Art. -Nr.: HY-10395

PD173955

1 Cited Publications

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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.

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Reinheit: 99.12%
CAS. Nr.: 260415-63-2
Formel: C₂₁H₁₆Cl₂N₄OS
Molecular Weight:443.35

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PD173955 Chemical Structure

CAS. Nr.: 260415-63-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 22 nM (Src)^[1].

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen :

Abl
Bcr-Abl

Alle Src Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	>30 μM Compound: PD-17395	Inhibition of wild type NPM/ALK autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay Inhibition of wild type NPM/ALK autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay	[PMID: 16970400]
BaF3	IC₅₀	>30 μM Compound: PD-17395	Inhibition of wild type NPM/ALK kinase activity in BaF3 cells by radioenzymatic assay Inhibition of wild type NPM/ALK kinase activity in BaF3 cells by radioenzymatic assay	[PMID: 16970400]
BaF3	IC₅₀	1.8 μM Compound: PD-17395	Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay	[PMID: 16970400]
BaF3	IC₅₀	2 μM Compound: PD-17395	Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay	[PMID: 16970400]
BaF3	IC₅₀	2.5 μM Compound: PD-17395	Inhibition of NPM/ALK L256T mutant kinase activity in BaF3 cells by radioenzymatic assay Inhibition of NPM/ALK L256T mutant kinase activity in BaF3 cells by radioenzymatic assay	[PMID: 16970400]
BaF3	IC₅₀	3 μM Compound: PD-17395	Inhibition of NPM/ALK L256T mutant autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay Inhibition of NPM/ALK L256T mutant autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay	[PMID: 16970400]
HCT-8	IC₅₀	1.131 μM Compound: PD-0173955	Inhibition of HCT-8 cell proliferation Inhibition of HCT-8 cell proliferation	[PMID: 10974196]
HCT-8	IC₅₀	1.3 μM Compound: PD-0173955	Inhibition of HCT-8 clonogenic growth in soft agar without pretreatment Inhibition of HCT-8 clonogenic growth in soft agar without pretreatment	[PMID: 10974196]
HCT-8	IC₅₀	2.52 μM Compound: PD-0173955	Inhibition of HCT-8 clonogenic growth in soft agar with pretreatment Inhibition of HCT-8 clonogenic growth in soft agar with pretreatment	[PMID: 10974196]
HT-29	IC₅₀	0.81 μM Compound: PD-0173955	Inhibition of HT-29 cell proliferation Inhibition of HT-29 cell proliferation	[PMID: 10974196]
HT-29	IC₅₀	1.21 μM Compound: PD-0173955	Inhibition of HT-29 clonogenic growth in soft agar with pretreatment Inhibition of HT-29 clonogenic growth in soft agar with pretreatment	[PMID: 10974196]
HT-29	IC₅₀	1.29 μM Compound: PD-0173955	Inhibition of HT-29 clonogenic growth in soft agar without pretreatment Inhibition of HT-29 clonogenic growth in soft agar without pretreatment	[PMID: 10974196]
SW-620	IC₅₀	0.924 μM Compound: PD-0173955	Inhibition of SW-620 cell proliferation Inhibition of SW-620 cell proliferation	[PMID: 10974196]
SW-620	IC₅₀	0.98 μM Compound: PD-0173955	Inhibition of SW-620 clonogenic growth in soft agar without pretreatment Inhibition of SW-620 clonogenic growth in soft agar without pretreatment	[PMID: 10974196]
SW-620	IC₅₀	1.13 μM Compound: PD-0173955	Inhibition of SW-620 clonogenic growth in soft agar with pretreatment Inhibition of SW-620 clonogenic growth in soft agar with pretreatment	[PMID: 10974196]

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.

Chemical Information

CAS. Nr. 260415-63-2
Appearance Solid
Molecular Weight 443.35
Formel C₂₁H₁₆Cl₂N₄OS
Color White to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

Technical University of Munich

24.01.2018.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2556 mL

11.2778 mL

22.5555 mL

5 mM

0.4511 mL

2.2556 mL

4.5111 mL

10 mM

0.2256 mL

1.1278 mL

2.2556 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Moasser MM, et al. Inhibition of Src kinases by a selective tyrosine kinase inhibitor causes mitotic arrest. Cancer Res. 1999 Dec 15;59(24):6145-52. PMID: 10626805. [Content Brief]

[2]. Martinelli G, et al. Dual tyrosine kinase inhibitors in chronic myeloid leukemia. Leukemia. 2005 Nov;19(11):1872-9. [Content Brief]

[3]. Netzer WJ, et al. Gleevec shifts APP processing from a β-cleavage to a nonamyloidogenic cleavage. Proc Natl Acad Sci U S A. 2017 Feb 7;114(6):1389-1394. [Content Brief]

[4]. Wolff NC, et al. PD166326, a novel tyrosine kinase inhibitor, has greater antileukemic activity than imatinib mesylate in a murine model of chronic myeloid leukemia. Blood. 2005 May 15;105(10):3995-4003. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

PD173955

1 Cited Publications

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PD173955

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

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Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PD173955

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PD173955

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Angiogenesis-Related Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PD173955

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PD173955 Related Classifications

HY-10395 Related Classifications