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

Tyrphostin AG 879  (Synonyms: AG 879)

Cat. No.: HY-20878 Purity: 99.85%
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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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 88 In-stock
25 mg USD 209 In-stock
50 mg USD 352 In-stock
100 mg USD 605 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 2 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

TrkA

 

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].

MedChemExpress (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].

MedChemExpress (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.
Molecular Weight

316.46

Formula

C18H24N2OS

CAS No.
Appearance

Solid

Color

White to yellow

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (158.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.85%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1600 mL 15.7998 mL 31.5996 mL 78.9989 mL
5 mM 0.6320 mL 3.1600 mL 6.3199 mL 15.7998 mL
10 mM 0.3160 mL 1.5800 mL 3.1600 mL 7.8999 mL
15 mM 0.2107 mL 1.0533 mL 2.1066 mL 5.2666 mL
20 mM 0.1580 mL 0.7900 mL 1.5800 mL 3.9499 mL
25 mM 0.1264 mL 0.6320 mL 1.2640 mL 3.1600 mL
30 mM 0.1053 mL 0.5267 mL 1.0533 mL 2.6333 mL
40 mM 0.0790 mL 0.3950 mL 0.7900 mL 1.9750 mL
50 mM 0.0632 mL 0.3160 mL 0.6320 mL 1.5800 mL
60 mM 0.0527 mL 0.2633 mL 0.5267 mL 1.3166 mL
80 mM 0.0395 mL 0.1975 mL 0.3950 mL 0.9875 mL
100 mM 0.0316 mL 0.1580 mL 0.3160 mL 0.7900 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Tyrphostin AG 879
Cat. No.:
HY-20878
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