PD173955
Based on 1 publication(s) in Google Scholar
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.05%
- CAS No.: 260415-63-2
- Formule: C21H16Cl2N4OS
- Masse moléculaire:443.35
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PD173955
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Activité biologique
IC50: 22 nM (Src)[1].
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Cell Line
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Type | Value | Description | References |
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| BaF3 | IC50 |
>30 μM
Compound: PD-17395
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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
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[PMID: 16970400] |
| BaF3 | IC50 |
>30 μM
Compound: PD-17395
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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
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[PMID: 16970400] |
| BaF3 | IC50 |
1.8 μM
Compound: PD-17395
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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
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[PMID: 16970400] |
| BaF3 | IC50 |
2 μM
Compound: PD-17395
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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
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[PMID: 16970400] |
| BaF3 | IC50 |
2.5 μM
Compound: PD-17395
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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
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[PMID: 16970400] |
| BaF3 | IC50 |
3 μM
Compound: PD-17395
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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
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[PMID: 16970400] |
| HCT-8 | IC50 |
1.131 μM
Compound: PD-0173955
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Inhibition of HCT-8 cell proliferation
Inhibition of HCT-8 cell proliferation
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[PMID: 10974196] |
| HCT-8 | IC50 |
1.3 μM
Compound: PD-0173955
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Inhibition of HCT-8 clonogenic growth in soft agar without pretreatment
Inhibition of HCT-8 clonogenic growth in soft agar without pretreatment
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[PMID: 10974196] |
| HCT-8 | IC50 |
2.52 μM
Compound: PD-0173955
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Inhibition of HCT-8 clonogenic growth in soft agar with pretreatment
Inhibition of HCT-8 clonogenic growth in soft agar with pretreatment
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[PMID: 10974196] |
| HT-29 | IC50 |
0.81 μM
Compound: PD-0173955
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Inhibition of HT-29 cell proliferation
Inhibition of HT-29 cell proliferation
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[PMID: 10974196] |
| HT-29 | IC50 |
1.21 μM
Compound: PD-0173955
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Inhibition of HT-29 clonogenic growth in soft agar with pretreatment
Inhibition of HT-29 clonogenic growth in soft agar with pretreatment
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[PMID: 10974196] |
| HT-29 | IC50 |
1.29 μM
Compound: PD-0173955
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Inhibition of HT-29 clonogenic growth in soft agar without pretreatment
Inhibition of HT-29 clonogenic growth in soft agar without pretreatment
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[PMID: 10974196] |
| SW-620 | IC50 |
0.924 μM
Compound: PD-0173955
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Inhibition of SW-620 cell proliferation
Inhibition of SW-620 cell proliferation
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[PMID: 10974196] |
| SW-620 | IC50 |
0.98 μM
Compound: PD-0173955
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Inhibition of SW-620 clonogenic growth in soft agar without pretreatment
Inhibition of SW-620 clonogenic growth in soft agar without pretreatment
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[PMID: 10974196] |
| SW-620 | IC50 |
1.13 μM
Compound: PD-0173955
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Inhibition of SW-620 clonogenic growth in soft agar with pretreatment
Inhibition of SW-620 clonogenic growth in soft agar with pretreatment
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[PMID: 10974196] |
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.
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Cell Line:MDA-MB-468
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Concentration:5 μM
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Incubation Time:24 h
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Result:Blocked 95% of the cells in the G2-M phase.
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Cell Line:MO7e, R10(-)(a cell line derived from P210-MO7e)
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Concentration:0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
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Incubation Time:48 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c mice model of chronic myeloid leukemia (CML)[4]
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Dosage:50 mg/kg
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Administration:Oral gavage (p.o.), Twice daily for 4 days
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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
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CAS No. 260415-63-2
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Appearance Solid
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Masse moléculaire 443.35
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Formule C21H16Cl2N4OS
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Color White to yellow
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SMILES
O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=CC(SC)=C4)N=C3N1C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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
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Most Recent
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (277 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[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]
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 |
PD173955 Related Classifications
HY-10395 Related Classifications
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