Dacarbazine

製品コードS1221 バッチS122104

印刷

化学情報

 Chemical Structure Synonyms DTIC-Dome, Imidazole Carboxamide,NSC-45388 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C6H10N6O

分子量 182.18 CAS No. 4342-03-4
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 12 mg/mL (65.86 mM)
Water (warmed with 50ºC water bath) 2 mg/mL (10.97 mM)
Ethanol (warmed with 50ºC water bath) 1 mg/mL (5.48 mM)
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

0.750mg/ml (4.12mM) Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 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.
in vitro Treatment of Dacarbazine sensitizes melanomas to lysis of peptide-specific CTL and it is mediated through Fas-independent pathway[2].
in vivo Treatment of combination of Axitinib and this compound 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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 UACC903 (UACC) cells
濃度 20 μM
反応時間 48 h
実験の流れ

Apotosis assay: UACC903 (UACC) cells treated with or without this compound (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.

動物実験 動物モデル B16F1 melanoma xenograft model(C57BL/6 mice background)
投薬量 80 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/10840932/
  • https://pubmed.ncbi.nlm.nih.gov/15034078/
  • https://pubmed.ncbi.nlm.nih.gov/23946779/

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Pan-inhibition of super-enhancer-driven oncogenic transcription by next-generation synthetic ecteinascidins yields potent anti-cancer activity [ Nat Commun, 2025, 16(1):512] PubMed: 39779693
In situ and dynamic screening of extracellular vesicles as predictive biomarkers in immune-checkpoint inhibitor therapies [ J Nanobiotechnology, 2025, 23(1):411] PubMed: 40457452
Biofabrication of pheochromocytoma and paraganglioma tumor organoids and assessment of response to systemic therapy [ Sci Rep, 2025, 15(1):35889] PubMed: 41087622
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
APOBEC3B coordinates R-loop to promote replication stress and sensitize cancer cells to ATR/Chk1 inhibitors [ Cell Death Dis, 2023, 14(6):348] PubMed: 37270643
Protocatechuic aldehyde acts synergistically with dacarbazine to augment DNA double-strand breaks and promote apoptosis in cutaneous melanoma cells [ BMC Complement Med Ther, 2023, 23(1):111] PubMed: 37024907
Protocatechuic aldehyde acts synergistically with dacarbazine to augment DNA double-strand breaks and promote apoptosis in cutaneous melanoma cells [ BMC Complement Med Ther, 2023, 23(1):111] PubMed: 37024907
Cytidine analogs are synthetic lethal with base excision repair default due to MBD4 deficiency [ NPJ Precis Oncol, 2022, 6(1:81)] PubMed: 36323843
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] PubMed: 35207746
Extra Virgin Olive Oil Secoiridoids Modulate the Metabolic Activity of Dacarbazine Pre-Treated and Treatment-Naive Melanoma Cells [ Molecules, 2022, 27(10)3310] PubMed: 35630786

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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