| Stereochemistry | ABSOLUTE |
| Molecular Formula | C12H22AsN3O6S |
| Molecular Weight | 411.306 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[As](C)SC[C@H](NC(=O)CC[C@H](N)C(O)=O)C(=O)NCC(O)=O
InChI
InChIKey=JGDXFQORBMPJGR-YUMQZZPRSA-N
InChI=1S/C12H22AsN3O6S/c1-13(2)23-6-8(11(20)15-5-10(18)19)16-9(17)4-3-7(14)12(21)22/h7-8H,3-6,14H2,1-2H3,(H,15,20)(H,16,17)(H,18,19)(H,21,22)/t7-,8-/m0/s1
| Molecular Formula | C12H22AsN3O6S |
| Molecular Weight | 411.306 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Darinaparsin is a novel mitochondrial-targeted agent being developed for the treatment of various hematologic and solid cancers. In a Phase II study in the US, intravenous darinaparsin demonstrated evidence of clinical activity in malignant lymphoma, and in particular peripheral T-cell lymphoma (PTCL). Darinaparsin was granted Orphan Drug Designation in the US and Europe as a treatment of PTCL. The oral formulation is also being tested in Phase I for the treatment of solid tumors. Darinaparsin induces G2/M cell cycle arrest and apoptosis in tumor cells, primarily through disruption of mitochondrial functions, increased reactive oxygen species (ROS) production and modulation of signal transduction pathways.
Approval Year
Doses
AEs
Sourcing
PubMed
Patents
Sample Use Guides
In the latest clinical trial, darinaparsin was given to patients with peripheral T-cell lymphoma at a dose of 300 mg/m2 once daily for 5 consecutive days every 21 days.
Route of Administration:
Intravenous
Du145, PC3, and LnCap prostate cancer cells and primary prostate cells were plated at a density of 3,500 cells/200 mL in 96-well plates. 24 hours after plating, darinaparsin was added at various concentrations (from 0.001 uM to 100 uM). 72 hours after treatment, the MTS reagent was added to the cells. The color change was monitored at 490 nm and data were acquired by SOFT max pro. IC50 concentrations of Du145, PC3, and LnCap cells ranged from approximately 5 to 10 uM. Primary prostate cancer cells isolated from five different patients were equally sensitive to darinaparsin with IC50 concentrations ranging from 2.5 to 20 uM.
