Art. -Nr.: HY-103274

PD180970

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PD180970 is a highly potent and ATP-competitive p210^Bcr-Abl kinase inhibitor, with an IC₅₀ of 5 nM for inhibiting the autophosphorylation of p210^Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC₅₀s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research.

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Reinheit: 99.27%
CAS. Nr.: 287204-45-9
Formel: C₂₁H₁₅Cl₂FN₄O
Molecular Weight:429.27

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PD180970 Chemical Structure

CAS. Nr.: 287204-45-9

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]

Bcr-Abl

5 nM (IC₅₀, p210^Bcr-Abl kinase)

Src

0.8 nM (IC₅₀)

KIT

50 nM (IC₅₀)

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen :

Abl
Bcr-Abl

Alle Src Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.215 μM Compound: PD-0180970	Inhibition of 3H-thymidine incorporation into A-431 cells Inhibition of 3H-thymidine incorporation into A-431 cells	[PMID: 10974196]
HCT-8	IC₅₀	0.26 μM Compound: PD-0180970	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	0.45 μM Compound: PD-0180970	Inhibition of HCT-8 cell proliferation Inhibition of HCT-8 cell proliferation	[PMID: 10974196]
HCT-8	IC₅₀	0.61 μM Compound: PD-0180970	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	0.461 μM Compound: PD-0180970	Inhibition of HT-29 cell proliferation Inhibition of HT-29 cell proliferation	[PMID: 10974196]
HT-29	IC₅₀	0.464 μM Compound: PD-0180970	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	1.52 μM Compound: PD-0180970	Inhibition of HT-29 clonogenic growth in soft agar without pretreatment Inhibition of HT-29 clonogenic growth in soft agar without pretreatment	[PMID: 10974196]
K562	IC₅₀	5 nM Compound: 2, PD180970	Inhibition of STAT5 DNA binding activity in human K562 cells after 24 hrs by electrophoretic mobility shift assay Inhibition of STAT5 DNA binding activity in human K562 cells after 24 hrs by electrophoretic mobility shift assay	10.1039/C1MD00175B
NIH3T3	IC₅₀	0.17 μM Compound: PD-0180970	Inhibition of 3H-thymidine incorporation into NIH3T3 cells Inhibition of 3H-thymidine incorporation into NIH3T3 cells	[PMID: 10974196]
SW-620	IC₅₀	0.285 μM Compound: PD-0180970	Inhibition of SW-620 cell proliferation Inhibition of SW-620 cell proliferation	[PMID: 10974196]

In Vitro

PD180970 (0.5 μM; 24-96 hours) treatment causes cell death K562 cells^[1].
PD180970 (0.5 μM; 24-48 hours) treatment induces apoptosis of K562 cells. The result shows increase in annexin V-PI double-positive cells^[1].
PD180970 inhibits tyrosine phosphorylation of p210Bcr-Abl, Gab2, and CrkL in K562 cells with IC50 values of 170 nM, 80 nM, and 80 nM, respectively. In vitro, PD180970 potently inhibits autophosphorylation of p210^Bcr-Abl (IC₅₀ of 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC₅₀ of 2.2 nM)^[1].
The blocking Bcr-Abl kinase activity using PD180970 in the human K562 CML cell line resulted in inhibition of Stat5 DNA-binding activity with an IC₅₀ of 5 nM^[2].

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

Cell Viability Assay^[1]

Cell Line:

K562 cells
Concentration:

0.5 μM
Incubation Time:

24 hours, 48 hours, 72 hours, 96 hours
Result:

Resulted in cell death.

Apoptosis Analysis^[1]

Cell Line:

K562 cells
Concentration:

0.5 μM
Incubation Time:

24 hours, 48 hours
Result:

Increased annexin V-positive/PI-negative cells.

In Vivo

PD180970 (5 mg/kg; intraperitonial injection; daily; for 7 days) mitigates MPTP-induced neuronal loss in mice. PD180970 has the neuroprotective ability in a preclinical mouse model of Parkinson's disease (PD)^[4].

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

Animal Model:

Male C57BL/6J mice (3-4 months old) injected with MPTP^[4]
Dosage:

5 mg/kg
Administration:

Intraperitonial injection; daily; for 7 days
Result:

Decreased number of activated microglia on activation by MPTP in mice brains. And showed significant reduction in intensity of Iba1 expression in activated microglia.

Chemical Information

CAS. Nr. 287204-45-9
Appearance Solid
Molecular Weight 429.27
Formel C₂₁H₁₅Cl₂FN₄O
Color Light yellow to yellow
SMILES

O=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=C(F)C(C)=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	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (232.95 mM; Need ultrasonic; 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

2.3295 mL

11.6477 mL

23.2954 mL

5 mM

0.4659 mL

2.3295 mL

4.6591 mL

10 mM

0.2330 mL

1.1648 mL

2.3295 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.

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 90% Corn Oil

Solubility: ≥ 1.25 mg/mL (2.91 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 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 (278 KB)
SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 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]. J F Dorsey, et al. The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210Bcr-Abl tyrosine kinase and induces apoptosis of K562 leukemic cells. Cancer Res. 2000 Jun 15;60(12):3127-31. [Content Brief]

[2]. Mei Huang, et al. Inhibition of Bcr-Abl kinase activity by PD180970 blocks constitutive activation of Stat5 and growth of CML cells. Oncogene. 2002 Dec 12;21(57):8804-16. [Content Brief]

[3]. Amie S Corbin, et al. Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970. Blood. 2004 Dec 1;104(12):3754-7. [Content Brief]

[4]. Suresh Sn, et al. Small molecule modulator of aggrephagy regulates neuroinflammation to curb pathogenesis of neurodegeneration. EBioMedicine. 2019 Dec;50:260-273. [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	2.3295 mL	11.6477 mL	23.2954 mL	58.2384 mL
	5 mM	0.4659 mL	2.3295 mL	4.6591 mL	11.6477 mL
	10 mM	0.2330 mL	1.1648 mL	2.3295 mL	5.8238 mL
	15 mM	0.1553 mL	0.7765 mL	1.5530 mL	3.8826 mL
	20 mM	0.1165 mL	0.5824 mL	1.1648 mL	2.9119 mL
	25 mM	0.0932 mL	0.4659 mL	0.9318 mL	2.3295 mL
	30 mM	0.0777 mL	0.3883 mL	0.7765 mL	1.9413 mL
	40 mM	0.0582 mL	0.2912 mL	0.5824 mL	1.4560 mL
	50 mM	0.0466 mL	0.2330 mL	0.4659 mL	1.1648 mL
	60 mM	0.0388 mL	0.1941 mL	0.3883 mL	0.9706 mL
	80 mM	0.0291 mL	0.1456 mL	0.2912 mL	0.7280 mL
	100 mM	0.0233 mL	0.1165 mL	0.2330 mL	0.5824 mL

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PD180970

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

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Multi-Target Compound Library

Bioactive Compound Library Max

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Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PD180970 Related Classifications

HY-103274 Related Classifications