Tyrphostin 8
Based on 1 Customer Validation
Tyrphostin 8 is a tyrosine kinase, with an IC50 of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC50=21 μM).
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 3785-90-8
- Formula: C10H6N2O
- Molecular Weight:170.17
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All EGFR Isoforms
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Biological Activity
|
EGFR 560 μM (IC50) |
calcineuin phosphatase 21 μM (IC50) |
Tyrphostin 8 (10-100 μM; pretreated for 20 min) blocks the Carbachol-initiated PKCδ tyrosine phosphorylation and ERK1/2 activation in parotid acinar cells[1].
Tyrphostin 8 (10-100 μM) produces a rapid and large increase in the basal O2 consumption of parotid acinar[1].
Tyrphostin 8 (10-100 μM) reduces the parotid ATP content by ～90% at the concentration of 100 μM[1].
Tyrphostin 8 increases apical-to-basolateral transport of insulin-transferrin conjugate by enhancing transferrin receptor-mediated transcytosis in filter-grown Caco-2 cell monolayer[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Parotid acinar cells
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Concentration:10, 100 μM
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Incubation Time:Pretreated for 20 min
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Result:Reduced the increase in tyrosine phosphorylation of PKCδ initiated by carbachol.
Reduced the activation of ERK1/2 by carbachol.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3785-90-8
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Appearance Solid
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Molecular Weight 170.17
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Formula C10H6N2O
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Color Light yellow to yellow
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SMILES
C1=C(C=CC(=C1)O)C=C(C#N)C#N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (587.65 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (stored under nitrogen). 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 (stored under nitrogen). 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)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Soltoff SP. Evidence that tyrphostins AG10 and AG18 are mitochondrial uncouplers that alter phosphorylation-dependent cell signaling. J Biol Chem. 2004 Mar 19;279(12):10910-8. [Content Brief]
[2]. Xia CQ, et, al. Tyrphostin-8 enhances transferrin receptor-mediated transcytosis in Caco-2- cells and inreases hypoglycemic effect of orally administered insulin-transferrin conjugate in diabetic rats. Pharm Res. 2001 Feb;18(2):191-5. [Content Brief]
[3]. Martin BL. Inhibition of calcineurin by the tyrphostin class of tyrosine kinase inhibitors. Biochem Pharmacol. 1998 Aug 15;56(4):483-8. [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 (stored under nitrogen). 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 | 5.8765 mL | 29.3824 mL | 58.7648 mL | 146.9119 mL |
| 5 mM | 1.1753 mL | 5.8765 mL | 11.7530 mL | 29.3824 mL | |
| 10 mM | 0.5876 mL | 2.9382 mL | 5.8765 mL | 14.6912 mL | |
| 15 mM | 0.3918 mL | 1.9588 mL | 3.9177 mL | 9.7941 mL | |
| 20 mM | 0.2938 mL | 1.4691 mL | 2.9382 mL | 7.3456 mL | |
| 25 mM | 0.2351 mL | 1.1753 mL | 2.3506 mL | 5.8765 mL | |
| 30 mM | 0.1959 mL | 0.9794 mL | 1.9588 mL | 4.8971 mL | |
| 40 mM | 0.1469 mL | 0.7346 mL | 1.4691 mL | 3.6728 mL | |
| 50 mM | 0.1175 mL | 0.5876 mL | 1.1753 mL | 2.9382 mL | |
| 60 mM | 0.0979 mL | 0.4897 mL | 0.9794 mL | 2.4485 mL | |
| 80 mM | 0.0735 mL | 0.3673 mL | 0.7346 mL | 1.8364 mL | |
| 100 mM | 0.0588 mL | 0.2938 mL | 0.5876 mL | 1.4691 mL |
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