Dasatinib

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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)
Datasheet
Citations (4)
Reviews

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.

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

Certificate of Analysis / Product Datasheet
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4 Citations for Dasatinib

Citations are publications that use Tocris products. Selected citations for Dasatinib include:

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

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


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