Cookie Policy: This site uses cookies to improve your experience. You can find out more about our use of cookies in our Privacy Policy. By continuing to browse this site you agree to our use of cookies.
AdipoGen Life Sciences
Dasatinib
35
CHF
CHF 35.00
In stock
AG-CR1-3540-M01010 mgCHF 35.00
AG-CR1-3540-M05050 mgCHF 50.00
AG-CR1-3540-M250250 mgCHF 180.00
| Product Details | |
|---|---|
| Synonyms | BMS-354825; Sprycel; N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide |
| Product Type | Chemical |
| Properties | |
| Formula |
C22H26ClN7O2S |
| MW | 488.0 |
| CAS | 302962-49-8 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO (50mg/ml) or DMF (25mg/ml). |
| Identity | Determined by 1H-NMR. |
| InChi Key | ZBNZXTGUTAYRHI-UHFFFAOYSA-N |
| Smiles | ClC1=C(NC(C2=CN=C(NC3=CC(N4CCN(CCO)CC4)=NC(C)=N3)S2)=O)C(C)=CC=C1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Dasatinib is a potent multi-kinase inhibitor of the non-receptor tyrosine kinases Abl and Src as well as other members of the Src family. Dasatinib is a highly potent pan-Src/Bcr-Abl inhibitor (Ki values are 16 and 30 pM, respectively). It is also effective at sub-nanomolar concentrations, inhibiting Lyn, Fyn, EPHA2, PDGFR, c-Kit, Lck and Yes. At nanomolar concentrations, Dasatinib also blocks the activity of several other receptor and non-receptor tyrosine kinases, plus drug resistant mutants.
- Dasatinib has potential therapeutic value in diseases that are characterized by elevated levels of these kinases, including some forms of cancer and fibrotic disease. It suppresses invasion and induces cell cycle arrest and apoptosis of head and neck squamous cell carcinoma and non-small cell lung cancer cells. Inhibits proliferation of tumor cells in vitro and exhibits anticancer acivity in vivo in a mouse chronic myelogenous leukemia (CML) xenograft model.
- Dasatinib shows immunosuppressive, senolytic and antiviral properties. Dasatinib inhibits replication of SARS-CoV and MERS-CoV in vitro (EC50 = 2.1 and 5.5 μM, respectively) and shows also activity against Denuge virus and SARS-CoV-2.
Product References
- 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: L.J. Lombardo, et al.; J. Med. Chem. 47, 6658 (2004)
- Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases: T.A. Carter, et al.; PNAS 102, 11011 (2005)
- Dasatinib (BMS-354825) tyrosine kinase inhibitor suppresses invasion and induces cell cycle arrest and apoptosis of head and neck squamous cell carcinoma and non-small cell lung cancer cells: F.M. Johnson, et al.; Clin. Cancer Res. 11, 6924 (2005)
- 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 (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor: J. Das, et al.; J. Med. Chem. 49, 6819 (2006)
- Intracellular tyrosine kinases as novel targets for anti-fibrotic therapy in systemic sclerosis: J.H.W. Distler & O. Distler; Rheumatology 47, 10 (2008)
- Dasatinib in chronic myeloid leukemia: a review: D.G. Aguilera & A.M. Tsimberidou; Ther. Clin. Risk. Manag. 5, 281 (2009)
- Dasatinib: a potent SRC inhibitor in clinical development for the treatment of solid tumors: J. Araujo & C. Logothetis; Cancer Treat. Rev. 36, 492 (2010) (Review)
- Dasatinib: an anti-tumour agent via Src inhibition: A. Gnoni, et al.; Curr. Drug Targets. 12, 563 (2011) (Review)
- Comprehensive analysis of kinase inhibitor selectivity: M.I. Davis, et al.; Nat. Biotechnol. 29, 1046 (2011)
- Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib: X. Ren, et al.; J. Med. Chem. 56, 879 (2013)
- Repurposing of clinically developed drugs for treatment of Middle East Respiratory Syndrome coronavirus infection: J. Dyall, et al.; Antimicrob. Agents Chemother. 58, 4885 (2014)
- Src Tyrosine Kinase Inhibitors: New Perspectives on Their Immune, Antiviral, and Senotherapeutic Potential: J. Rivera-Torres & E. San Jose; Front. Pharmacol. 10, 1011 (2019)
- Repurposing of Kinase Inhibitors for Treatment of COVID-19: E. Weisberg, et al.; Pharma. Res. 37, 167 (2020)
- Structure-Based Virtual Screening Reveals Ibrutinib and Zanubrutinib as Potential Repurposed Drugs against COVID-19: S. Kaliamurthi, et al.; Int. J. Mol. Sci. 22, 7071 (2021)
- c-Src-mediated phosphorylation and activation of kinesin KIF1C promotes elongation of invadopodia in cancer cells: T. Saji, et al.; J. Biol. Chem. 102090, ahead of print (2022)
Related Products
