Cat. No.: HY-122113

PD173952

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PD173952 is a tyrosine kinases inhibitor with IC₅₀s of 0.3, 1.7 and 6.6 nM against Lyn, Abl and Csk, respectively. PD173952 is also a potent Myt1 kinase inhibitor with a K_i of 8.1 nM. PD173952 induces apoptosis.

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Pureté: 99.58%
CAS No.: 305820-75-1
Formule: C₂₄H₂₁Cl₂N₅O₂
Masse moléculaire:482.36

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

PD173952 Chemical Structure

CAS No.: 305820-75-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]^[2]

Lyn

0.3 nM (IC₅₀)

Abl

1.7 nM (IC₅₀)

Csk

6.6 nM (IC₅₀)

Myt1

8.1 nM (Ki)

PKMYT1

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Voir tous les produits spécifiques à Isoform Bcr-Abl :

Abl
Bcr-Abl

Voir tous les produits spécifiques à Isoform Wee1 :

PKMYT1

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.245 μM Compound: PD-0173952	Inhibition of 3H-thymidine incorporation into A-431 cells Inhibition of 3H-thymidine incorporation into A-431 cells	[PMID: 10974196]
HCT-8	IC₅₀	1.26 μM Compound: PD-0173952	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	1.38 μM Compound: PD-0173952	Inhibition of HCT-8 clonogenic growth in soft agar with pretreatment Inhibition of HCT-8 clonogenic growth in soft agar with pretreatment	[PMID: 10974196]
HCT-8	IC₅₀	1.5 μM Compound: 6v	Inhibitory activity against HCT-8 human colon adenocarcinoma cells was determined. Inhibitory activity against HCT-8 human colon adenocarcinoma cells was determined.	[PMID: 10956222]
HCT-8	IC₅₀	1.53 μM Compound: PD-0173952	Inhibition of HCT-8 cell proliferation Inhibition of HCT-8 cell proliferation	[PMID: 10974196]
HT-29	IC₅₀	0.2 μM Compound: 6v	Inhibitory activity against HT-29 human colon adenocarcinoma cells was determined. Inhibitory activity against HT-29 human colon adenocarcinoma cells was determined.	[PMID: 10956222]
HT-29	IC₅₀	0.2 μM Compound: PD-0173952	Inhibition of HT-29 cell proliferation Inhibition of HT-29 cell proliferation	[PMID: 10974196]
HT-29	IC₅₀	1.21 μM Compound: PD-0173952	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	1.37 μM Compound: PD-0173952	Inhibition of HT-29 clonogenic growth in soft agar without pretreatment Inhibition of HT-29 clonogenic growth in soft agar without pretreatment	[PMID: 10974196]
NIH3T3	IC₅₀	0.17 μM Compound: PD-0173952	Inhibition of 3H-thymidine incorporation into NIH3T3 cells Inhibition of 3H-thymidine incorporation into NIH3T3 cells	[PMID: 10974196]
SW-620	IC₅₀	0.17 μM Compound: 6v	Inhibitory activity against SW-620 human colon adenocarcinoma cells was determined. Inhibitory activity against SW-620 human colon adenocarcinoma cells was determined.	[PMID: 10956222]
SW-620	IC₅₀	0.174 μM Compound: PD-0173952	Inhibition of SW-620 cell proliferation Inhibition of SW-620 cell proliferation	[PMID: 10974196]
SW-620	IC₅₀	0.47 μM Compound: PD-0173952	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	0.53 μM Compound: PD-0173952	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

PD173952 (0-1000 nM; 12 h) inhibits tyrosine phosphorylation of p210^Bcr-Abl and CrkL in K562 cells in a concentration-dependent manner^[1].
PD173952 (0.5 μM; 1-4 days) inhibits K562 cell viability^[1].
PD173952 (0.5 μM; 24 and 48 h) induces apoptosis of K562 and MEG-01 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

K562 cells
Concentration:

0, 25, 50, 100, 200, 500 and 1000 nM
Incubation Time:

12 h
Result:

Inhibited tyrosine phosphorylation of p210^Bcr-Abl and CrkL.

Cell Viability Assay^[1]

Cell Line:

K562 cells
Concentration:

0.5 μM
Incubation Time:

1-4 days
Result:

Caused cell death in a time-dependent manner.

Western Blot Analysis^[1]

Cell Line:

K562 and MEG-01 cells
Concentration:

0.5 μM
Incubation Time:

24 and 48 h
Result:

85-kDa PARP fragment was detected.

Chemical Information

CAS No. 305820-75-1
Appearance Solid
Masse moléculaire 482.36
Formule C₂₄H₂₁Cl₂N₅O₂
Color Light yellow to yellow
SMILES

O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=C(N5CCOCC5)C=C4)N=C3N1C
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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iScience

Decoding sunitinib resistance in ccRCC: Metabolic-reprogramming-induced ABAT and GABAergic system shifts. [Abstract]

2024 Jun 28;27(7):110415. PMID: 39100925

Solvant et solubilité

In Vitro:

DMSO : 16.67 mg/mL (34.56 mM; ultrasonic and warming and heat to 60°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

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0731 mL

10.3657 mL

20.7314 mL

5 mM

0.4146 mL

2.0731 mL

4.1463 mL

10 mM

0.2073 mL

1.0366 mL

2.0731 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, 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (252 KB)
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- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
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- Portuguese - PT (252 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)
Instruction de manipulation (2659 KB)

Références

[1]. Dorsey JF, et al. Interleukin-3 protects Bcr-Abl-transformed hematopoietic progenitor cells from apoptosis induced by Bcr-Abl tyrosine kinase inhibitors. Leukemia. 2002 Sep;16(9):1589-95. [Content Brief]

[2]. Wichapong K, et al. Application of docking and QM/MM-GBSA rescoring to screen for novel Myt1 kinase inhibitors. J Chem Inf Model. 2014 Mar 24;54(3):881-93. [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, 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	2.0731 mL	10.3657 mL	20.7314 mL	51.8285 mL
	5 mM	0.4146 mL	2.0731 mL	4.1463 mL	10.3657 mL
	10 mM	0.2073 mL	1.0366 mL	2.0731 mL	5.1829 mL
	15 mM	0.1382 mL	0.6910 mL	1.3821 mL	3.4552 mL
	20 mM	0.1037 mL	0.5183 mL	1.0366 mL	2.5914 mL
	25 mM	0.0829 mL	0.4146 mL	0.8293 mL	2.0731 mL
	30 mM	0.0691 mL	0.3455 mL	0.6910 mL	1.7276 mL

Keywords

PD173952

1 Cited Publications

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PD173952

Apoptosis Compound Library

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Serine/Threonine Kinase Inhibitor Library

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Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

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Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) PD173952

Voir tous les produits spécifiques à Isoform Src

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Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PD173952 Related Classifications

HY-122113 Related Classifications