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Palbociclib Isethionate

产品编号 T6240 CAS 827022-33-3

别名: Palbociclib (PD0332991) Isethionate, 帕博西尼羟乙基磺酸盐, PD 0332991 isethionate, 帕布昔利布羟乙基磺酸盐

Palbociclib Isethionate (PD 0332991 isethionate) 是一种高选择性的CDK4/6抑制剂，IC50为11 nM 和16 nM。它对一组 36 种额外的蛋白激酶没有抑制作用。

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Palbociclib Isethionate Chemical Structure

Palbociclib Isethionate, CAS 827022-33-3

规格	价格/CNY	货期
1 mg	￥ 197	现货
5 mg	￥ 452	现货
10 mg	￥ 659	现货
25 mg	￥ 987	现货
50 mg	￥ 1,330	现货
100 mg	￥ 1,930	现货
200 mg	￥ 2,380	现货
500 mg	￥ 3,950	现货
1 mL * 10 mM (in DMSO)	￥ 626	现货

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其他形式的 Palbociclib Isethionate:

选择批次

纯度: 99.85%

纯度: 99.27%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Palbociclib Isethionate (PD 0332991 isethionate) is a selective inhibitor of CDK4/6 (IC50s: 11/16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.
靶点活性	CDK4-CyclinD1:11 nM (cell free), CDK6-CyclinD2:15 nM (cell free), CDK4-CyclinD3:9 nM (cell free)
体外活性	PD 0332991 is a highly specific inhibitor of Cdk4 (IC50, 0.011 micromol/L) and Cdk6 (IC50, 0.016 micromol/L). It is a potent antiproliferative agent against retinoblastoma (Rb)-positive tumor cells in vitro, inducing an exclusive G1 arrest, with a concomitant reduction of phospho-Ser780/Ser795 on the Rb protein [1]. In all of the cell lines except KP-MRT-YM, PD 0332991 inhibited cell proliferation >50% (IC50 values 0.01 to 0.6 μM), and induced G1-phase cell cycle arrest. The sensitivity of the MRT cell lines to PD 0332991 was inversely correlated with p16 expression. KP-MRT-YM cells overexpress p16 and were resistant to the growth inhibitory effect of PD 0332991 [2]. Cell lines representing luminal estrogen receptor-positive (ER+) subtype (including those that are HER2 amplified) were most sensitive to growth inhibition by PD 0332991 while nonluminal/basal subtypes were most resistant [3].
体内活性	Oral administration of PD 0332991 to mice bearing the Colo-205 human colon carcinoma produces marked tumor regression. Therapeutic doses of PD 0332991 cause elimination of phospho-Rb and the proliferative marker Ki-67 in tumor tissue and down-regulation of genes under the transcriptional control of E2F [1].
激酶实验	CDK assays for IC50determinations and kinetic evaluation were performed in 96-well filter plates. All CDK-cyclin kinase complexes were expressed in insect cells through baculovirus infection and purified as described previously. The substrate for the assays was a fragment (amino acids 792–928) of pRb fused to GST. The total volume for each well was 0.1 ml containing a final concentration of 20 mM Tris-HCl, pH 7.4, 50 mMNaCl, 1 mM dithiothreitol, 10 mMMgCl2, 25 μM ATP (for CDK4-cyclin D1, CDK6-cyclin D2, and CDK6-cyclin D3) or 12 μM ATP (for CDK2-cyclin E, CDK2-cyclin A, and CDC2-cyclin B) containing 0.25 μCi of [γ-32P]ATP, 20 ng of enzyme, 1 μg of GST·RB-Cterm, and appropriate dilutions of inhibitor. All components except the [γ-32P]ATP were added to the wells, and the plate was placed on a plate mixer for 2 min. The reaction was then started by adding the [γ-32P]ATP, and the plate was incubated at 25?°C for 15 min. The reaction was terminated by addition of 0.1 ml of 20% trichloroacetic acid, and the plate was kept at 4?°C for at least 1 h to allow the substrate to precipitate. The wells were then washed five times with 0.2 ml of 10% trichloroacetic acid, and radioactive incorporation was determined with a β plate counter. Kinase assays for PDGFr, FGFr, EGFr, SRC, and PKC kinases were performed as described previously [4].
细胞实验	Cells were seeded at 2 × 10^4 per well in a 96-well Cytostar T plate and incubated overnight to allow cells to attach. Varying concentrations of PD 0332991 were added to the wells and incubated for 24 hours at 37°C. [14C]thymidine (0.1 μCi) was added to each well and incorporation of the radiolabel was allowed to proceed for 72 hours. Incorporated radioactivity was determined with a β plate counter [1].
动物实验	Mice (18–22 g) were randomized and then implanted s.c. with tumor fragments (～30 mg) into the region of the right axilla. Treatment was initiated when tumors reached 100 to 150 mg. PD 0332991 was given according to the schedule and dose indicated in the table and figure legends by gavage as a solution in sodium lactate buffer (50 mmol/L, pH 4.0) based on mean group body weight. In all experiments, there were 12 mice in the control group and 8 mice each in the treated groups. Additional details for each experiment are given in the table legends [1].

别名	Palbociclib (PD0332991) Isethionate, 帕博西尼羟乙基磺酸盐, PD 0332991 isethionate, 帕布昔利布羟乙基磺酸盐
分子量	573.66
分子式	C24H29N7O2·C2H6O4S
CAS No.	827022-33-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 5.7 mg/mL (10 mM)

H2O: 57.4 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / H2O	1 mM	1.7432 mL	8.716 mL	17.4319 mL	43.5798 mL
	5 mM	0.3486 mL	1.7432 mL	3.4864 mL	8.716 mL
	10 mM	0.1743 mL	0.8716 mL	1.7432 mL	4.358 mL
H2O	20 mM	0.0872 mL	0.4358 mL	0.8716 mL	2.179 mL
	50 mM	0.0349 mL	0.1743 mL	0.3486 mL	0.8716 mL
	100 mM	0.0174 mL	0.0872 mL	0.1743 mL	0.4358 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. 2. Katsumi Y, et al. Sensitivity of malignant rhabdoid tumor cell lines to PD 0332991 is inversely correlated with p16 expression. Biochem Biophys Res Commun, 2011, 413(1), 62-68. 3. Finn RS, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11(5):R77. 4. Fry DW, et al. Cell cycle and biochemical effects of PD 0183812. A potent inhibitor of the cyclin D-dependent kinases CDK4 and CDK6. J Biol Chem. 2001 May 18;276(20):16617-23.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Palbociclib Isethionate 827022-33-3 Cell Cycle/Checkpoint CDK Inhibitor hepatocellular carcinoma HER2 inhibit Palbociclib Breast cancer PD0332991 PD 0332991 PD-0332991 cell cycle Cyclin dependent kinase Palbociclib (PD0332991) Isethionate 帕博西尼羟乙基磺酸盐 PD 0332991 isethionate HCC 帕布昔利布羟乙基磺酸盐 estrogen receptor inhibitor

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Palbociclib Isethionate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords