2. Protein Tyrosine Kinase/RTK
  3. Bcr-Abl
  4. AG957

AG957  (Synonyms: Tyrphostin AG957; NSC 654705)

Cat. No.: HY-117718
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AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity.

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

AG957 Chemical Structure

AG957 Chemical Structure

CAS No. : 140674-76-6

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Based on 1 publication(s) in Google Scholar

AG957 Related Antibodies

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Description

AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity[1][2]. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity[3].

In Vitro

AG957 inhibit p210bcr-abl tyrosine kinase activity. AG957 inhibits DNA synthesis as early as 2 h (60% inhibition at 20 microM). AG957 inhibits p210bcr-abl tyrosine phosphorylation in living cells by 1 h without an inhibition of total protein phosphorylation[1]. Tyrphostin AG957, a protein tyrosine kinase (PTK) inhibitor which has activity against the p210BCR/ABL kinase, on beta1 integrin function in CML progenitors[2].
AG957 (0.1-100 μM ) pretreatment results in significant inhibition of proliferation of chronic myelogenous leukemia (CML) colony-forming cells (CFC) CML CFC[2].
AG957 (25 μM) partially inhibits phosphorylation of several proteins that are BCR/ABL PTK substrates and are involved in normal integrin signaling in BCR/ABL expressing cells[2].

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

AG957 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: CML and CFC
Concentration: 0, 0.1, 1, 10, 100 μM
Incubation Time: Pretreatment for 1 hour
Result: A significant dose-dependent inhibition of CML CFC growth was seen following preincubation with AG957.

Western Blot Analysis[2]

Cell Line: K562 and BCR/ABL-tranfected M07e cells (MBA-4)
Concentration: 25 μM
Incubation Time: 24 hours
Result: Partially inhibited tyrosine phosphorylation of p210BCR/ABL, the focal adhesion protein paxillin, the p85 regulatory subunit of the PI3K and the adapter protein cbl in K562 cells.
Inhibited phosphorylation of these proteins as well as the adapter protein crkl in MBA4 cells.
In Vivo

AG957 (10 mg/kg; intratracheally 1 h before intratracheal LPS challenge) blocks c-Abl activity in the lung of mice[4].

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

Animal Model: C57BL/6J mice[4]
Dosage: 10 mg/kg
Administration: Intratracheally 1 h before intratracheal LPS challenge
Result: LPS induced significant phosphorylation of paxillin at Y31 and Y118. Inhibition of c-Abl by AG957 attenuated LPS-induced phosphorylation of paxillin at both sites.
LPS induced significant phosphorylation of VE-cadherin in DMSO-treated mice, which was attenuated in AG957-treated mice.
Molecular Weight

273.28

Formula

C15H15NO4
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

OC1=C(C=C(C=C1)O)CNC2=CC=C(C=C2)C(OC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (365.93 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 3.6593 mL 18.2963 mL 36.5925 mL
5 mM 0.7319 mL 3.6593 mL 7.3185 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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.
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 3.6593 mL 18.2963 mL 36.5925 mL 91.4813 mL
5 mM 0.7319 mL 3.6593 mL 7.3185 mL 18.2963 mL
10 mM 0.3659 mL 1.8296 mL 3.6593 mL 9.1481 mL
15 mM 0.2440 mL 1.2198 mL 2.4395 mL 6.0988 mL
20 mM 0.1830 mL 0.9148 mL 1.8296 mL 4.5741 mL
25 mM 0.1464 mL 0.7319 mL 1.4637 mL 3.6593 mL
30 mM 0.1220 mL 0.6099 mL 1.2198 mL 3.0494 mL
40 mM 0.0915 mL 0.4574 mL 0.9148 mL 2.2870 mL
50 mM 0.0732 mL 0.3659 mL 0.7319 mL 1.8296 mL
60 mM 0.0610 mL 0.3049 mL 0.6099 mL 1.5247 mL
80 mM 0.0457 mL 0.2287 mL 0.4574 mL 1.1435 mL
100 mM 0.0366 mL 0.1830 mL 0.3659 mL 0.9148 mL
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AG957 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:

AG957140674-76-6Tyrphostin AG957 NSC 654705AG 957AG-957Tyrphostin AG 957Tyrphostin AG-957NSC654705NSC 654705NSC-654705Bcr-AblChronicmyelogenousleukemiaintegrinstyrosinekinaseBCR/ABLhematopoiesispaxillinc-AbllipopolysaccharidecytoskeletonInhibitorinhibitorinhibit

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