MDL | - |
---|---|
Molecular Weight | 381.90 |
Molecular Formula | C16H16ClN3O2S2 |
SMILES | O=C(C1=C(NC(NC(C2=CC=C(Cl)C=C2)=O)=S)SC(C)=C1CC)N |
PI4KIIα 0.47 μM (IC 50 ) |
PI-273 (2 μM; 48 hours) blocks the cell cycle at the G2-M phase
[1]
.
PI-273 (2 μM; 48 hours) induces cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3
[1]
.
PI-273 (0.5-2 μM; for 3 days) can suppress the AKT signaling pathway in a dose- and time-dependent manner
[1]
.
PI-273 of 1 μM and 2 μM inhibits the cell proliferation of both MCF-7 and T-47D cells in a time-dependent manner
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cycle Analysis [1]
Cell Line: | MCF-7, T-47D, SK-BR-3, MDA-MB-231, SUM229PE, Hs 578T cells |
Concentration: | 2 μM |
Incubation Time: | 48 hours |
Result: | Blocked the cell cycle at the G2-M phase. |
Apoptosis Analysis [1]
Cell Line: | MCF-7, T-47D, and SK-BR-3 cells |
Concentration: | 2 μM |
Incubation Time: | 48 hours |
Result: | Induced cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3. |
Western Blot Analysis [1]
Cell Line: | MCF-7 cells |
Concentration: | 0.5, 1, 2 μM |
Incubation Time: | For 3 days |
Result: | Suppressed the AKT signaling pathway in a dose- and time-dependent manner. |
PI-273 (intraperitoneal injection; 25 mg/kg/day; 15 days) profoundly suppresses the tumor volume and weight in the MCF-7 xenografts
[1]
.
PI-273 (0.5 mg/kg (intravenously) or 1.5 mg/kg (intragastrically); 0.08-5 hours) has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | Eight-week-old male BALB/c nude mice with MCF-7 cell [1] |
Dosage: | 25 mg/kg |
Administration: | Intraperitoneal injection; daily; 15 days |
Result: | Suppressed the tumor volume and weight in the MCF-7 xenografts. |
Animal Model: | Male Sprague-Dawley (SD) rats [1] |
Dosage: | 0.5 mg/kg (intravenously) or 1.5 mg/kg (intragastrically) (Pharmacokinetic Study) |
Administration: | Intravenously or intragastrically; 0.08, 0.16, 0.33, 0.67, 1, 1.5, 2, 3 and 5 hours |
Result: | Has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%. |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 6.02 mg/mL ( 15.76 mM ; ultrasonic and warming and heat to 60°C)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.6185 mL | 13.0924 mL | 26.1849 mL |
5 mM | 0.5237 mL | 2.6185 mL | 5.2370 mL |
10 mM | 0.2618 mL | 1.3092 mL | 2.6185 mL |