PD 166326 - CAS:185039-91-2

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PD 166326

目录号 : KCM12172 CAS No. : 185039-91-2 纯度 : ≥95%

Data Sheet 产品使用指南

PD 166326 is a pyridopyrimidine-type inhibitor of receptor tyrosine kinases that inhibits c-abl (IC = 8 nM) and Bcr/Abl-dependent cell growth (IC = 0.4 nM). In addition to targeting a select group of receptor tyrosine kinases, PD 166326 also potently inhibits c-src (IC = 6 nM). Orally administered PD 166326 is well tolerated and effectively blocks Bcr/Abl kinase activity in vivo. Moreover, PD 166326 affects a distinct set of kinases from those targeted by imatinib mesylate (STI571) and can reduce the growth of some imatinib-resistant cells both in vitro and in vivo in animal models of chronic myelogenous leukemia.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock

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生物活性

PD 166326 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.

IC₅₀&Target

Abl

8 nM (IC₅₀)

体外研究

PD 166326 (0.1-2.5 nM; 48 h) can effectively inhibit Bcr/Abl dependent proliferation in R10 (-) cells, with an IC₅₀ of 0.2 nM.
PD 166326 (5-50 nM; 48 h) can inhibit the proliferation of parental MO7E cells dependent on stem cell factors, with an IC₅₀ of 12 nM.
PD 166326 can effectively inhibit purified recombinant c-bl tyrosine kinase in vitro, with an IC₅₀ of 8 nM.
PD 166326 can effectively inhibit purified recombinant c-src tyrosine kinase in vitro, with an IC₅₀ of 6 nM.
PD 166326 can effectively inhibit the proliferation of K562 Bcr bl positive cells, with an IC₅₀ of 0.3 nM.
PD 166326 can effectively inhibit the proliferation of BaF3 p210Bcr bl Bcr bl positive cells, with an IC₅₀ of 6.0 nM.

Cell Proliferation Assay

Cell Line:	parental MO7E cells (stem cell factor-dependent)
Concentration:	5 nM, 10 nM, 50 nM
Incubation Time:	48 hours
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

Cell Line:	K562 cells
Concentration:	0.05-5 nM
Incubation Time:	24 hours
Result:	Inhibited MAPK phosphorylation in parallel with reduced Bcr-abl autophosphorylation.

体内研究

PD 166326 (50 mg/kg; oral administration; The control effect of twice daily treatment on chronic myeloid leukemia (CML) in mice is superior to that of imatinib mesylate.

Animal Model:	Balb/c mice
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.

分子式

C₂₁H₁₆Cl₂N₄O₂

分子量

427.28

CAS号

185039-91-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°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)

溶解性数据

In Vitro:

DMSO: 100 mg/mL (234.04 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

纯度： ≥95%

Data Sheet

产品使用指南

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.

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器