PD166326

Name: PD166326
Brand: MedChemExpress
SKU: HY-118144
Rating: 4.5 (0 reviews)

Cat. No.: HY-118144 Purity: 99.99%: Data Sheet
COA

SDS
Handling Instructions
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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.

PD166326 Chemical Structure

CAS No. : 185039-91-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Lck Fyn Blk Fgr Hck Lyn Yes Csk SRC-3

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Abl Bcr-Abl

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Abl

8 nM (IC₅₀)

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.

Molecular Weight

427.28

Formula

C₂₁H₁₆Cl₂N₄O₂

CAS No.

185039-91-2

Appearance

Solid

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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, 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.99%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (247 KB) HNMR (231 KB) RP-HPLC (261 KB) MS (72 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]

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

PD166326 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PD166326

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