Dasatinib

Product Description

Dasatinib is a highly potent pan-Src/Bcr-Abl inhibitor (K_i values are 16 and 30 pM, respectively. Inhibits Bcr-Abl, Src, Lck, Fyn, c-kit and Yes with IC₅₀ values in the subnanomolar range. Inhibits proliferation of tumor cells in vitro and exhibits anticancer acivity in vivo in a mouse chronic myelogenous leukemia (CML) xenograft model. Inhibits replication of SARS-CoV and MERS-CoV in vitro (EC₅₀ values are 2.1and 5.5 μM, respectively). Dasatinib also enhances CD3-targeted lentiviral vector-mediated gene transfer by 3 to 10-fold. Targets and eliminates senescent cells. Orally bioavailable.

Solubility

Preparing Stock Solutions for Dasatinib

The following data is based on the product molecular weight 488.01

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.05 mL	10.25 mL	20.49 mL
5 mM	0.41 mL	2.05 mL	4.10 mL
10 mM	0.20 mL	1.02 mL	2.05 mL
50 mM	0.04 mL	0.20 mL	0.41 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Braun Dasatinib is a potent enhancer for CAR T cell generation by CD3-targeted lentiviral vectors. Mol.Ther.Methods Clin.Dev. 2022 PMID: 36620073
• Lombardo Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J.Med.Chem. 2004 PMID: 15615512
• Dyall Repurposing of clinically developed drugs for treatment of Middle East Respiratory Syndrome coronavirus infection. Antimicrob.Agents Chemother. 2014 PMID: 24841273
• Das 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide J.Med.Chem. 2006 PMID: 17154512