Diaveridine

Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.

Product information

CAS Number: 5355-16-8

Molecular Weight: 260.29

Formula: C13H16N4O2

Chemical Name: 5-[(3,4-dimethoxyphenyl)methyl]pyrimidine-2,4-diamine

Smiles: COC1=CC=C(CC2=CN=C(N)N=C2N)C=C1OC

InChiKey: LDBTVAXGKYIFHO-UHFFFAOYSA-N

InChi: InChI=1S/C13H16N4O2/c1-18-10-4-3-8(6-11(10)19-2)5-9-7-16-13(15)17-12(9)14/h3-4,6-7H,5H2,1-2H3,(H4,14,15,16,17)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 32 mg/mL (122.94 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Diaveridine is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent. Treatments with Diaveridine for 90 min have a strong bactericidal effect on S. typhimurium TA1535, and no bacterial growth is observed at 10μg/mL or more. Without metabolic activation, treatment with Diaveridine for 48 h, but not 24 h, causes a dose-dependent, significant increase in the frequency of aberrant metaphases. At 100 μg/mL, 60% of the metaphases contain chromosome aberrations.

In Vivo:

The sperm abnormality of the Diaveridine (DVD) treatment groups at all dose levels (Diaveridine, 128 to 512 mg/kg) shows no significant differences compare with the negative control group. There are no significant differences of micronucleus between the negative control group and the Diaveridine treatment groups (Diaveridine, 128 to 512 mg/kg). The chromosome aberration of the Diaveridine treatment groups at all dose levels and the negative control group are significantly lower than those in the positive control group treated with cyclophosphamide (P<0.05), indicating that Diaveridine at the doses studied does not cause abnormal chromosome aberration. The results demonstrate that the Diaveridine administration does not produce significant changes in the ratio of organ-to-body weight, compare with the negative control group in the end period of the study.

Products are for research use only. Not for human use.