Description
AG957 is a tyrosine phosphorylation inhibitor that targets transforming Bcr-Abl fusion proteins (p185Bcr-Abl, p210Bcr-Abl), as well as normal c-Abl . The abl proto-oncogene is expressed in all cell types. The protein p140c-abl is localized both to the nucleus and the cytoplasm. The abl transforming proteins p160gag-abl, p210bcr-abl, and p185bcr-abl are exclusively cytoplasmic proteins. The intrinsic protein tyrosine kinase activity of the transforming abl proteins is higher than that of the normal p140c-abl . AG957 is a tyrosine phosphorylation inhibitor. AG957 inhibited human p185Bcr-Abl, p210Bcr-Abl and normal c-Abl with IC50 values of 4.3, 1, and 7.1 μM, respectively. AG957 inhibited mouse normal c-Abl with IC50 value of 6 μM. AG957 also inhibited epidermal growth factor receptor with IC50 value of 0.25 μM. In chronic myelogenous leukemia (CML) K562 cells, AG957 inhibited p210bcr-abl kinase activity and cell growth. AG957 at 20 μM also inhibited DNA synthesis as early as 2 h by 60% . In K562 cells, AG957, a selective Bcr-Abl inhibitor, blocked taxol-induced PKCi activation and sensitized these cells to taxol-induced apoptosis . In mice, AG957, the c-Abl inhibitor, attenuated LPS-induced pulmonary permeability .
Product information
CAS Number: 140674-76-6
Molecular Weight: 273.28
Formula: C15H15NO4
Chemical Name: methyl 4-{[(2,5-dihydroxyphenyl)methyl]amino}benzoate
Smiles: COC(=O)C1C=CC(=CC=1)NCC1C=C(O)C=CC=1O
InChiKey: QSFREBZMBNRGOK-UHFFFAOYSA-N
InChi: InChI=1S/C15H15NO4/c1-20-15(19)10-2-4-12(5-3-10)16-9-11-8-13(17)6-7-14(11)18/h2-8,16-18H,9H2,1H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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