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  4. Dimesna

Dimesna (BNP-7787), the disulfide form of Mesna (HY-13679), is a platinum-related toxicity protective agent. Dimesna converts to Mesna, which in turn inactivates toxic platinum substances. Dimesna does not interfere with the antitumor activity of platinum compounds. Dimesna does not affect the antiproliferative effects of Cisplatin (HY-17394) or Carboplatin (HY-17393). Dimesna counteracts Cisplatin-induced nephrotoxicity. Dimesna exerts selective protective effects on the kidneys. Dimesna can be used in studies related to ovarian cancer and Cisplatin-induced nephrotoxicity.

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Dimesna

Dimesna Chemical Structure

CAS No. : 16208-51-8

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Based on 1 publication(s) in Google Scholar

Other Forms of Dimesna:

Dimesna Related Antibodies

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1 Publications Citing Use of MCE Dimesna

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Description

Dimesna (BNP-7787), the disulfide form of Mesna (HY-13679), is a platinum-related toxicity protective agent. Dimesna converts to Mesna, which in turn inactivates toxic platinum substances. Dimesna does not interfere with the antitumor activity of platinum compounds. Dimesna does not affect the antiproliferative effects of Cisplatin (HY-17394) or Carboplatin (HY-17393). Dimesna counteracts Cisplatin-induced nephrotoxicity. Dimesna exerts selective protective effects on the kidneys. Dimesna can be used in studies related to ovarian cancer and Cisplatin-induced nephrotoxicity[2][3].

In Vitro

Dimesna (0-5.0 mmol/L; 1-24 h) alone exerts no effect on total protein, thymidine incorporation or uridine incorporation in LLC-PK1 cells, and fails to protect LLC-PK1 cells from toxicity induced by ifosfamide, cyclophosphamide, 4-hydroperoxyifosfamide, chloroacetaldehyde or acrolein[1].
Dimesna (≥2.0×103 μM; 96 h) does not reduce the antiproliferative effects of cisplatin or carboplatin on A2780 or OVCAR-3 ovarian cancer cells, and only inhibits the growth of these cells when exposed for 96 h at a concentration of ≥2.0×103 μM[2].

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

Dimesna Related Antibodies

Cell Viability Assay[1]

Cell Line: LLC-PK1 renal tubular cells
Concentration: 0-5.0 mmol/l (alone; co-incubated with ifosfamide/cyclophosphamide/4-OOH-ifosfamide/chloracetaldehyde/acrolein); 1.0-5.0 mmol/l (co-incubated with 4-OOH-cyclophosphamide)
Incubation Time: 1-24 h (alone); 1 h pre-incubation + 23 h co-incubation (with cytostatic metabolites)
Result: Had no significant effect on total protein, thymidine incorporation, or uridine incorporation at all tested concentrations and times when used alone.
Moderately stimulated thymidine incorporation, but had no significant effect on total protein or uridine incorporation when co-incubated with 150 μmol/l ifosfamide.
Had no significant effect on total protein, thymidine incorporation, or uridine incorporation when co-incubated with 150 μmol/l cyclophosphamide.
Further reduced total protein and thymidine incorporation at 1.0, 3.0, 5.0 mmol/l, and further reduced uridine incorporation at 3.0, 5.0 mmol/l (P < 0.05) when co-incubated with 75 μmol/l 4-OOH-cyclophosphamide.
Failed to protect cells from toxicity induced by 150 μmol/l 4-OOH-ifosfamide, with total protein, thymidine incorporation, and uridine incorporation remaining strongly reduced.
Failed to protect cells from toxicity induced by 75 μmol/l chloracetaldehyde, with no statistically significant difference in total protein, thymidine incorporation, or uridine incorporation compared to chloracetaldehyde alone.
Failed to protect cells from toxicity induced by 100 μmol/l acrolein, with total protein, thymidine incorporation, and uridine incorporation remaining severely reduced.
In Vivo

Dimesna (BNP-7787) (1000 mg/kg; i.v.) does not interfere with the antitumour activity of cisplatin or carboplatin in OVCAR-3 ovarian cancer xenografts, and co-administration with 60 mg/kg carboplatin results in significantly greater tumour growth inhibition than carboplatin alone (specific growth delay of 4.72 vs. 4.01 for carboplatin alone)[2].
Dimesna (BNP-7787) (1000 mg/kg; i.v.; bolus injection) administered to tumour-bearing Fischer rats results in preferential accumulation of its metabolite mesna in the kidney, with kidney mesna AUC0-t 4.5-fold higher than plasma mesna AUC0-t, while maintaining low mesna levels in plasma and tumour tissue relative to mesna administration[3].

