Dasatinib is an inhibitor of tyrosine kinases. I would like to test the effect of Dasatinib in vivo on my T cells. However, Dasatinib has a very low solubility (0.5mg/ml) with PBS, which is usually used, and I would like to use 0.4mg/mouse and inject it IP.
Does anyone have either worked with Dasatinib in vivo and can tell me how they dissolved it and with what solvent besides DMSO or PBS?
Thanks!
Cyclodextrin can be used to improve the aqueous solubility of dasatinib. Here is a paper on the subject:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6386909/
Dasatinib solutions prepared in citrate buffer could be used.
[1] For example, as published by Hughes et al (Tumor Microenviron. 2018; 130–36):
For in vitro use, Dasatinib was dissolved in DMSO at a concentration of 10 mM and stored at -20°C. Subsequent dilutions were made in PBS immediately prior to use.
For in vivo use, Dasatinib was dissolved in 80 mM citrate buffer and delivered by oral gavage. A stock solution of 30 mg/mL was prepared weekly and stored at 4°C. Subsequent dilutions were made daily.
[2] Another example (Baumgart et al, Cancer Chemother Pharmacol. 2017; 79–723):
The daily dose of dasatinib (8 mg/kg) was selected based on tolerability in a 6-month oral toxicity study in SD rats (unpublished data). Exposures in this rat study at 8 mg/kg were projected to be 800 ng h/mL, which is 2 × the exposure at the approved dose of 100 mg/day (397 ng h/mL). Dose selection at 8 mg/kg for this study was also based upon a 5 mg/kg daily dose of dasatinib that has demon- strated efficacy in a mouse model of leukemia. The vehicles was a 80 mM sodium citrate for dasatinib.
Thank you for your answer. Meanwhile I find that 4% DMSO+30% PEG 300+5% Tween 80+ddH2O to obtain 5mg/mL of Dasatinib. (https://www.selleckchem.com/products/Dasatinib.html). I used PBS to obtain my desired concentration of 4mg/mL and it was totally dissolved.
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