1. Protein Tyrosine Kinase/RTK
  2. Bcr-Abl Src
  3. PD173955

PD173955 is an orally active inhibitor of Src (IC50= 22 nM), Yes, Abl, ATP and MAP kinases. PD173955 can effectively prevent the mitotic process and has anticancer activity.

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

PD173955 Chemical Structure

PD173955 Chemical Structure

CAS No. : 260415-63-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 209 In-stock
Solution
10 mM * 1 mL in DMSO USD 209 In-stock
Solid
1 mg USD 90 In-stock
5 mg USD 190 In-stock
10 mg USD 336 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PD173955

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PD173955 is an orally active inhibitor of Src (IC50= 22 nM), Yes, Abl, ATP and MAP kinases. PD173955 can effectively prevent the mitotic process and has anticancer activity[1][2][3][4].

IC50 & Target

IC50: 22 nM (Src)[1].

In Vitro

PD173955 inhibits cell growth in MDA-MB-468 and MCF-7 breast cancer cells with IC50 values of 500 nM and 1 μM, respectively[1].
PD173955 (100 nM; 10 min) significantly inhibits the activity of src and yes kinases in MDA-MB-468 breast cancer cells[1].
PD173955 (5 μM; 24 h) can block the cells in the G2-M phase and has anti-mitotic activity in MDA-MB-468 breast cancer cells[1].
PD166326 (0.1-1000 nM; 42 h) can inhibit cell proliferation in R10(-) cells with IC50 0.2 nM, and can inhibit stem cell factor (SCF) -dependent proliferation in parental MO7e cells with IC50 12 nM[4].

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

Cell Cycle Analysis[1]

Cell Line: MDA-MB-468
Concentration: 5 μM
Incubation Time: 24 h
Result: Blocked 95% of the cells in the G2-M phase.

Cell Proliferation Assay[4]

Cell Line: MO7e, R10(-)(a cell line derived from P210-MO7e)
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 48 h
Result: Completely blocked the growth of R10 cells at 2.5 nM.
Inhibited stem cell factor (SCF) -dependent proliferation at 5-10 nM and completely inhibited SCF-dependent growth at 50 nM.
In Vivo

PD166326 (50 mg/kg; Oral gavage; Twice daily) has anti-leukemia activity in CML mice[4].

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

Animal Model: Balb/c mice model of chronic myeloid leukemia (CML)[4]
Dosage: 50 mg/kg
Administration: Oral gavage (p.o.), Twice daily for 4 days
Result: Significantly inhibited constitutive tyrosine phosphorylation of numerous proteins (including Lyn) in primary Bcr/abl expressing leukemia cells.
Reduced the number of mice with splenomegaly and inhibited splenomegaly in at least half of the mice compared to the control group.
Was effective in reducing the peripheral blood granulocytosis of the murine CML-like disease.
Molecular Weight

443.35

Formula

C21H16Cl2N4OS

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=CC(SC)=C4)N=C3N1C

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 : 10 mg/mL (22.56 mM; ultrasonic and warming and heat to 80°C; 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 2.2556 mL 11.2778 mL 22.5555 mL
5 mM 0.4511 mL 2.2556 mL 4.5111 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.

  • Molarity Calculator

  • Dilution Calculator

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

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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 (5.64 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% Corn Oil

    Solubility: ≥ 1 mg/mL (2.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 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 (10.0 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

Purity: 99.12%

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 2.2556 mL 11.2778 mL 22.5555 mL 56.3889 mL
5 mM 0.4511 mL 2.2556 mL 4.5111 mL 11.2778 mL
10 mM 0.2256 mL 1.1278 mL 2.2556 mL 5.6389 mL
15 mM 0.1504 mL 0.7519 mL 1.5037 mL 3.7593 mL
20 mM 0.1128 mL 0.5639 mL 1.1278 mL 2.8194 mL
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PD173955 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.

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PD173955
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