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Submit ReviewDasatinib
Description: Highly potent pan-Src/Bcr-Abl inhibitor
Alternative Names: BMS-354825
Chemical Name: N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide
Purity: ≥98% (HPLC)
Biological Activity for Dasatinib
Dasatinib is a highly potent pan-Src/Bcr-Abl inhibitor (Ki 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.
Compound Libraries for Dasatinib
Dasatinib is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Dasatinib
| M. Wt | 488.01 |
| Formula | C22H26ClN7O2S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 302962-49-8 |
| PubChem ID | 3062316 |
| InChI Key | ZBNZXTGUTAYRHI-UHFFFAOYSA-N |
| Smiles | CC1=NC(NC2=NC=C(C(NC3=C(C=CC=C3Cl)C)=O)S2)=CC(N4CCN(CC4)CCO)=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Dasatinib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 48.8 | 100 |
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 will affect the solvent volumes required to prepare stock solutions.
| 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 | 4.1 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.05 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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Product Datasheets for Dasatinib
References for Dasatinib
References are publications that support the biological activity of the product.
Das et al (2006) 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. 49 6819 PMID: 17154512
Lombardo et al (2004) 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. 47 6658 PMID: 15615512
Dyall et al (2014) Repurposing of clinically developed drugs for treatment of Middle East Respiratory Syndrome coronavirus infection. Antimicrob.Agents Chemother. 58 4885 PMID: 24841273
Braun et al (2022) Dasatinib is a potent enhancer for CAR T cell generation by CD3-targeted lentiviral vectors. Mol.Ther.Methods Clin.Dev. 28 90 PMID: 36620073
If you know of a relevant reference for Dasatinib, please let us know.
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4 Citations for Dasatinib
Citations are publications that use Tocris products. Selected citations for Dasatinib include:
Ghassan et al (2021) Breast tumor stiffness instructs bone metastasis via maintenance of mechanical conditioning. Cell Rep 35 109293 PMID: 34192535
Jeremy S et al (2021) Melanoma cells adopt features of both mesenchymal and amoeboid migration within confining channels. Sci Rep 11 17804 PMID: 34493759
Ran et al (2020) Eliminating senescent chondrogenic progenitor cells enhances chondrogenesis under intermittent hydrostatic pressure for the treatment of OA. Stem Cell Res Ther 11 199 PMID: 32450920
Asma et al (2020) Resolvin E1 is a pro-repair molecule that promotes intestinal epithelial wound healing. Proc Natl Acad Sci U S A 117 9477-9482 PMID: 32300016
Do you know of a great paper that uses Dasatinib from Tocris? Please let us know.
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