[CAS NO. 148741-30-4] TyrphostinAG879
PRODUCTS SPECIFICATIONS [148741-30-4]
DESCRIPTION [148741-30-4]
Overview
| MDL | MFCD00236450 |
|---|---|
| Molecular Weight | 316.46 |
| Molecular Formula | C18H24N2OS |
| SMILES | S=C(N)/C(C#N)=C/C1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 |
1 Publications Citing Use of MCE
Summary
Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation ( IC 50 of 10 μM), but not TrKB and TrKC . Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC 50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR . Tyrphostin AG 879 has anticancer activity [1] [2] [3] .
In Vitro
Tyrphostin AG 879 (0.5-50 μM; 48 hours; HL-60, U-937, PC-3, HTB-82, HTB-114, TE-671, HTB-115 and HTB-88 cells) treatment significantly and dose dependently decreases cell proliferation in all the cell lines
[1]
.
Tyrphostin AG 879 (0.5-50 μM; 48 hours; HL-60, U-937, PC-3, HTB-82, HTB-114, TE-671, HTB-115 and HTB-88 cells) treatment also induces a dose-dependent increase in apoptosis with the exception of the lines TE-671 and HTB-88 cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [1]
| Cell Line: | HL-60, U-937, PC-3, HTB-82, HTB-114, TE-671, HTB-115 and HTB-88 cells |
| Concentration: | 0.5 μM, 5 μM, 20 μM and 50 μM |
| Incubation Time: | 48 hours |
| Result: | Significantly and dose dependently decreased cell proliferation in all the cell lines. |
Apoptosis Analysis [1]
| Cell Line: | HL-60, U-937, PC-3, HTB-82, HTB-114, TE-671, HTB-115 and HTB-88 cells |
| Concentration: | 0.5 μM, 5 μM, 20 μM and 50 μM |
| Incubation Time: | 48 hours |
| Result: | Induced a dose-dependent increase in apoptosis. |
In Vivo
Tyrphostin AG 879 (100 mg/kg;subcutaneous injection; administered 10 times in 19 days; for 21 days; athymic, immunodepressed NOD/SCID female mice) treatment induces in vivo a decrease in cancer growth in grafted athymic NOD/SCID mice [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Athymic, immunodepressed NOD/SCID female mice (20 g) with HTB-114 and HL-60 cells [1] |
| Dosage: | 100 mg/kg |
| Administration: | Subcutaneous injection; administered 10 times in 19 days; for 21 days |
| Result: | Resulted in dramatic reductions in tumor sizes. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 158.00 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
References
- [1] Rende M et al. Role of nerve growth factor and its receptors in non-nervous cancer growth: efficacy of a tyrosine kinase inhibitor (AG879) and neutralizing antibodies antityrosine kinase receptor A and antinerve growth factor: an in-vitro and in-vivo stud
- [2] Zhou Y et al. Blockade of EGFR and ErbB2 by the novel dual EGFR and ErbB2 tyrosine kinase inhibitor GW572016 sensitizes human colon carcinoma GEO cells to apoptosis. Cancer Res. 2006 Jan 1;66(1):404-11.
- [3] Levitzki A, et al. Tyrosine kinase inhibition: an approach to drug development. Science. 1995 Mar 24;267(5205):1782-8.
Synonyms