PHT-427 (CS-0223)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 500mg | $750 | Check With Us |
| 1g | $1150 | Check With Us |
| 5g | $1725 | Check With Us |
: Cat #: V0165 CAS #: 1191951-57-1 Purity ≥ 98%
Description: PHT-427 (CS0223) is a novel, potent, orally bioactive and dual inhibitor of Akt and PDPK1 (PtdIns dependent protein kinase-1) with potential anticancer activity.
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| Molecular Weight (MW) | 409.61 |
|---|---|
| Molecular Formula | C20H31N3O2S2 |
| CAS No. | 1191951-57-1 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 82 mg/mL (200.2 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 60 mg/mL (146.5 mM) | |
| Solubility In Vivo | 5% DMSO+95% Corn oil: 5mg/mL |
| SMILES Code | O=S(C1=CC=C(CCCCCCCCCCCC)C=C1)(NC2=NN=CS2)=O |
| Synonyms | PHT427; PHT-427; PHT 427 |
| Protocol | In Vitro | The effects of PHT-427 on cell signaling are investigated by RPPA using a panel of 86 antibodies to phospho- and non-phosphorylated signaling protein related to PtdIns-3-K/PDPK1/Akt signaling in PC-3 prostate cells where PtdIns-3-K/PDPK1/Akt signaling is activated because of homozygous PTEN mutation. After 16 hours, a reduction is observed in phospho-Ser241-PDPK1 phospho-Thr308-Akt by both 10 µM PH-427 and 0.1 µM Wortmannin. Finally, phospho-Ser657-protein kinase C (PKC) and total SGK1 are decreased by treatment with both PHT-427 and Wortmannin. These results suggest that at 10 µM PHT-427 inhibits both Akt and PDKP1. The BxPC-3 and MiaPaCa-2 pancreatic cancer cell lines are probed by Western blotting following up to 24 hr exposure to 10 µM PHT-427, which is below the IC50 for cell growth inhibition of around 30 µM, to determine the effects of PHT-427 on of the PtdIns-3-K/PDPK1/Akt signaling pathway components. |
|---|---|---|
| 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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.4413 mL | 12.2067 mL | 24.4135 mL | 48.8269 mL |
| 5mM | 0.4883 mL | 2.4413 mL | 4.8827 mL | 9.7654 mL |
| 10mM | 0.2441 mL | 1.2207 mL | 2.4413 mL | 4.8827 mL |
| 20mM | 0.1221 mL | 0.6103 mL | 1.2207 mL | 2.4413 mL |
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