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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.
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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Citations for Dasatinib
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Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
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Kinases Product Listing
A collection of over 400 products for kinase research, the listing includes inhibitors of:
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