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

Animal Model: Hsd: athymic nude-nu (female, 8-10 weeks old)[2]
Dosage: 1000 mg/kg (pre-cisplatin 5 mg/kg); 1000 mg/kg (pre-cisplatin 8 mg/kg); 1000 mg/kg (with carboplatin 60 mg/kg); 1000 mg/kg (with carboplatin 90 mg/kg); 1000 mg/kg (monotherapy)
Administration: i.v.; weekly ×2 (pre-cisplatin 5 mg/kg); i.v.; every 2 weeks ×2 (pre-cisplatin 8 mg/kg); i.v.; twice per treatment cycle, weekly ×2 (with carboplatin 60 mg/kg); i.v.; twice per treatment cycle, weekly ×2 (with carboplatin 90 mg/kg); i.v.; weekly ×2 (monotherapy)
Result: Exhibited mean maximum weight loss of 6.6±6.1%, no toxic deaths, specific growth delay of 3.48, and mean relative tumour volume of 2.55±0.42 on day 31 when given 5 minutes before 5 mg/kg cisplatin, with no significant difference in tumour growth inhibition compared to cisplatin alone.
Exhibited mean maximum weight loss of 24.8±9.2%, no toxic deaths, specific growth delay of 6.34, and mean relative tumour volume of 0.39±0.08 on day 31 when given 5 minutes before 8 mg/kg cisplatin, with no significant difference in tumour growth inhibition compared to amifostine-pretreated cisplatin.
Exhibited mean maximum weight loss of 9.9±11.9%, no toxic deaths, specific growth delay of 4.72, and mean relative tumour volume of 0.50±0.14 on day 31 when given with 60 mg/kg carboplatin, which was significantly smaller than carboplatin alone (P<0.01).
Exhibited mean maximum weight loss of 11.4±3.1%, 2 out of 6 mice died from toxicity, specific growth delay of 8.44, and mean relative tumour volume of 0.17±0.03 on day 31 when given with 90 mg/kg carboplatin.
Exhibited mean maximum weight loss of 0.0±3.2%, no toxic deaths, specific growth delay of 0.22, and mean relative tumour volume of 29.28±4.38 on day 31 as monotherapy, with no tumour growth inhibition observed.
Clinical Trial
Molecular Weight

326.34

Formula

C4H8Na2O6S4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(CCSSCCS(=O)(O[Na])=O)(O[Na])=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (306.43 mM; Need ultrasonic)

DMSO : 68 mg/mL (208.37 mM; Need ultrasonic and warming; 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 3.0643 mL 15.3214 mL 30.6429 mL
5 mM 0.6129 mL 3.0643 mL 6.1286 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
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 (sealed storage, away from moisture). 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 / H2O 1 mM 3.0643 mL 15.3214 mL 30.6429 mL 76.6072 mL
5 mM 0.6129 mL 3.0643 mL 6.1286 mL 15.3214 mL
10 mM 0.3064 mL 1.5321 mL 3.0643 mL 7.6607 mL
15 mM 0.2043 mL 1.0214 mL 2.0429 mL 5.1071 mL
20 mM 0.1532 mL 0.7661 mL 1.5321 mL 3.8304 mL
25 mM 0.1226 mL 0.6129 mL 1.2257 mL 3.0643 mL
30 mM 0.1021 mL 0.5107 mL 1.0214 mL 2.5536 mL
40 mM 0.0766 mL 0.3830 mL 0.7661 mL 1.9152 mL
50 mM 0.0613 mL 0.3064 mL 0.6129 mL 1.5321 mL
60 mM 0.0511 mL 0.2554 mL 0.5107 mL 1.2768 mL
80 mM 0.0383 mL 0.1915 mL 0.3830 mL 0.9576 mL
100 mM 0.0306 mL 0.1532 mL 0.3064 mL 0.7661 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Dimesna Related Classifications

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.

Keywords:

Dimesna16208-51-8BNP-7787BNP7787BNP 7787Drug DerivativeDrug derivativehuman ovarian cancer cell lineskidney epithelial cellsFischer ratsreactive oxygen speciesnude miceOVCAR-3 xenograftsred blood cellsWARD colon tumoursLLC-PK1 cellsA2780 cellsInhibitorinhibitorinhibit

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