302962-49-8 Dasatinib AKSci J10239
 
 
Loading Please Wait...
  J10239    
Dasatinib
, 99% (HPLC)
 
BMS-354825




IDENTITY
CAS Number:302962-49-8
MDL Number:MFCD11046566
MF:C22H26ClN7O2S
MW:488.01
SPECIFICATIONS & PROPERTIES
Purity:99% (HPLC)
Spectra:NMR, LCMS, FT-IR, HPLC
Physical Form:White to off-white to light yellow powder
Melting Point:275-286°C
Long-Term Storage:Store at room temperature
UN #:Not hazmat

BIOLOGICAL INFO
Solubility:DMSO: 98mg/mL; H2O: <1mg/mL; EtOH: <1mg/mL
Application(s):Multi- BCR/ABL and Src family tyrosine kinase inhibitor
Form:Free Base

REVIEW

 Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.

REFERENCES
[1]Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ, Gillooly KM, Behnia K, Schieven GL, Wityak J, Barrish JC: 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 Med Chem. 2006 Nov 16;49(23):6819-32.
[2] 'Talpaz M, Shah NP, Kantarjian H, Donato N, Nicoll J, Paquette R, Cortes J, O''Brien S, Nicaise C, Bleickardt E, Blackwood-Chirchir MA, Iyer V, Chen TT, Huang F, Decillis AP, Sawyers CL: Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N Engl J Med. 2006 Jun 15;354(24):2531-41. '

GHS

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


Current as of January 17, 2019


Download SDS

CATEGORIES

 APIs and Bioactives > Protein Kinase Inhibitors


PubChem