Drug Information

Drug (ID: DG80001) and It's Reported Resistant Information

• Name: Mafosfamide Sodium Salt
• Synonyms: Mafosfamide Sodium Salt|84211-05-2|2-[[2-[bis(2-chloroethyl)amino]-2-oxo-1,3,2lambda5-oxazaphosphinan-4-yl]sulfanyl]ethanesulfonic acid|Z 7557;Z-7557;Z7557;cis-Mafosfamide;Mafosfamid|C9H19Cl2N2O5PS2|CHEMBL59990|SCHEMBL1652310|PBUUPFTVAPUWDE-UHFFFAOYSA-N|6-AMINOCOUMARINHYDROCHLORIDE|MFCD28899125|AKOS015909832|DA-75248|G91294|2-[[2-[bis(2-chloroethyl)amino]-2-oxo-1,3,2|E5-oxazaphosphinan-4-yl]sulfanyl]ethanesulfonic acid|2-[2-(bis-(2 chloroethyl)-amino)-2-oxo-tetrahydro-2H-1,3,2-oxazaphosphorin-4-yl-thio]-ethanesulphonic acid|2-[2-(bis-(2-chloroethyl)-amino)-2-oxo-tetrahydro-2H-1,3,2-oxazaphosphorin-4-yl-thio]-ethanesulphonic acid
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
  Ewing sarcoma [ICD-11: 2B52]; [1]
• Formula: 9
• IsoSMILES: InChI=1S/C9H19Cl2N2O5PS2/c10-2-4-13(5-3-11)19(14)12-9(1-6-18-19)20-7-8-21(15,16)17/h9H,1-8H2,(H,12,14)(H,15,16,17)
• InChI: C1COP(=O)(NC1SCCS(=O)(=O)O)N(CCCl)CCCl
• InChIKey: PBUUPFTVAPUWDE-UHFFFAOYSA-N
• PubChem CID: 104746
• DrugBank ID: DB12083

Type(s) of Resistant Mechanism of This Drug

  EADR: Epigenetic Alteration of DNA, RNA or Protein

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Ewing sarcoma [ICD-11: 2B52]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: hsa-miR-125b-1 [1]

• Resistant Disease: Ewing sarcoma [ICD-11: 2B52.0]
• Molecule Alteration: Expression; Up-regulation
• Experimental Note: Revealed Based on the Cell Line Data
• In Vitro Model: VH-64 cells; Bones; Homo sapiens (Human); CVCL_9672
• In Vitro Model: Sk-N-MC cells; Bones; Homo sapiens (Human); CVCL_0530
• In Vitro Model: RD-ES cells; Bones; Homo sapiens (Human); CVCL_2169
• In Vitro Model: Sk-ES cells; Bones; Homo sapiens (Human); CVCL_0627
• In Vitro Model: TC-71 cells; Bones; Homo sapiens (Human); CVCL_2213
• Experiment for Molecule Alteration: qRT-PCR; Western blot
• Experiment for Drug Resistance: Chemosensitivity assay
• Mechanism Description: We found miR-125b to be upregulated in two different Dox-resistant EWS cell lines. The upregulation of miR-125b was also confirmed in the EWS tumors having survived chemotherapy regimen which includes doxorubicin. When miR-125b was knocked down in EWS cells, both the Dox-resistant and parental cells showed an enhanced sensitivity to doxorubicin, which was associated with the upregulation of the pro-apoptotic molecules, p53 and Bak. Inversely, the overexpression of miR-125b in parental EWS cells resulted in enhanced drug resistance, not only to doxorubicin, but also to etoposide and vincristine.

References

• Ref 1: VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancerMol Cancer Ther. 2013 Feb;12(2):151-61. doi: 10.1158/1535-7163.MCT-12-0466. Epub 2012 Dec 27.