Dacarbazine

Catalog No.S1221 Synonyms: DTIC-Dome

Dacarbazine Chemical Structure

Molecular Weight(MW): 182.18

Dacarbazine is a triazene derivative with antineoplastic activity. Dacarbazine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis; used in the treatment of various cancers.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 60 In stock
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Biological Activity

Description Dacarbazine is a triazene derivative with antineoplastic activity. Dacarbazine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis; used in the treatment of various cancers.
Targets
Nucleoside antimetabolite/analog [1]
In vitro

Treatment of Dacarbazine sensitizes melanomas to lysis of peptide-specific CTL and it is is mediated through Fas-independent pathway[2].

Assay
Methods Test Index PMID
Western blot
ATM / p-ATM / p21(Waf1/Cip1) / Survivin ; 

PubMed: 27632933     


Combined ABT-888 (0-10 µM) and dacarbazine (0-600 µM) treatment induced phosphorylated-ATM and p21(Waf1/Cip1), while either agent alone generated minimal expression. These findings indicate activation of the ATM-mediated DNA repair pathway secondary to drug-induced DNA damage. While dacarbazine alone produced no observed effect on expression of the Inhibitor of Apoptosis gene Survivin, the addition of 10µM ABT-888 led to near complete depletion of its expression.

27632933
Growth inhibition assay
Cell viability; 

PubMed: 21976975     


Cytotoxicity of DTIC, DR5 mAb, DTIC-NPs, DTIC-NPs + DR5 mAb, and DTIC-NPs-DR5 mAb in A375 cells and NIH cells. The cells were incubated using different concentrations of DTIC, DR5 mAb, DTIC-NPs, NPs-DR5 mAb, DTIC-NPs + DR5 mAb and DTIC-NPs-DR5 mAb (contain the same DTIC) for a time period of 72 hours (mean ± standard deviation; n = 5). *P < 0.05; **P < 0.01; ***P < 0.001. DTIC, dacarbazine; mAb, monoclonal antibody; NPs, nanoparticles.

21976975
In vivo Treatment of combination of Axitinib and DTIC demonstrates significant antitumor activity against melanoma flank xenografts, reduces tumor cell proliferation and decreases the area of tumor necrosis and increases apoptosis. It also reduces meta-tasis-related factors and prolongs lifespan in mice[3].

Protocol

Cell Research:

[2]

+ Expand
  • Cell lines: UACC903 (UACC) cells
  • Concentrations: 20 μM
  • Incubation Time: 48 h
  • Method:

    Apotosis assay: UACC903 (UACC) cells treated with or without DTIC (20 μM) for 48 h are incubated with agonist anti-Fas Ab, CH-11 (500 ng/ml), for 5 and 16 h, respectively. To distinguish whether death/apoptosis is mediated by FasR, blocking anti-Fas Ab ZB4 (2 mg/ml) is added in the corresponding groups. At the end of incubation, cells are harvested and stained with propidium iodide and FITC-annexin V (BD PharMingen) for detecting apoptosis according to the instruction provided by the company. Ten thousand cells from each group are collected, and dead and apoptotic cells are analyzed without gating using CellQuest software.


    (Only for Reference)
Animal Research:

[3]

+ Expand
  • Animal Models: B16F1 melanoma xenograft model(C57BL/6 mice background)
  • Formulation: 0.9% sodium chloride
  • Dosages: 80 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 12 mg/mL warmed (65.86 mM)
Water 2 mg/mL warmed (10.97 mM)
Ethanol 1 mg/mL warmed (5.48 mM)
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC Na
For best results, use promptly after mixing.
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 182.18
Formula

C6H10N6O

CAS No. 4342-03-4
Storage powder
in solvent
Synonyms DTIC-Dome

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03761095 Recruiting Drug: PTC596|Drug: Dacarbazine Leiomyosarcoma PTC Therapeutics March 13 2019 Phase 1
NCT01974752 Completed Drug: 75mg selumetinib|Drug: placebo|Drug: Dacarbazine Metastatic|Uveal Melanoma AstraZeneca April 2014 Phase 3
NCT01133977 Completed Drug: Lenvatinib|Drug: Dacarbazine Stage IV Melanoma Eisai Inc.|Quintiles Inc. April 2010 Phase 1|Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    Could you please help me test some common vehicles for S1221 in vivo experiments?

  • Answer:

    S1221 can dissolve in 0.5% CMC Na at 30mg/ml as a suspension. After stayed for a period of time, the powder will drop down to the bottom of the tube, so please vortex well before use.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID