| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Tyrphostin A1 is an inactive analog of tyrosine kinase (TK) inhibitors with minimal effects on TK (IC₅₀ > 1250 μM for epidermal growth factor receptor (EGFR) kinase) [1]
. It is used to differentiate TK-mediated effects from non-specific actions. The study suggests a direct, TK-independent action that increases membrane conductance, likely by stimulating Na⁺/Ca²⁺ exchange. [2] |
|---|---|
| ln Vitro |
In guinea pig ventricular myocytes, Tyrphostin A1 (100 μM) significantly increased membrane slope conductance (G₋₄₀/₀) by 1.6 ± 0.3 nS (n=4, P < 0.05) under conditions designed to minimize Na⁺, Ca²⁺, K⁺, and Na⁺/K⁺ pump currents. This stimulatory effect mimicked that of the TK-inhibiting analog Tyrphostin A23, but was distinct from the effects of another TK inhibitor, genistein (GST), in terms of sensitivity to external Ni²⁺ and Na⁺ removal. [2]
The Tyrphostin A1-induced current (shared properties with A23-induced current) was inhibited by omitting external Na⁺ or Ca²⁺, suppressed by chelating internal Ca²⁺ (using pCa10.5 dialysate), and blocked by external Cd²⁺ and Ni²⁺, but was insensitive to changes in internal Cl⁻ concentration and to the Cl⁻ channel blocker anthracene-9-carboxylic acid. The reversal potential (Eᵣₑᵥ) of the induced current was close to the calculated Eᵣₑᵥ for Na⁺/Ca²⁺ exchange. [2] |
| Cell Assay |
The cell-based assay involved whole-cell patch-clamp recordings on enzymatically isolated guinea pig ventricular myocytes. Cells were superfused at 36°C with a modified Tyrode's solution containing (in mM): 140 NaCl, 1 CaCl₂, 1 MgCl₂, 1 BaCl₂, 10 glucose, 0.01 verapamil, and 5 HEPES (pH 7.4 with NaOH). Cells were dialyzed with a pipette-filling solution containing (in mM): 30 CsCl, 106 caesium aspartate, 8 NaCl, 5 MgATP, 5 EGTA, and 5 HEPES (pH 7.2 with CsOH); pCa was set to 7 by adding CaCl₂. Modifications to these solutions (e.g., Na⁺-free, Ca²⁺-free, different pCa buffers) were used in specific experiments. Membrane currents were recorded using an amplifier and software at a 10 kHz sampling rate. The holding potential was -40 mV, with 200-ms test steps to 0 mV applied at 0.2 Hz. Current-voltage relationships were periodically measured. Tyrphostin A1 was prepared as a 100 mM stock solution in DMSO and applied at 100 μM final concentration. Membrane slope conductance between -40 and 0 mV (G₋₄₀/₀) was measured to assess drug effects. [2]
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| Animal Protocol |
The study mentions that experiments were performed in accordance with guidelines for laboratory animal care approved by the Japanese Pharmacological Society, using enzymatically isolated guinea pig ventricular myocytes. [2]
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| References |
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| Additional Infomation |
Tyrphostin 1 is a methoxybenzene compound with anti-aging effects. Tyrphostin A1 is an inactive compound used as a negative control for the inhibition of epidermal growth factor receptor tyrosine kinase activity. Tyrphostin A1 is a synthetic compound and an inactive analog used to distinguish the effects of tyrosine kinase (TK)-mediated effects from the non-specific effects of tyrosine kinase inhibitors. [1] In this study, tyrosine kinase inhibitor A1 increased the membrane conductance of cardiomyocytes without inhibiting TK, suggesting a direct non-targeting effect. Based on ion-dependent and reversal potential measurements, evidence suggests that stimulation of the Na⁺/Ca²⁺ exchanger may be its mechanism of action. This highlights that tyrosine kinase inhibitors can exert TK-independent effects on ion transport systems. [2]
|
| Molecular Formula |
C11H8N2O
|
|---|---|
| Molecular Weight |
184.19
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| Exact Mass |
184.064
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| CAS # |
2826-26-8
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| PubChem CID |
2063
|
| Appearance |
Off-white to yellow solid powder
|
| Density |
1.169g/cm3
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| Boiling Point |
352.4ºC at 760mmHg
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| Melting Point |
113-116ºC(lit.)
|
| Flash Point |
148.8ºC
|
| Vapour Pressure |
3.85E-05mmHg at 25°C
|
| Index of Refraction |
1.589
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| LogP |
2.125
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
|
| Heavy Atom Count |
14
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| Complexity |
289
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
UOHFCPXBKJPCAD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H8N2O/c1-14-11-4-2-9(3-5-11)6-10(7-12)8-13/h2-6H,1H3
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| Chemical Name |
2-[(4-methoxyphenyl)methylidene]propanedinitrile
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| Synonyms |
Tyrphostin 1 Tyrphostin1 Tyrphostin-1
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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 |
| 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 : ≥ 100 mg/mL (~542.92 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (11.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.4292 mL | 27.1459 mL | 54.2918 mL | |
| 5 mM | 1.0858 mL | 5.4292 mL | 10.8584 mL | |
| 10 mM | 0.5429 mL | 2.7146 mL | 5.4292 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05487781 | ENROLLING BY INVITATION | Combination Product: Tirfostina/L-Carnitina | Healthy | Molecule X LLC | 2022-05-24 | Early Phase 1 |
| NCT05879250 | RECRUITING | Procedure: Biospecimen Collection Procedure: Magnetic Resonance Imaging Radiation: Radiation Therapy |
Glioblastoma, IDH-Wildtype MGMT-Unmethylated Glioblastoma |
Northwestern University | 2024-05-22 | Phase 2 |
| NCT01904123 | COMPLETED | Other: Laboratory Biomarker Analysis Other: Pharmacological Study Drug: STAT3 Inhibitor WP1066 |
Metastatic Malignant Neoplasm in the Brain Metastatic Melanoma Recurrent Brain Neoplasm Recurrent Glioblastoma Recurrent Malignant Glioma |
M.D. Anderson Cancer Center | 2018-07-13 | Phase 1 |
| NCT04334863 | COMPLETED | Drug: WP1066 | Brain Metastases Brain Tumor Medulloblastoma |
Emory University | 2020-05-04 | Phase 1 |
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