Triapine is a potent ribonucleotide reductase inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis.
|Cell lines||Wild-type KB and HU-resistant KB nasopharyngeal carcinoma cells.|
|Preparation method||Plating cells at a density of 104 cells/mL per well in 24-well plates. Adding drugs to cells and incubations are continued for a period of 3 generations (untreated control cells), followed by assessment of cell growth by the methylene blue assay.|
|Incubation time||A period of 3 generations|
|Animal models||BALB/cBA/2 (CD2F1) mice with the L1210 leukemia and the M109 lung carcinoma, athymic nu/nu mice with the human A2780 ovarian carcinoma xenograft.|
|Formulation||0.9% NaCl or water|
|Administration||i.p. or i.v.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 20 mg/mL|
|Related DNA/RNA Synthesis Products|
GC7 Sulfate is a deoxyhypusine synthase (DHPS) inhibitor.
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Pyridostatin Trifluoroacetate Salt is a G-quadruplexe stabilizer, with a Kd of 490 nM.
Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
TAS-102 is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride.
6-Thio-2′-deoxyguanosine (6-thio-dG) is a nucleoside analog and telomerase substrate that is incorporated into de novo–synthesized telomeres.
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