Dasatinib
| Code | Size | Price |
|---|
| AG-CR1-3540-M010 | 10 mg | £35.00 |
Quantity:
| AG-CR1-3540-M050 | 50 mg | £45.00 |
Quantity:
| AG-CR1-3540-M250 | 250 mg | £140.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
AMBIENT
Storage:
Short Term: +4°C Long Term: -20°C
Documents
Further Information
Alternate Names/Synonyms:
BMS-354825; Sprycel; N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide
Appearance:
White to off-white solid.
CAS:
302962-49-8
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS06,GHS08,GHS09
Handling Advice:
Keep cool and dry.
Hazards:
H301, H360D, H400
InChi:
InChI=1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)
InChiKey:
ZBNZXTGUTAYRHI-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 302962-49-8. Formula: C22H26ClN7O2S. MW: 488. 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.
MDL:
MFCD11046566
Molecular Formula:
C22H26ClN7O2S
Molecular Weight:
488
Package Type:
Plastic Vial
Precautions:
P264, P270, P301, P310, P321, P330, P405, P501, P201, P202, P281, P308, P313, P273, P391
Product 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.
Purity:
>98% (HPLC)
Signal word:
Danger
SMILES:
ClC1=C(NC(C2=CN=C(NC3=CC(N4CCN(CCO)CC4)=NC(C)=N3)S2)=O)C(C)=CC=C1
Solubility Chemicals:
Soluble in DMSO (50mg/ml) or DMF (25mg/ml).
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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)