1. Cell Cycle/DNA Damage Apoptosis
  2. Topoisomerase Apoptosis
  3. Pyrazoloacridine

Pyrazoloacridine  (Synonyms: NSC 366140; PD 115934)

Cat. No.: HY-108969 Purity: 98.05%
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Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment.

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Pyrazoloacridine Chemical Structure

Pyrazoloacridine Chemical Structure

CAS No. : 99009-20-8

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Description

Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment[1][2].

In Vitro

Pyrazoloacridine (NSC 366140, PD 115934) exhibits IC50 values of 10.7 μM and 4.5 μM for oxic and hypoxic HCT-8 cells[1].
Pyrazoloacridine (NSC 366140, 2-4 μM) abolishes the catalytic activity of both topo I and topo II in vitro[2].
Pyrazoloacridine (NSC 366140) displays activity against cisplatin- and paclitaxel-resistant ovarian cancer[2].
Pyrazoloacridine (NSC 366140) has been shown to cause delayed DNA fragmentation in MCF-7 breast cancer cells[2].
Pyrazoloacridine (NSC 366140) induces apoptosis in P53-deficient Hep 3B human hepatoma cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[2]

Cell Line: K562 Myeloid Leukemia Cells.
Concentration: 0-500 μM.
Incubation Time: 1 h or 24 h.
Result: When K562 cells were incubated with PA for 1 h and then plated in soft agar, an IC50 of -50 μM was observed. In contrast, when cells were incubated for 24 h with PA, the IC50 was 1.25 μM.
Clinical Trial
Molecular Weight

367.40

Formula

C19H21N5O3

CAS No.
Appearance

Solid

Color

Light brown to orange

SMILES

O=[N+](C1=CC=C2C3=C1NC4=CC=C(OC)C=C4C3=NN2CCCN(C)C)[O-]

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 : 16.67 mg/mL (45.37 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7218 mL 13.6091 mL 27.2183 mL
5 mM 0.5444 mL 2.7218 mL 5.4437 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.05%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7218 mL 13.6091 mL 27.2183 mL 68.0457 mL
5 mM 0.5444 mL 2.7218 mL 5.4437 mL 13.6091 mL
10 mM 0.2722 mL 1.3609 mL 2.7218 mL 6.8046 mL
15 mM 0.1815 mL 0.9073 mL 1.8146 mL 4.5364 mL
20 mM 0.1361 mL 0.6805 mL 1.3609 mL 3.4023 mL
25 mM 0.1089 mL 0.5444 mL 1.0887 mL 2.7218 mL
30 mM 0.0907 mL 0.4536 mL 0.9073 mL 2.2682 mL
40 mM 0.0680 mL 0.3402 mL 0.6805 mL 1.7011 mL
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Pyrazoloacridine Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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