| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
| Targets |
EGFR (epidermal growth factor receptor) tyrosine kinase. Lavendustin A also inhibits p60c-src with lower potency. It is selective over PKA, PKC, and PI 3-kinase. The inhibition is reversible and does not compete with ATP.
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|---|---|
| ln Vitro |
In medium-dispersed cultures, lavendustin A (5-50μM) suppresses progesterone synthesis in a dose-dependent manner [3].
Lavendustin A inhibits EGFR tyrosine kinase with an IC50 of 11 nM. It inhibits p60c-src with an IC50 of 500 nM. It inhibits antigen-induced activation of PTK and histamine release from mast cells with IC50 values of 80 µM and 112 µM, respectively. Selectivity over PKA, PKC, and PI 3-kinase is >100 µM. |
| ln Vivo |
Lavendustin A (10 μg) reduced 133Xe clearance and overall fibrovascular development area in sponges treated with VEGF165 (250 ng) [2].
Lavendustin A is active in vivo. It inhibits VEGF-induced angiogenesis. Detailed in vivo activity data including specific animal models, administration routes, and efficacious doses has not been extensively reported in the available literature. Further studies would be needed to fully characterize its in vivo pharmacological profile. |
| Enzyme Assay |
EGFR tyrosine kinase assay: EGFR is immunoprecipitated from A431 cell lysates and incubated with varying concentrations of Lavendustin A, 20 mM HEPES pH 7.4, 10 mM MgCl₂, 1 mM MnCl₂, 0.1 mM sodium vanadate, and 20 µM ATP containing [γ-³²P]ATP at 30°C for 10 min. The reaction is terminated by adding SDS sample buffer, and proteins are separated by SDS-PAGE. Phosphorylated EGFR is detected by autoradiography or phosphorimaging. IC50 is calculated from the inhibition curve.
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| Cell Assay |
Cell proliferation assay: Cancer cell lines (e.g., A431 or other EGFR-overexpressing cells) are seeded in 96-well plates and treated with Lavendustin A at varying concentrations (0.001-100 µM) for 48-72 hours. Cell viability is measured using MTT or WST-1 assay. The absorbance is read at 570 nm (MTT) or 450 nm (WST-1). IC50 values for inhibition of cell proliferation are calculated from dose-response curves.
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| Animal Protocol |
No detailed in vivo animal experimental protocols have been published in the available literature. In vivo studies would typically involve xenograft tumor models in nude mice bearing EGFR-dependent tumors. Lavendustin A would be administered via intraperitoneal or intravenous routes at various doses, with tumor volume measured regularly. Endpoints would include tumor growth inhibition, survival analysis, and histopathological evaluation.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data has been published in the available literature. Lavendustin A has a molecular weight of 381.4 Da and purity >98%. It is cell-permeable and active in vivo. Comprehensive PK parameters such as bioavailability, half-life, volume of distribution, and clearance remain to be characterized.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published in the available literature. Lavendustin A is for research use only. As with all tyrosine kinase inhibitors, potential off-target effects and cytotoxicity should be considered. Standard laboratory safety practices should be followed when handling this compound.
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| References |
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| Additional Infomation |
5-[(2,5-dihydroxyphenyl)methyl-[(2-hydroxyphenyl)methyl]amino]-2-hydroxybenzoic acid is an aromatic amine. Lavenderin A has been reported in Streptomyces, and relevant data are available. Lavenderin A is a compound isolated from Streptomyces griseogreen strains, and it may exert antitumor activity by inhibiting protein tyrosine kinases and microtubule polymerization. (NCI)
Lavendustin A is a potent, selective, and reversible EGFR tyrosine kinase inhibitor that does not compete with ATP. It shows selectivity over PKA, PKC, and PI 3-kinase (IC50 >100 µM). It inhibits p60c-src with an IC50 of 500 nM. Lavendustin A inhibits VEGF-induced angiogenesis and shows cytotoxic effects on tumor cell lines. No clinical trials or approved上市 status have been reported. |
| Molecular Formula |
C21H19NO6
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|---|---|
| Molecular Weight |
381.384
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| Exact Mass |
381.121
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| CAS # |
125697-92-9
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| Related CAS # |
125697-92-9;
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| PubChem CID |
3894
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| Appearance |
Off-white to light brown solid powder
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| Boiling Point |
741.7ºC at 760 mmHg
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| Melting Point |
205-215 °C
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| Flash Point |
402.4ºC
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| Vapour Pressure |
4.23E-23mmHg at 25°C
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| LogP |
3.414
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
517
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ULTTYPMRMMDONC-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
5-[[(2,5-Dihydroxyphenyl)methyl][(2-hydroxyphenyl)methyl]amino]-2-hydroxybenzoic acid
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| Synonyms |
Lavendustin A RG 14355 RG-14355 RG14355.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~65.55 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6221 mL | 13.1103 mL | 26.2206 mL | |
| 5 mM | 0.5244 mL | 2.6221 mL | 5.2441 mL | |
| 10 mM | 0.2622 mL | 1.3110 mL | 2.6221 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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