PX-316
PX-316 is an Akt inhibitor. PX-316 can phosphorylate Akt, but does not inhibit the phosphorylation of PDK1 or PKC. PX-316 uniquely increases the expression of a group of mitochondrial-related genes. PX-316 can be used for the study of colon cancer and breast cancer.
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- CAS. Nr.: 253440-95-8
- Formel: C28H57O10P
- Molecular Weight:584.72
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
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Akt |
PX-316 (0-15 μM, 2 h) specifically inhibits Akt (IC50 = 1.7 μM) activation in HT-29 human colon cancer cells without affecting upstream kinase PDK1 or related kinase PKC[1].
PX-316 (0.5-20 μM, 3 days) inhibits the proliferation of MCF-7 and HT-29 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29 human colon cancer cells
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Concentration:0 μM, 5 μM, 10 μM, 15 μM
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Incubation Time:2 h
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Result:Inhibited EGF-induced Akt phosphorylation (phosphorylation of Ser473 site) in a concentration-dependent manner with an IC50 value of 1.7 μM, but did not inhibit PDK1 phosphorylation (Ser241 site) or PKC phosphorylation (Thr638/641 site).
PX-316 (50-150 mg/kg, i.p., once for 4-10 days) demonstrates dose- and regimen-dependent antitumor activity in two different mice xenograft models of human tumors (MCF-7 and HT-29)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HT-29 colon cancer cells(107)were injected subcutaneously into the flanks of male severe combined immunodeficient (scid) mice[1].
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Dosage:37.5 mg/kg, 75 mg/kg, 150 mg/kg
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Administration:I.p., once
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Result:A single administration of 150 mg/kg inhibited Akt (Ser473) phosphorylation in tumors by up to 78% at 10 hours, recovering to 34% inhibition after 48 hours.
The half-maximal inhibitory dose (ID50) for Akt phosphorylation in tumors was 80 mg/kg, while the ID50 for normal tissue (spleen) was 128 mg/kg.
At a concentration of 150 mg/kg, phosphorylation of GSK-3β (Ser9), a downstream target of Akt, was also inhibited, with inhibition rates of 53% and 77% at 5 hours and 24 hours, respectively.
At a dose of 75 mg/kg, whether administered once daily for 5 consecutive days or once every 3 days for 5 consecutive days, Akt activity was consistently inhibited (inhibition rate of 70%-80%).
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Animal Model:MCF-7 human breast cancer cells (107 cells) were mixed with Matrigel and subcutaneously injected into the flank of female SCID mice. One day before tumor cell inoculation, mice were subcutaneously implanted with 60-day sustained-release 17-β-estradiol pellets to support the growth of this estrogen-dependent tumor[1].
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Dosage:50 mg/kg, 75 mg/kg, 100 mg/kg
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Administration:I.p., once daily for 10 days, 10 days and 5 days, respectively
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Result:75 mg/kg showed a good inhibitory effect (T/C = 20%), while 100 mg/kg showed a slightly weaker effect (T/C = 39%).
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Animal Model:HT-29 human colon cancer cells (107 cells) were subcutaneously injected into the flank of SCID mice[1].
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Dosage:100 mg/kg, 150 mg/kg
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Administration:I.p., once daily for 4 days
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Result:Caused growth inhibition of 5-day HT-29 colon cancer xenografts when administered for 4 days IP at 150 mg/kg/day (T/C33.3%, P<0.05) but no activity at 100 mg/kg/day.
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Chemical Information
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CAS. Nr. 253440-95-8
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Molecular Weight 584.72
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Formel C28H57O10P
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SMILES
CCCCCCCCCCCCCCCCCCOC[C@@H](OC)COP(O[C@H]1[C@@H]([C@H]([C@@H](C[C@H]1O)O)O)O)(O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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