Cat. No.: HY-118144

PD166326

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PD166326 is an orally active tyrosine kinase inhibitor with a IC₅₀ of 8 nM against abl tyrosine kinase and a IC₅₀ of 6 nM against src tyrosine kinase. PD166326 blocks Bcr/Abl kinase activity. PD166326 inhibits Bcr/Abl-dependent proliferation and cell cycle progression. PD166326 reduces peripheral blood granulocytosis, alleviates splenomegaly and prolongs survival in a mouse model of chronic myeloid leukemia. PD166326 can be used in research related to chronic myeloid leukemia.

For research use only. We do not sell to patients.

Purity: 99.99%
CAS No.: 185039-91-2
Formula: C₂₁H₁₆Cl₂N₄O₂
Molecular Weight:427.28

Storage:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

PD166326 Chemical Structure

CAS No.: 185039-91-2

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Abl

8 nM (IC₅₀)

All Src Isoforms :

All Bcr-Abl Isoforms :

Abl
Bcr-Abl

All p38 MAPK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-8	IC₅₀	<5 μM Compound: PD-0166326	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	<5 μM Compound: PD-0166326	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	1.11 μM Compound: PD-0166326	Inhibition of HCT-8 cell proliferation Inhibition of HCT-8 cell proliferation	[PMID: 10974196]
HT-29	IC₅₀	0.526 μM Compound: PD-0166326	Inhibition of HT-29 cell proliferation Inhibition of HT-29 cell proliferation	[PMID: 10974196]
HT-29	IC₅₀	10.3 μM Compound: PD-0166326	Inhibition of HT-29 clonogenic growth in soft agar without pretreatment Inhibition of HT-29 clonogenic growth in soft agar without pretreatment	[PMID: 10974196]
HT-29	IC₅₀	7.96 μM Compound: PD-0166326	Inhibition of HT-29 clonogenic growth in soft agar with pretreatment Inhibition of HT-29 clonogenic growth in soft agar with pretreatment	[PMID: 10974196]
Jurkat	IC₅₀	2100 nM Compound: 1, PD-166326	Cytotoxicity against Philadelphia chromosome negative human Jurkat cells by Alamar Blue fluorescent assay Cytotoxicity against Philadelphia chromosome negative human Jurkat cells by Alamar Blue fluorescent assay	[PMID: 19889540]
K562	IC₅₀	<10 nM Compound: 1, PD-166326	Cytotoxicity against Philadelphia chromosome positive human K562 cells by Alamar Blue fluorescent assay Cytotoxicity against Philadelphia chromosome positive human K562 cells by Alamar Blue fluorescent assay	[PMID: 19889540]
KU812 cell line	IC₅₀	<10 nM Compound: 1, PD-166326	Cytotoxicity against Philadelphia chromosome positive human KU812 cells by Alamar Blue fluorescent assay Cytotoxicity against Philadelphia chromosome positive human KU812 cells by Alamar Blue fluorescent assay	[PMID: 19889540]
Macrophage	CC₅₀	5 μM Compound: 66; PD 166326	Cytotoxicity against macrophage (unknown origin) cells Cytotoxicity against macrophage (unknown origin) cells	[PMID: 33539089]
MEG-01	IC₅₀	<10 nM Compound: 1, PD-166326	Cytotoxicity against Philadelphia chromosome positive human MEG01 cells by Alamar Blue fluorescent assay Cytotoxicity against Philadelphia chromosome positive human MEG01 cells by Alamar Blue fluorescent assay	[PMID: 19889540]
SW-620	IC₅₀	<5 μM Compound: PD-0166326	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	1.8 μM Compound: PD-0166326	Inhibition of SW-620 cell proliferation Inhibition of SW-620 cell proliferation	[PMID: 10974196]

In Vitro

PD166326 (0.1-2.5 nM; 48 h) potently inhibits Bcr/Abl-dependent proliferation of R10(-) cells, with an IC₅₀ of 0.2 nM^[1].
PD166326 (5-50 nM; 48 h) inhibits stem cell factor-dependent proliferation of parental MO7E cells, with an IC₅₀ of 12 nM^[1].
PD166326 (10 min; 30°C) potently inhibits purified recombinant c-abl tyrosine kinase in vitro with an IC₅₀ of 8 nM^[2].
PD166326 potently inhibits purified recombinant c-src tyrosine kinase in vitro with an IC₅₀ of 6 nM^[2].
PD166326 (4-7 days) potently inhibits the growth of K562 Bcr-abl-positive cells with an IC₅₀ of 0.3 nM^[2].
PD166326 (4-7 days) potently inhibits the growth of BaF3 p210Bcr-abl Bcr-abl-positive cells with an IC₅₀ of 6.0 nM^[2].

