Lavendustin C
Based on 1 Customer Validation
Lavendustin C is a potent Ca2+ calmodulin-dependent kinase II (CaMK II) inhibitor with an IC50 of 0.2 μM. Lavendustin C inhibits EGFR-associated tyrosine kinase (IC50=0.012 μM) and pp60c-src(+) kinase (IC50=0.5 μM) .
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.17%
- CAS No.: 125697-93-0
- Formule: C14H13NO5
- Masse moléculaire:275.26
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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CaMK II 0.2 μM (IC50) |
EGFR 0.012 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
4 μM
Compound: 2
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Displacement of [gamma-32P]-ATP from Epidermal growth factor receptor in A431 cell-free extracts
Displacement of [gamma-32P]-ATP from Epidermal growth factor receptor in A431 cell-free extracts
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10.1016/S0960-894X(97)00014-0 |
| ER22 | IC50 |
0.15 μM
Compound: II12
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Inhibition of EGFR(epidermal growth factor receptor) autophosphorylation in ER22 cell membranes
Inhibition of EGFR(epidermal growth factor receptor) autophosphorylation in ER22 cell membranes
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[PMID: 8145236] |
| ER22 | IC50 |
92 μM
Compound: II12
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Inhibition of EGF-stimulated DNA synthesis in ER22 cells, by measuring [3H]Me-dT incorporation into ER 22 cells
Inhibition of EGF-stimulated DNA synthesis in ER22 cells, by measuring [3H]Me-dT incorporation into ER 22 cells
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[PMID: 8145236] |
| HaCaT | IC50 |
>100 μM
Compound: 3
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Cytotoxicity against human HaCaT cells
Cytotoxicity against human HaCaT cells
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[PMID: 20570145] |
| HaCaT | IC50 |
>=100 μM
Compound: 2
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Inhibitory activity of HaCaT keratinocyte cell line
Inhibitory activity of HaCaT keratinocyte cell line
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[PMID: 7990108] |
| HEK293 | IC50 |
1.34 μM
Compound: 8c
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Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay
Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay
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[PMID: 20731357] |
Lavendustin C (Compound 5) shows potent inhibitory activity, and it may be the core structure responsible for inhibition of tyrosine kinase[1].
Lavendustin C (10-150 μM) inhibits tyrosine kinase-associated neutrophil degranulation and superoxide generation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 125697-93-0
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Appearance Solid
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Masse moléculaire 275.26
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Formule C14H13NO5
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Color Off-white to light yellow
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SMILES
O=C(O)C1=CC(NCC2=CC(O)=CC=C2O)=CC=C1O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (363.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. T Onoda, et al.Isolation of a Novel Tyrosine Kinase Inhibitor, Lavendustin A, From Streptomyces Griseolavendus. J Nat Prod. Nov-Dec 1989;52(6):1252-7. [Content Brief]
[2]. T J O'Dell, et al.Long-term Potentiation in the Hippocampus Is Blocked by Tyrosine Kinase Inhibitors. Nature. 1991 Oct 10;353(6344):558-60. [Content Brief]
[3]. H M Burt, et al. Inhibition of Crystal-Induced Neutrophil Activation by a Protein Tyrosine Kinase Inhibitor. J Leukoc Biol. 1994 Jan;55(1):112-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6329 mL | 18.1646 mL | 36.3293 mL | 90.8232 mL |
| 5 mM | 0.7266 mL | 3.6329 mL | 7.2659 mL | 18.1646 mL | |
| 10 mM | 0.3633 mL | 1.8165 mL | 3.6329 mL | 9.0823 mL | |
| 15 mM | 0.2422 mL | 1.2110 mL | 2.4220 mL | 6.0549 mL | |
| 20 mM | 0.1816 mL | 0.9082 mL | 1.8165 mL | 4.5412 mL | |
| 25 mM | 0.1453 mL | 0.7266 mL | 1.4532 mL | 3.6329 mL | |
| 30 mM | 0.1211 mL | 0.6055 mL | 1.2110 mL | 3.0274 mL | |
| 40 mM | 0.0908 mL | 0.4541 mL | 0.9082 mL | 2.2706 mL | |
| 50 mM | 0.0727 mL | 0.3633 mL | 0.7266 mL | 1.8165 mL | |
| 60 mM | 0.0605 mL | 0.3027 mL | 0.6055 mL | 1.5137 mL | |
| 80 mM | 0.0454 mL | 0.2271 mL | 0.4541 mL | 1.1353 mL | |
| 100 mM | 0.0363 mL | 0.1816 mL | 0.3633 mL | 0.9082 mL |
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