WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205920
Description: VAL-083 is a bi-functional alkylating agent, with potential antineoplastic activity. Upon administration, VAL-083 crosses the blood brain barrier (BBB) and appears to be selective for tumor cells. This agent alkylates and crosslinks DNA which ultimately leads to a reduction in cancer cell proliferation. In addition, VAL-083 does not show cross-resistance to other conventional chemotherapeutic agents and has a long half-life in the brain.
MedKoo Cat#: 205920
Chemical Formula: C6H10O4
Exact Mass: 146.05791
Molecular Weight: 146.14
Elemental Analysis: C, 49.31; H, 6.90; O, 43.79
Synonym: VAL083; VAL083; VAL083; Dianhydrodulcitol; Dianhydrogalactitol; Dulcitol Diepoxide;
IUPAC/Chemical Name: (1R,2S)-1-((R)-oxiran-2-yl)-2-((S)-oxiran-2-yl)ethane-1,2-diol
InChi Key: AAFJXZWCNVJTMK-GUCUJZIJSA-N
InChi Code: InChI=1S/C6H10O4/c7-5(3-1-9-3)6(8)4-2-10-4/h3-8H,1-2H2/t3-,4+,5+,6-
SMILES Code: O[C@@H]([C@@H]1OC1)[C@@H]([C@H]2OC2)O
VAL-083 has demonstrated activity in cyclophosphamide, BCNU and phenylanine mustard resistant cell lines and no evidence of cross-resistance has been encountered in published clinical studies. Based on the presumed alkylating functionality of VAL-083, published literature suggests that DNA repair mechanisms associated with Temodar and nitrosourea resistance, such as 06-methylguanine methyltransferace (MGMT), may not confer resistance to VAL-083. VAL-083 readily crosses the blood brain barrier where it maintains a long half-life in comparison to the plasma. Published preclinical and clinical research demonstrates that VAL-083 is selective for brain tumor tissue. VAL-083 has been assessed in multiple studies as chemotherapy in the treatment of newly diagnosed and recurrent brain tumors. In published clinical studies, VAL-083 has previously been shown to have a statistically significant impact on median survival in high grade gliomas when combined with radiation vs. radiation alone. The main dose-limiting toxicity related to the administration of VAL-083 in previous clinical studies was myelosuppression. (source: http://www.delmarpharma.com/product_development_programs/val083/).
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