Dasatinib

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Cat.No. 6793 - Dasatinib | C22H26ClN7O2S | CAS No. 302962-49-8
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
Reviews
Literature

Biological Activity

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.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 48.8 100

Preparing Stock Solutions

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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References

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


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Citations for Dasatinib

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Literature in this Area

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