2. Protein Tyrosine Kinase/RTK Apoptosis
  3. PDGFR c-Kit FLT3 Apoptosis
  4. Tyrphostin AG1296

Tyrphostin AG1296  (Synonyms: AG1296)

Cat. No.: HY-13894 Purity: 99.69%
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Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.

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

Tyrphostin AG1296 Chemical Structure

Tyrphostin AG1296 Chemical Structure

CAS No. : 146535-11-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 152 In-stock
Solution
10 mM * 1 mL in DMSO USD 152 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 187 In-stock
25 mg USD 385 In-stock
50 mg USD 605 In-stock
100 mg USD 1045 In-stock
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Based on 1 publication(s) in Google Scholar

Tyrphostin AG1296 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Tyrphostin AG1296

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Description

Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range[1][2][3].

IC50 & Target[2]

PDGFRα

 

PDGFRβ

 

Cellular Effect
Cell Line Type Value Description References
Caco-2 IC50
0.2 μM
Compound: TYRPHOSTIN AG 1296 (AG 1296)
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
10.21203/rs.3.rs-23951/v1
Caco-2 CC50
1.36 μM
Compound: TYRPHOSTIN AG 1296 (AG 1296)
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
10.21203/rs.3.rs-23951/v1
In Vitro

Tyrphostin AG1296 (0.625-20 μM; 72 h) suppresses viability of PLX4032-resistant melanoma cells[4].
Tyrphostin AG1296 (2.5-20 μM; 48 h) induces apoptosis of A375R cells[4].
Tyrphostin AG1296 (5 and 20 μM; 2 h) inhibits PDGFR phosphorylation in A375R cells[4].
Tyrphostin AG1296 (0.0625-1 μM; 8 h) inhibits migration of A375R cells[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tyrphostin AG1296 Related Antibodies

Cell Viability Assay[4]

Cell Line: PLX4032-resistant cell lines (A375R and SK-MEL-5R)
Concentration: 0.625, 1.25, 5, 20 μM
Incubation Time: 72 h
Result: Reduced the viability of both PLX4032-sensitive and PLX4032-resistant cell lines.

Apoptosis Analysis[4]

Cell Line: A375R cells
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 48 h
Result: Induced dramatic apoptosis in A375R cells.

Western Blot Analysis[4]

Cell Line: A375R cells
Concentration: 5, 20 μM
Incubation Time: 2 h
Result: Inhibited phosphorylation of both PDGFR-α and PDGFR-β.
In Vivo

Tyrphostin AG1296 (40 and 80 mg/kg; i.p. daily for two weeks) suppresses A375R tumor growth in vivo[4].
Tyrphostin AG1296 (2 mg/kg; i.p. every other day for 3 weeks) inhibits the atherosclerotic plaque progression and enhances plaque stability by inhibiting inflammatory responses, reducing the expression of matrix metalloproteinases and promoting macrophages from proinflammatory phenotype to anti-inflammatory phenotype[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nud/nud mice are injected with A375R cells[4]
Dosage: 40, 80 mg/kg
Administration: I.p. daily for two weeks
Result: Led to an intermediate level of tumor growth suppression at dose of 40 mg/kg, and significant inhibition of A375R tumor growth at dose of 80 mg/kg.
Well tolerated by healthy mice without significant signs of overt toxicity or weight loss.
Molecular Weight

266.29

Formula

C16H14N2O2
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

COC1=C(OC)C=C2N=CC(C3=CC=CC=C3)=NC2=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 : 33.33 mg/mL (125.16 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 3.7553 mL 18.7765 mL 37.5530 mL
5 mM 0.7511 mL 3.7553 mL 7.5106 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (9.39 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7553 mL 18.7765 mL 37.5530 mL 93.8826 mL
5 mM 0.7511 mL 3.7553 mL 7.5106 mL 18.7765 mL
10 mM 0.3755 mL 1.8777 mL 3.7553 mL 9.3883 mL
15 mM 0.2504 mL 1.2518 mL 2.5035 mL 6.2588 mL
20 mM 0.1878 mL 0.9388 mL 1.8777 mL 4.6941 mL
25 mM 0.1502 mL 0.7511 mL 1.5021 mL 3.7553 mL
30 mM 0.1252 mL 0.6259 mL 1.2518 mL 3.1294 mL
40 mM 0.0939 mL 0.4694 mL 0.9388 mL 2.3471 mL
50 mM 0.0751 mL 0.3755 mL 0.7511 mL 1.8777 mL
60 mM 0.0626 mL 0.3129 mL 0.6259 mL 1.5647 mL
80 mM 0.0469 mL 0.2347 mL 0.4694 mL 1.1735 mL
100 mM 0.0376 mL 0.1878 mL 0.3755 mL 0.9388 mL
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Tyrphostin AG1296 Related Classifications

Help & FAQs
  • 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.

Keywords:

Tyrphostin AG1296146535-11-7AG1296Tyrphostin AG 1296Tyrphostin AG-1296AG 1296AG-1296PDGFRc-KitFLT3ApoptosisPlatelet-derived growth factor receptorSCFRCD117Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3platelet-derivedgrowthfactorPDGFαβstemcellInhibitorinhibitorinhibit

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