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Merck
CN

428150

Lavendustin A

A cell-permeable, reversible, and substrate competitive inhibitor of EGF receptor tyrosine kinase and p60c-src with little effect on protein kinase A or protein kinase C.

别名:

Lavendustin A, 5-Amino-[(N-2,5-dihydroxybenzyl)-Nʹ-2-hydroxybenzyl]salicylic Acid, RG14355

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关于此项目

经验公式(希尔记法):
C21H19NO6
化学文摘社编号:
分子量:
381.38
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

off-white

solubility

ethanol: 10 mg/mL, DMSO: soluble

shipped in

ambient

storage temp.

−20°C

SMILES string

N(Cc3c(ccc(c3)O)O)(Cc2c(cccc2)O)c1cc(c(cc1)O)C(=O)O

InChI

1S/C21H19NO6/c23-16-6-8-19(25)14(9-16)12-22(11-13-3-1-2-4-18(13)24)15-5-7-20(26)17(10-15)21(27)28/h1-10,23-26H,11-12H2,(H,27,28)

InChI key

ULTTYPMRMMDONC-UHFFFAOYSA-N

General description

A cell-permeable, reversible, and substrate competitive inhibitor of EGF receptor tyrosine kinase (IC50 = 11 nM) and p60c-src (IC50 = 500 nM) with little effect on protein kinase A or protein kinase C (IC50 >200 µM). Also inhibits NMDA-stimulated cGMP production (IC50 = 30 nM). Exhibits anti-proliferative properties. Suppresses the angiogenic action of vascular endothelial growth factor (VEGF) in rats.
A cell-permeable, reversible, substrate competitive, and potent inhibitor of EGF receptor tyrosine kinase (IC50 = 11 nM) and pp60c-src (IC50 = 500 nM) with little effect on protein kinase A or protein kinase C (IC50 >200 µM). Also inhibits NMDA-stimulated cGMP production (IC50 = 30 nM). Exhibits anti-proliferative properties. Suppresses the angiogenic action of vascular endothelial growth factor in rats.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
EGF receptor tyrosine kinase
Product does not compete with ATP.
Reversible: yes
Target IC50: 11 nM and 500 nM against EGF receptor tyrosine kinase and p60c-src, respectively

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Further dilute with aqueous buffer just prior to use.

Other Notes

Hu, D.E., and Fan, T.-P. 1995. Br. J. Pharmacol. 114, 262.
Rodriguez, J., et al. 1994. Neuropharmacology 33, 1267.
Hsu, C.-Y., et al. 1991. J. Biol. Chem.266, 21105.
O’Dell, T.J., et al. 1991. Nature 353, 558; Onoda, T., et al. 1989. J. Nat. Prod.52, 1252.
Bishop, J.M. 1983. Annu. Rev. Biochem. 52, 307.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)


存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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全球贸易项目编号

货号GTIN
428150-1MG04055977210545