製品番号: HY-122113

PD173952

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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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純度: 99.58%
CAS 番号: 305820-75-1
分子式: C₂₄H₂₁Cl₂N₅O₂
分子量:482.36

保管条件:

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

PD173952 構造式

CAS 番号: 305820-75-1

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価格（税別）

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数量

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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

Src アイソフォーム固有の製品をすべて表示 :

Bcr-Abl アイソフォーム固有の製品をすべて表示 :

Abl
Bcr-Abl

Wee1 アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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.

化学情報

CAS 番号 305820-75-1
性状 Solid
分子量 482.36
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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

View the Complete Stock Solution Preparation Table

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Cytoskeleton Compound Library

Anti-Alzheimer's Disease 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

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

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

MedChemExpress（MCE）の使用を引用している文献 PD173952

Src アイソフォーム固有の製品をすべて表示

Bcr-Abl アイソフォーム固有の製品をすべて表示

Wee1 アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

PD173952 関連分類

HY-122113 関連分類