| Identification | Back Directory | [Name]
TYRPHOSTIN B48 | [CAS]
133550-35-3 | [Synonyms]
494
AG 494
CS-2755
TYRPHOSTIN B48
-494 Tyrphostin
AG-494 Tyrphostin
TYRPHOSTIN AG 494
TyrphostinAG494>
AG-494;AG 494;AG494
AG 494 (Tyrphostin AG 494)
-2-Cyano-3-(3,4-dihydroxyphenyl)
A-CYANO-(3,4-DIHYDROXY)-N-PHENYLCINNAMIDE
A-CYANO-(3,4-DIHYDROXY)-N-PHENYLCINNAMAMIDE
ALPHA-CYANO-(3,4-DIHYDROXY)-N-PHENYLCINNAMIDE
N-PHENYL-3,4-DIHYDROXYBENZYLIDENECYANOACETAMIDE
(E)-2-Cyano-3-(3,4-dihydroxyphenyl)-N-phenylacrylamide
(E)-2-Cyano-3-(3,4-dihydrophenyl)-N-phenyl-2-propenamide
(E)-2-CYANO-3-(3,4-DIHYDROXYPHENYL)-N-PHENYL-2-PROPENAMIDE
2-Propenamide,2-cyano-3-(3,4-dihydroxyphenyl)-N-phenyl-, (2E)-
N-Phenyl-3,4-dihydroxybenzylidenecyanoacetamide, Tyrphostin B48 | [Molecular Formula]
C16H12N2O3 | [MDL Number]
MFCD00209863 | [MOL File]
133550-35-3.mol | [Molecular Weight]
280.28 |
| Chemical Properties | Back Directory | [Melting point ]
249 °C(dec.) | [storage temp. ]
−20°C
| [solubility ]
DMSO: soluble
| [form ]
Yellow solid. | [color ]
Light yellow to Amber to Dark green |
| Hazard Information | Back Directory | [Description]
Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative, compounds that act as PTK blockers. PTK inhibitors that preferentially inhibit the epidermal growth factor (EGF) receptor kinase block EGF-dependent cell proliferation. AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 μM in HT-22 cells. | [Uses]
AG-494 is a member of the tyrphostin family of tyrosine kinase inhibitors and is a potent inhibitor of EGF receptor autophosphorylation (IC50=1.2 μM) and EGF-dependent cell growth (IC50=6 μM). It selectively inhibits HER1 (EGF receptor) vs. HER1-2 receptor autophosphorylation (HER1: IC50=1.1 μM; HER1-2: IC50=45 μM). HER1-2 is a chimeric receptor consisting of the external HER1 domain fused to an internal HER2 domain. Blocks CDK2 activation and causescells to arrest at late G1 and during S phase. | [Biological Activity]
Potent inhibitor of epidermal growth factor receptor (EGFR) kinase (IC 50 = 0.7 μ M). Selective over ErbB2, PDGFR and insulin receptor kinase (IC 50 values are 42, 6 and > 100 μ M respectively). | [References]
[1]. osherov n, levitzki a. tyrphostin ag 494 blocks cdk2 activation. febs lett, 1997, 410(2-3): 187-190.
[2]. kleinberger-doron n, shelah n, capone r, et al. inhibition of cdk2 activation by selected tyrphostins causes cell cycle arrest at late g1 and s phase. exp cell res, 1998, 241(2): 340-351.
[3]. liu x, qin j, luo q, et al. cross-talk between egf and bmp9 signalling pathways regulates the osteogenic differentiation of mesenchymal stem cells. j cell mol med, 2013, 17(9): 1160-1172.
[4]. bojko a1, reichert k, adamczyk a, et al. the effect of tyrphostins ag494 and ag1478 on the autocrine growth regulation of a549 and du145 cells. folia histochem cytobiol, 2012, 50(2): 186-195. |
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