| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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Purity: ≥98%
Tyrphostin-9 (also named as Malonoben; SF-6847; RG-50872; AG-17; GCP-5126; NSC-242557) is a novel and potent epidermal growth factor receptor (EGFR) inhibitor with potential anticancer activity. In the human epidermoid carcinoma cell line A431, it inhibits EGFR with an IC50 value of 460 µM. It exhibits strong in vitro anti-proliferative activity against a range of cancer cell lines, including PDGF-dependent SMC, which has an IC50 of 40 nM.
| Targets |
PDGFR (IC50 = 0.5 μM); EGFR (IC50 = 460 μM)
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| ln Vivo |
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| Enzyme Assay |
Tyrosine kinase inhibitor tyrophostin A9 is a strong inducer of mitochondrial fission. Out of the 51 tyrosine kinase inhibitors tested against the TNF-induced respiratory burst, tyrphostin A9 proved to be the most effective and selective.
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| Cell Assay |
Tyrphostin A9 prevented the tyrosine phosphorylation of pyk2 induced by TNF without impairing the bactericidal activity of the cells. Tyrphostin A9 (IC50 = 500 nM) is a PDGF receptor tyrosine kinase inhibitor. According to recent research, smooth muscle cells can transition from a contractile to a synthetic phenotype without the need for PDGF receptor tyrosine kinase signaling. However, it appears that these enzymes play a significant role in regulating cell division and intracellular membrane trafficking.
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| Animal Protocol |
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| References |
| Molecular Formula |
C18H22N2O
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| Molecular Weight |
282.38
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| Exact Mass |
282.17
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| Elemental Analysis |
C, 76.56; H, 7.85; N, 9.92; O, 5.67
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| CAS # |
10537-47-0
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)C=C(C#N)C#N
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| InChi Key |
MZOPWQKISXCCTP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22N2O/c1-17(2,3)14-8-12(7-13(10-19)11-20)9-15(16(14)21)18(4,5)6/h7-9,21H,1-6H3
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| Chemical Name |
2-[(3,5-ditert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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: 5 mg/mL (17.71 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O 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 | 3.5413 mL | 17.7066 mL | 35.4133 mL | |
| 5 mM | 0.7083 mL | 3.5413 mL | 7.0827 mL | |
| 10 mM | 0.3541 mL | 1.7707 mL | 3.5413 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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