1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. Anticancer agent 108

Anticancer agent 108 (Compound 3.10) is a potent P-gp inhibitor with significant antitumor activity and less toxicity to normal and pseudonormal cells. Anticancer agent 108 (Compound 3.10) had no acute toxic effect on С57BL/6 mice.

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Anticancer agent 108 Chemical Structure

Anticancer agent 108 Chemical Structure

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Description

Anticancer agent 108 (Compound 3.10) is a potent P-gp inhibitor with significant antitumor activity and less toxicity to normal and pseudonormal cells. Anticancer agent 108 (Compound 3.10) had no acute toxic effect on С57BL/6 mice[1].

In Vitro

Anticancer agent 108 (10 μM; 48 h) significantly inhibits the proliferation of cancer cells[1].
Anticancer agent 108 (50, 100, 250, 500 nM; 72 h) inhibits the proliferation of KB-3-1 cells[1].
Anticancer agent 108 (0.5, 2.5, 5 μM; 3, 24 h) uses endoplasmic reticulum (ER) stress to induce apoptosis[1].
Anticancer agent 108 (5, 10 μM; 24 h) induces apoptosis of MDA-MB-231 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: 60 cancer cell lines representing nine different types (leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cancers)
Concentration: 10 μM
Incubation Time: 48 h
Result: Possessed prominent antitumor activity (mean growth −61.06%; the range of growth −99.55 to 18.52). In addition, inhibited the growth of 25 tested cancer cell lines with percent growth of <0, and showed not only cytostatic effect but also cytotoxic properties.

Cell Proliferation Assay[1]

Cell Line: KB-3-1 cells
Concentration: 50, 100, 250, 500 nM
Incubation Time: 72 h
Result: Almost 14 times bigger comparing to survival fraction after incubation of KB-3-1 cells with doxorubicin in the same concentration (100 nM) used as a positive control. However, at applying 500 nM concentration, did not observe the growth of KB-3-1 cell colonies after 72 h of drug exposure.

Western Blot Analysis[1]

Cell Line: KB-3-1 cells
Concentration: 0.5, 2.5, 5 μM
Incubation Time: 3, 24 h
Result: Dose-dependently increased the expression of BIP (immunoglobulin heavy chain binding protein) at 24 hours, while no changes in the levels of the above proteins were found at 3 hours.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 5, 10 μM
Incubation Time: 24 h
Result: Induced apoptosis in the MDA-MB-231 breast cancer cells proceeding through two pathways, extrinsic and intrinsic.
In Vivo

Anticancer agent 108 (single dose, i.p. 20 mg/kg) does not induce a loss of body mass in animals, their rapid death, leukopenia, erythropenia, and a decrease in the level of hemoglobin in blood of mice.

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

Animal Model: С57BL/6 mice[1]
Dosage: 20 mg/kg
Administration: single dose, i.p. 20 mg/kg
Result: Did not induce a loss of body mass in animals, their rapid death, leukopenia, erythropenia, and a decrease in the level of hemoglobin in blood of mice.
Molecular Weight

383.40

Formula

C18H9NO5S2

SMILES

O=C1NC2=C(C(C3=C(C(C4=C(C(O)=CC=C4)C3=O)=O)S2)C5=CC=CO5)S1

Shipping

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 108
Cat. No.:
HY-149240
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