[CAS NO. 925069-34-7]  PI-273

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PRODUCTS SPECIFICATIONS [925069-34-7]

Catalog
HY-103489
Brand
MCE
CAS
925069-34-7

DESCRIPTION [925069-34-7]

Overview

MDL-
Molecular Weight381.90
Molecular FormulaC16H16ClN3O2S2
SMILESO=C(C1=C(NC(NC(C2=CC=C(Cl)C=C2)=O)=S)SC(C)=C1CC)N

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE


Summary

PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC 50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis [1] .


IC50 & Target

PI4KIIα

0.47 μM (IC 50 )


In Vitro

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.

In Vivo

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%.

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 6.02 mg/mL ( 15.76 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
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
* Please refer to the solubility information to select the appropriate solvent.