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Lavendustin A

BML-EI185

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EGFR inhibitor

Cell permeable tyrosine kinase inhibitor with little effect on cAMP-dependent protein kinase (PKA) or protein kinase C (PKC). Potent and selective inhibitor of the EGF receptor tyrosine kinase (IC₅₀=11nM). Binds to a site on the kinase which is distinct from the ATP and peptide substrate binding sites. Inhibits EGF-induced proliferation of cultured human myometrial smooth muscle cells and suppresses VEGF-induced angiogenesis in rats. Effective at 10µM in cultured leech neurons. Also inhibits NMDA-stimulated cGMP production.

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Product Details

Alternative Name	5-Amino-[(N-2,5-dihydroxybenzyl)-N’-2-hydroxybenzyl]salicylic acid, RG14355
Appearance	Off-white to tan solid.
CAS	125697-92-9
Couple Target	EGFR
Couple Type	Inhibitor
Formula	C₂₁H₁₉NO₆
MW	381.4
Purity	≥95% (HPLC)
Solubility	Soluble in DMSO or ethanol.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored, as supplied, at -20°C.
Handling	Protect from oxygen.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Sterile-filtered saliva is a strong inducer of IL-6 and IL-8 in oral fibroblasts: B. Cvikl, et al.; Clin. Oral. Investig. 19, 385 (2015), Application(s): Treatment of fibroblasts in culture, Abstract
Influence of the tyrosine kinase inhibitors STI571 (Glivec(R)), lavendustin A and genistein on human mast cell line (HMC-1(560)) activation: K. Lober, et al.; J. Cell Biochem. 103, 1076 (2007), Abstract
Inhibition of atrial wall stretch-induced cardiac hormone secretion by lavendustin A, a potent tyrosine kinase inhibitor: P. Taskinen, et al.; Endocrinology 140, 4198 (1999), Abstract
Analysis of epidermal growth factor action in human myometrial smooth muscle cells: J.L. Kornyei, et al.; J. Endocrinol. 146, 261 (1995), Abstract
Solid Phase Synthesis of Lavendustin A and Analogs: J. Green; J. Org. Chem. 60, 4287 (1995)
Suppression of VEGF-induced angiogenesis by the protein tyrosine kinase inhibitor, lavendustin A: D.E. Hu and T.-P.D. Fan; Br. J. Pharmacol. 114, 262 (1995), Abstract
Tyrosine phosphorylation during synapse formation between identified leech neurons: S. Catarsi, et al.; J. Physiol. 485, 775 (1995), Abstract
Blockade of nitric oxide synthesis by tyrosine kinase inhibitors in neurones: J. Rodriguez, et al.; Neuropharmacology 33, 1267 (1994), Abstract
Kinetic analysis of the inhibition of the epidermal growth factor receptor tyrosine kinase by Lavendustin-A and its analogue: C.-Y.J. Hsu, et al.; J. Biol. Chem. 266, 21105 (1991), Abstract
Long-term potentiation in the hippocampus is blocked by tyrosine kinase inhibitors: T.J. O’Dell, et al.; Nature 353, 558 (1991), Abstract

Last modified: May 29, 2024

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Lavendustin A

BML-EI185

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