Synonym
RSU 1164; RSU-1164; RSU1164;
IUPAC/Chemical Name
1-(2,3-dimethylaziridin-1-yl)-3-(2-nitro-1H-imidazol-1-yl)propan-2-ol
InChi Key
VKUQQJFQNDTATQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C10H16N4O3/c1-7-8(2)13(7)6-9(15)5-12-4-3-11-10(12)14(16)17/h3-4,7-9,15H,5-6H2,1-2H3
SMILES Code
OC(CN1C(C)C1C)CN2C=CN=C2[N+]([O-])=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
Preparing Stock Solutions
The following data is based on the
product
molecular weight
240.26
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Siemann DW. The chemosensitizing and cytotoxic effects of RSU 1164 and RSU 1165 in a murine tumor model. Int J Radiat Oncol Biol Phys. 1989 Apr;16(4):1115-8. PubMed PMID: 2703392.
2: Henry JM, Isaacs JT. Synergistic enhancement of the efficacy of the bioreductively activated alkylating agent RSU-1164 in the treatment of prostatic cancer by photodynamic therapy. J Urol. 1989 Jul;142(1):165-70. PubMed PMID: 2733098.
3: Hofer KG, Lakkis M, Hofer MG. Cytocidal effects of misonidazole, Ro 03-8799, and RSU-1164 on euoxic and hypoxic BP-8 murine sarcoma cells at normal and elevated temperatures. Cancer. 1989 Apr 15;63(8):1501-8. PubMed PMID: 2924258.
4: Deacon JM, Holliday SB, Ahmed I, Jenkins TC. Experimental pharmacokinetics of RSU-1069 and its analogues: high tumor/plasma ratios. Int J Radiat Oncol Biol Phys. 1986 Jul;12(7):1087-90. PubMed PMID: 3755713.
5: Walling J, Stratford IJ, Adams GE, Stephens MA. Dual-function radiation sensitizers and bioreductive drugs: factors affecting cellular uptake and sensitizing efficiency in analogues of RSU 1069. Int J Radiat Biol Relat Stud Phys Chem Med. 1988 Apr;53(4):641-9. PubMed PMID: 3258298.
6: Walling JM, Deacon J, Holliday S, Stratford IJ. High uptake of RSU 1069 and its analogues melanotic melanomas. Cancer Chemother Pharmacol. 1989;24(1):28-32. PubMed PMID: 2541936.
7: Roizin-Towle L, Pirro JP, Hall EJ. Studies with bifunctional bioreductive drugs. II. Cytotoxicity assayed with A-549 lung carcinoma cells of human origin. Radiat Res. 1990 Oct;124(1 Suppl):S50-5. PubMed PMID: 2236511.
8: Cole S, Stratford IJ, Adams GE, Fielden EM, Jenkins TC. Dual-function 2-nitroimidazoles as hypoxic cell radiosensitizers and bioreductive cytotoxins: in vivo evaluation in KHT murine sarcomas. Radiat Res. 1990 Oct;124(1 Suppl):S38-43. PubMed PMID: 2236508.
9: Hei TK, He ZY, Piao CQ, Hall EJ. Studies with bifunctional bioreductive drugs. I. In vitro oncogenic transforming potential. Radiat Res. 1990 Oct;124(1 Suppl):S44-9. PubMed PMID: 2236509.
10: Siemann DW. Enhancement of chemotherapy and nitroimidazole-induced chemopotentiation by the vasoactive agent hydralazine. Br J Cancer. 1990 Sep;62(3):348-53. PubMed PMID: 2206941; PubMed Central PMCID: PMC1971466.
11: Hei TK, Piao CQ, He ZY, Hall EJ. Mechanism of oncogenicity for bioreductive drugs. Int J Radiat Oncol Biol Phys. 1992;22(4):747-50. PubMed PMID: 1544847.
12: DeGraff WG, Russo A, Gamson J, Mitchell JB. Evaluation of nitroimidazole hypoxic cell radiosensitizers in a human tumor cell line high in intracellular glutathione. Int J Radiat Oncol Biol Phys. 1989 Apr;16(4):1021-4. PubMed PMID: 2522917.
13: Siemann DW, Sutherland RM. Potentiation of alkylating chemotherapy by dual function nitrofurans in multi-cell spheroids and solid tumors. Radiother Oncol. 1992 Aug;24(4):239-45. PubMed PMID: 1410579.
14: Siemann DW. Cytotoxicity of dual function nitrofurans in rodent and human tumor cells. Int J Radiat Oncol Biol Phys. 1992;22(4):697-700. PubMed PMID: 1544840.
