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Purity: ≥98%
Tyrphostin AG 879 (AG-879), a tyrphostin compound, is novel multi-tyrosine kinase inhibitor with potential antitumor activity. It exhibits 100- and 500-fold higher selectivity against ErbB2 over PDGFR and EGFR, and potently inhibits HER2/ErbB2 with an IC50 of 1 μM.
| Targets |
HER2-Neu (IC50 = 1.0 μM); Trk (IC50 = 10 μM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Tyrosine kinase inhibitor tyrphostinAG879 inhibits phosphorylation of TrKA but not TrKB or TrKC. Also an ErbB2 kinase inhibitor, it is at least 500 times more selective against ErbB2 (IC50 = 1 μmol/L) than it is against EGFR (IC50 >500 μmol/L).
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| Cell Assay |
Cells are cultured in 96-well plates with 100 μL of medium in each well. Each well receives ten microliters of MTT solution (5 mg/ml in PBS), and the incubation process is carried out for four hours at 37 °C. Next, add 100 μL of 10% SDS in 0.01 M HCl. Using a reference filter of 690 nm, absorption is measured at 550 nm in an ELISA reader following an overnight incubation at 37°C.
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| Animal Protocol |
nude mice carrying v-Ha-RAS transformed NIH 3T3 cells
20 mg/kg Intraperitoneally administrated on days 3, 5, 7, 10, 12, 14, and 17. |
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| References | ||
| Additional Infomation |
3-amino-2-[(3,5-ditert-butyl-4-oxo-1-cyclohexa-2,5-dienylidene)methyl]-3-mercapto-2-propenenitrile is a monoterpenoid.
Tyrphostin AG 879 is a compound that selectively inhibits protein tyrosine kinase and nerve growth factor-dependent tyrosine phosphorylation. (NCI) |
| Molecular Formula |
C18H24N2OS
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| Molecular Weight |
316.46
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| Exact Mass |
316.16
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| Elemental Analysis |
C, 68.32; H, 7.64; N, 8.85; O, 5.06; S, 10.13
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| CAS # |
148741-30-4
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| Related CAS # |
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| PubChem CID |
135419190
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| Appearance |
White to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
432.7±55.0 °C at 760 mmHg
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| Melting Point |
232 °C
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| Flash Point |
215.5±31.5 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.600
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| LogP |
4.76
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
477
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S=C(/C(/C#N)=C(\[H])/C1C([H])=C(C(=C(C=1[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])O[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])N([H])[H]
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| InChi Key |
XRZYELWZLNAXGE-KPKJPENVSA-N
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| InChi Code |
InChI=1S/C18H24N2OS/c1-17(2,3)13-8-11(7-12(10-19)16(20)22)9-14(15(13)21)18(4,5)6/h7-9,21H,1-6H3,(H2,20,22)/b12-7+
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| Chemical Name |
(E)-2-cyano-3-(3,5-ditert-butyl-4-hydroxyphenyl)prop-2-enethioamide
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| Synonyms |
AG 879; Tyrphostin AG 879; Tyrphostin AG879; Tyrphostin AG-879; AG879; AG-879
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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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1600 mL | 15.7998 mL | 31.5996 mL | |
| 5 mM | 0.6320 mL | 3.1600 mL | 6.3199 mL | |
| 10 mM | 0.3160 mL | 1.5800 mL | 3.1600 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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Annexin V and PI double staining for apoptosis. Cancer Res. 2005 Jul 1;65(13):5848-56. |
Effect of AG1478 + AG879 on inhibition of EGFR and ErbB2 phosphorylation. |
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