPK1 and p-Thr308-Akt, indicating that PHT-427 can inhibit Akt and pdkp1. PHT-427 acts on the plasma membrane and also inhibits Akt and PDKP1 PH domain translocation. PHT-427 induces apoptosis and inhibits AKT phosphorylation (mainly at Ser473 residue and less at Thr308 residue, IC50 is 6.3 μm, which does not affect all AKT protein expression. PHT-427 acts on Panc-1 cells and has an antiproliferative effect with an IC50 of 65 μm. |
| In vivo study | PHT-427 acts on BxPC-3 pancreatic cancer, MCF-7 breast cancer and A- 549 NSCL cancer xenografts, with significant anti-tumor activity. PHT-427 at a dose of 125 to 250 mg/kg on BxPC-3, tumor growth was inhibited by 80%. |
PHT-427 - Introduction
PHT-427 is an AKT inhibitor that inhibits AKT and PDPK1 at low micromolar concentrations in numerous cancer cell lines and exhibits good oral anti-tumor activity in mouse xenograft models. PHT-427 reduces the phosphorylation of AKT and PDPK1. Following the administration of a single oral dose of PHT-427 to mice bearing BxPC-3 human pancreatic tumor xenografts, PHT-427 inhibited the phosphorylation of both Akt and PDPK1 as well as downstream targets maximally at 8-12 h after administration corresponding to its peak plasma concentration, with PDPK1 inhibition extending to 24 hr.
Last Update：2022-10-16 17:41:18
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Product Name: PHT-427 Visit Supplier Webpage Request for quotationCAS: 1191951-57-1
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Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
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Product Name: PHT-427 Visit Supplier Webpage Request for quotationCAS: 1191951-57-1
Tel: 609-228-6898
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tech@medchemexpress.com
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Product Name: PHT-427 Visit Supplier Webpage Request for quotationCAS: 1191951-57-1
Tel: +86 0571-86722205
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Product Name: PHT-427 Visit Supplier Webpage Request for quotationCAS: 1191951-57-1
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