Dasatinib

CHF 60.00
In stock
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Product Details
Synonyms BMS-354825; Sprycel
Product Type Chemical
Properties
Formula C22H26ClN7O2S
MW 488.0
CAS 302962-49-8
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO or ethanol.
Declaration Manufactured by SynKinase.
Other Product Data Target: Abl - BCR - BTK | Kinase Group: PTK | Substrate: Tyrosine

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
InChi Key ZBNZXTGUTAYRHI-UHFFFAOYSA-N
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
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
The BCR-ABL oncogene triggers intracellular signaling, activating multiple transduction cascades, promoting the growth, proliferation and survival of hematopoietic cells. BCR-ABL plays a role in defective DNA repair, alteration of cellular adhesion and inhibition of apoptosis. Degregulated BCR-ABL tyrosine kinase activity is the molecular marker for CML. Inhibiting BCR-ABL tyrosine kinase activity leads to the induction of apoptosis and inhibits cellular proliferation in vitro and there are various BCR-ABL isoforms with differing activity levels as well. Dasatinib (BMS-354825, Sprycel®) is a potent multi-target kinase inhibitor of BCR-ABL. Dasatiinib performs better against ABL kinase than earlier drugs such as imatinib, and Dasatinib also is effective against SRC family of kinases, and other receptor kinases such as EPHA2, PDGFR, and c-Kit. Dasatinib's inhibiting potential against Src family kinase members is greater (IC(50) 0.5nM) than its inhibitory activity against ABL (1nM).
Product References
  1. 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)
  2. Dasatinib in chronic myeloid leukemia: a review: D.G. Aguilera & A.M. Tsimberidou; Ther. Clin. Risk. Manag. 5, 281 (2009)
  3. 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)
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