ChemicalBook Product Catalog API Antineoplastic agents Alkylating antineoplastic Dacarbazine citrate

Dacarbazine citrate

Product NameDacarbazine citrate
CAS64038-56-8
MFC12H18N6O8
MW374.31
EINECS
MOL File64038-56-8.mol

Usage And Synthesis

Uses

Dacarbazine citrate is a cell cycle nonspecific antineoplastic alkylating agent. Dacarbazine citrate inhibits T and B lymphoblastic response, with IC50 values of 50 and 10 μg/mL, respectively. Dacarbazine Citrate can be used for the research of apoptosis and various cancers such as metastatic malignant melanoma[1][2].

in vivo

Dacarbazine citrate (1 mg/kg, i.p.) evokes a concentration-dependent calcium response and the maximum calcium response with an EC₅₀ value of 16 μM in a subset of cells of cultured mouse DRG neurons and excites TRPA1 in rodent sensory neurons^[3].
Dacarbazine citrate (1 mg/kg, i.p.; 1, 3, 5 and 7 days for chronic pain or 1 mg/kg, i.p. for acute treatment) induces mechanical and cold allodynia in mice^[3].
Dacarbazine citrate-induced nociception can be reduced by TRPA1-deficient mice and antisense oligonucleotide for the TRPA1 receptor^[3].
Dacarbazine citrate-induced chronic nociception can be reduced by selective TRPA1 receptor antagonists and antioxidants^[3].
Dacarbazine citrate-induced nociception can be resisted by RPA1 antagonist or an antioxidant in a tumor-associated cancer pain model^[3].

Animal Model:	C57BL/6, Trpa1^+/+ or Trpa1^/ mice^[3]
Dosage:	1 mg/kg
Administration:	1 mg/kg, i.p. (for acute treatment); 1 mg/kg, i.p.; 1, 3, 5 and 7 days (for chronic pain)
Result:	Caused mechanical allodynia with acute or repeated administration.

References

[1] Abdullah A Al-Badr, et al. Dacarbazine. Profiles Drug Subst Excip Relat Methodol DOI:10.1016/bs.podrm.2015.12.002
[2] J M Rojo, et al. Inhibition of T and B lymphoblastic response by mithramycin, dacarbazine, prospidium chloride and peptichemio. Chemotherapy. 1983;29(5):345-51. DOI:10.1159/000238218
[3] Int J Cancer, et al. Dacarbazine alone or associated with melanoma-bearing cancer pain model induces painful hypersensitivity by TRPA1 activation in mice. Int J Cancer. 2020 May 15;146(10):2797-2809. DOI:10.1002/ijc.32648

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