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  4. Anticancer agent 303

Anticancer agent 303 is a selective, orally active anticancer agent belonging to the pyrazolopyridine derivatives. Anticancer agent 303 exhibits low cytotoxicity to healthy cells, with a selective window of approximately 2-fold between cancer cells and healthy cells. Anticancer agent 303 produces detectable systemic exposure in mice following intraperitoneal or oral administration. Anticancer agent 303 effectively inhibits the proliferation of prostate cancer and breast cancer cells.

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Anticancer agent 303

Anticancer agent 303 Chemical Structure

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Description

Anticancer agent 303 is a selective, orally active anticancer agent belonging to the pyrazolopyridine derivatives. Anticancer agent 303 exhibits low cytotoxicity to healthy cells, with a selective window of approximately 2-fold between cancer cells and healthy cells. Anticancer agent 303 produces detectable systemic exposure in mice following intraperitoneal or oral administration. Anticancer agent 303 effectively inhibits the proliferation of prostate cancer and breast cancer cells[1].

In Vitro

Anticancer agent 303 (compound 17) (5 μM; 72 h) inhibits the viability of PC-3, MCF-7 and HUVEC cells, with mean IC50 values of 4.8 μM, 3.9 μM and 8.7 μM, respectively[1].
Anticancer agent 303 (5 μM; 1-24 h) accumulates in PC-3 cells in a time-dependent manner, reaching a level of 245.8 ng/40,000 cells (104.5% of the initial administered dose) after 24 h of treatment at 5 μM[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: human prostate adenocarcinoma PC-3 cells
Concentration: 5 μM
Incubation Time: 72 h
Result: Reduced PC-3 cell viability to 36% relative to DMSO control.
Exhibited an average IC50 of 4.8 ± 0.9 μM.

Cell Cytotoxicity Assay[1]

Cell Line: human breast adenocarcinoma MCF-7 cells
Concentration: 5 μM
Incubation Time: 72 h
Result: Reduced MCF-7 cell viability to 33% relative to DMSO control.
Exhibited an average IC50 of 3.9 ± 0.9 μM.
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC0-t AUC0-∞ Bioavailability
Mice[1] 4 mg/kg i.p. 372.2 ng/mL 4.8 h 14.4 h 5847.1 ng·h/mL 8721.3 ng·h/mL /
Mice[1] 8 mg/kg p.o. 199.0 ng/mL 6.5 h 16.3 h 3338.0 ng·h/mL 5299.1 ng·h/mL 29.13 %
In Vivo

Anticancer agent 303 (compound 17) achieves systemic exposure in mice via intraperitoneal (i.p.) and oral (p.o.) administration. Intraperitoneal injection yields higher systemic exposure than oral administration, as indicated by increased Cmax and AUC, and has a shorter time to peak concentration (Tmax), while the elimination half-lives of the two administration routes are similar. In addition, the dose-normalized relative oral bioavailability of Anticancer agent 303 is 29.13%[1].

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

Molecular Weight

470.57

Formula

C27H30N6O2

SMILES

O=C(NC1=CC=CC=C1)NC2=CC(OCCNC3CCCCC3)=C4C(N(C5=CC=CC=C5)N=C4)=N2

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • 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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Product Name:
Anticancer agent 303
Cat. No.:
HY-181558
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