1. Neuronal Signaling
    Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    Apoptosis
  2. Trk Receptor
    EGFR
    Apoptosis
  3. Tyrphostin AG 879

Tyrphostin AG 879 (Synonyms: AG 879)

Cat. No.: HY-20878 Purity: 99.54%
Handling Instructions

Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity.

For research use only. We do not sell to patients.

Tyrphostin AG 879 Chemical Structure

Tyrphostin AG 879 Chemical Structure

CAS No. : 148741-30-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
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10 mg USD 80 In-stock
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25 mg USD 190 In-stock
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50 mg USD 320 In-stock
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100 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity[1][2][3].

IC50 & Target

IC50: 10 μM (TrKA phosphorylation)[1]
IC50: 1 μM (ErbB2)[2]

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].

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].

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.
Molecular Weight

316.46

Formula

C₁₈H₂₄N₂OS

CAS No.

148741-30-4

SMILES

S=C(N)/C(C#N)=C/C1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1

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
In Vitro: 

DMSO : ≥ 30 mg/mL (94.80 mM)

*"≥" means soluble, but saturation unknown.

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

Tyrphostin AG 879AG 879Tyrphostin AG879Tyrphostin AG-879AG879AG-879Trk ReceptorEGFRApoptosisTropomyosin related kinase receptor Epidermal growth factor receptorErbB-1HER1AntitumorTrKAphosphorylationtyrosineantiproliferationapoptosisp75ErbB2Inhibitorinhibitorinhibit

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