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

Cell Proliferation Assay^[1]

Cell Line:

parental MO7E cells (stem cell factor-dependent)
Concentration:

5 nM, 10 nM, 50 nM
Incubation Time:

48 h
Result:

Inhibited stem cell factor-dependent proliferation of parental MO7E cells with an IC₅₀ of 12 nM.
Inhibited proliferation at 5 to 10 nM.
Completely suppressed growth at 50 nM.

Western Blot Analysis^[2]

Cell Line:

K562 cells
Concentration:

0.05-5 nM
Incubation Time:

24 h
Result:

Inhibited MAPK phosphorylation in parallel with reduced Bcr-abl autophosphorylation.

In Vivo

PD166326 (50 mg/kg; p.o.; twice a day) provides better control of the murine CML-like illness than Imatinib
mesylate (HY-50946)^[1].

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

Animal Model:

Balb/c mice^[1]
Dosage:

50 mg/kg
Administration:

p.o.; twice a day
Result:

Ensured 100% of treated mice survived 3 to 4 weeks of treatment with no clinical signs of toxicity.
Reduced median spleen weight to 78 mg, over 8-fold less than placebo-treated animals (P < .001); two thirds of treated mice showed complete resolution of splenomegaly (spleen weights in the normal 50-100 mg range).
Lowered median peripheral white blood cell count to 15.0 × 10^9/L, almost 10-fold lower than placebo-treated animals (P < .01); 70% of treated mice achieved a WBC count less than 20.0 × 10^9/L.
Induced a marked reduction in constitutive tyrosine phosphorylation of leukemia-cell proteins, including an average phosphorylated Crk-L (p-Crk-L)/Crk-L ratio of 0.23 and a marked reduction in constitutive Lyn kinase activation, while ERK1/2 activation remained similar to placebo-treated mice.

Chemical Information

CAS No. 185039-91-2
Appearance Solid
Molecular Weight 427.28
Formula C₂₁H₁₆Cl₂N₄O₂
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (234.04 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

2.3404 mL

11.7019 mL

23.4039 mL

5 mM

0.4681 mL

2.3404 mL

4.6808 mL

10 mM

0.2340 mL

1.1702 mL

2.3404 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 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)
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)

References

[1]. 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;105(10):3995-4003. [Content Brief]

[2]. Huron DR, et al. A novel pyridopyrimidine inhibitor of abl kinase is a picomolar inhibitor of Bcr-abl-driven K562 cells and is effective against STI571-resistant Bcr-abl mutants. Clin Cancer Res. 2003 Apr;9(4):1267-73. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3404 mL	11.7019 mL	23.4039 mL	58.5096 mL
	5 mM	0.4681 mL	2.3404 mL	4.6808 mL	11.7019 mL
	10 mM	0.2340 mL	1.1702 mL	2.3404 mL	5.8510 mL
	15 mM	0.1560 mL	0.7801 mL	1.5603 mL	3.9006 mL
	20 mM	0.1170 mL	0.5851 mL	1.1702 mL	2.9255 mL
	25 mM	0.0936 mL	0.4681 mL	0.9362 mL	2.3404 mL
	30 mM	0.0780 mL	0.3901 mL	0.7801 mL	1.9503 mL
	40 mM	0.0585 mL	0.2925 mL	0.5851 mL	1.4627 mL
	50 mM	0.0468 mL	0.2340 mL	0.4681 mL	1.1702 mL
	60 mM	0.0390 mL	0.1950 mL	0.3901 mL	0.9752 mL
	80 mM	0.0293 mL	0.1463 mL	0.2925 mL	0.7314 mL
	100 mM	0.0234 mL	0.1170 mL	0.2340 mL	0.5851 mL

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PD166326

Bioactive Compound Library Max

Bioactive Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Serine/Threonine Kinase Inhibitor Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

MCE Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

All Src Isoforms

All Bcr-Abl Isoforms

All p38 MAPK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PD166326 Related Classifications

HY-118144 Related Classifications