PD 0332991 HCL 哌柏西利盐酸盐；帕博西尼盐酸盐

目录号 M1806 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务

PD-0332991 HCl是一种高度选择性的，具有口服活性的CDK4/6抑制剂，无细胞试验中IC50分别为11 nM/16 nM。它对CDK1/2/5，EGFR，FGFR，PDGFR，InsR等没有抑制活性。

别名：Palbociclib HCl

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	中国库存现货
5mg	¥ 480	中国库存现货
10mg	¥ 640	中国库存现货
25mg	¥ 980	中国库存现货
50mg	¥ 1460	中国库存现货

其他规格数量报价？

质量标准及产品资料

纯度： 99.90%
COA
MSDS
H-NMR
HPLC

产品信息

生物活性

PD-0332991 HCl是一种高度选择性的，具有口服活性的CDK4/6抑制剂，无细胞试验中IC50分别为11 nM/16 nM。它对CDK1/2/5，EGFR，FGFR，PDGFR，InsR等没有抑制活性。PD 0332991对CDK4/6具有绝对选择性，对其他CDKs几乎没有抑制活性。PD 0332991作用于MDA-MB-435乳腺癌细胞，有效降低Rb在Ser780 和 Ser795位点磷酸化，IC50分别为66 nM和63 nM。PD 0332991通过抑制细胞进入S期，有效抑制细胞生长，抑制 DNA复制。PD 0332991抑制胸苷渗透进Rb阳性人类乳腺癌(如MDA-MB-435, MCF-7), 结肠癌 (H1299), 和肺癌(Colo-205) 及白血病(CRRF-CEM和K562)的DNA中，IC50值为0.04-0.17 μM。PD 0332991显著增强MDA-MB-453在G1期的百分比。PD 0332991作用于CD138⁺原发性骨髓瘤细胞，初级非转化的B细胞，MM1.S和CAG HMCLs细胞系，抑制Rb磷酸化，IC50分别为 <0.1 μM, 0.05 μM, 和 60-70 nM。PD 0332991作用于CD138⁺原发性骨髓瘤细胞和初级非转化的B细胞，诱导细胞停滞在G1期。

使用AbMole产品发表的文献

NPJ Breast Cancer. 2022 Jan;8(1):1.

Effects of neoadjuvant trastuzumab, pertuzumab and palbociclib on Ki67 in HER2 and ER-positive breast cancer
BMC Biol. 2021 May 20;19(1):108.

Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
Journal of Molecular Structure. 2014 Jan 6;Pages 209-215.

A theoretical study of the structure and protonation of Palbociclib (PD 0332991)

产品使用成果展示

	数据来源	Breast Cancer Res (2009). Figure 4. PD 0332991 HCL
	方法	Proliferation assays
	细胞系/动物模型	SUM-190 and SUM-225 cell line
	浓度	100 nM
	处理时间	48 h
	实验结果	There was no evidence of apoptosis in even the most sensitive cell lines when PD 0332991 was used as a single agent

	数据来源	Breast Cancer Res (2009). Figure 3. PD 0332991 HCL
	方法	Western blot
	细胞系/动物模型	SUM-190 and SUM-225 cell line
	浓度	100 nM
	处理时间	48 h
	实验结果	These lines did not have a significant decrease in Rb phosphorylation with 100 nM PD 0332991.

实验参考

体外实验*
细胞系	HCT116, SW480, Lovo and LS174T cells
方法	Cell proliferation and colony formation assays Cells were seeded in a 96-well plate at 2000–6000 cells/well, incubated overnight at 37°C to allow adhesion, and then treated with inhibitors for 72 hours. Cell proliferation was determined using MTS solution (Promega), and formal assessment for synergy performed per the Chou Talalay method [64, 65] using CompuSyn (ComboSyn, Inc, Paramus, NJ). For colony formation assay, cells were seeded in a 6-well plate at 8000– 80,000 cells/well, incubated overnight at 37°C to allow adhesion, and then treated with inhibitors for 2–3 weeks. Cell colonies were fixed with ice-cold methanol and stained with 1% crystal violet. The density of colonies over the plate area was quantified by ImageJ (NIH) [66]. For detection of exposed phosphatidylserine residues reflective of apoptosis, Annexin V-FITC apoptosis assay kit (BD Biosciences) was used. Cells were seeded at 500,000 cells/ well in 6-well plates, incubated overnight at 37°C to allow adhesion, and then treated with inhibitors for 72 hours. Cells were washed and stained with annexin V-FITC and propidium iodide, and flow cytometry was performed using the Gallios flow cytometer (Beckman Coulter) and analyzed with Kaluza flow analysis software (Beckman Coulter). To measure cell senescence, treated cells were stained for senescence-associated beta-galactosidase (Chemicon). Cells were seeded at 500,000 cells/well in 6-well plates, incubated overnight at 37°C to allow adhesion, and then treated with inhibitors for 72 hours. Cells were washed with PBS, fixed with glutaraldehyde and methanol, washed twice more, and then incubated overnight in the dark at 37°C under ambient atmospheric conditions with X-Gal. Subsequently, cells were washed, and 10 high-powered light microscopy images of each well were captured, and cells with blue staining were manually counted.
浓度	0~400nM
处理时间	72 h

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
动物模型	Primary human-tumor xenograft models in NU/J6-week old female mice
配制	PBS
剂量	100 mg/kg per os daily for 21 days
给药处理	oral gavage

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	483.99
分子式	C24H29N7O2.HCl
CAS号	827022-32-2
溶解性（25°C）	DMSO 4 mg/mL warmed Water 30 mg/mL
储存条件	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.0662 mL	10.3308 mL	20.6616 mL
5 mM	0.4132 mL	2.0662 mL	4.1323 mL
10 mM	0.2066 mL	1.0331 mL	2.0662 mL

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Lee MS, et al. Oncotarget. Efficacy of the combination of MEK and CDK4/6 inhibitors in vitro and in vivo in KRAS mutant colorectal cancer models.

[2] Liu F et al. Mol Cancer Ther. Cdk4/6 Inhibition Induces Epithelial-Mesenchymal Transition and Enhances Invasiveness in Pancreatic Cancer Cells.

[3] Dean JL et al. Cell Cycle. Therapeutic response to CDK4/6 inhibition in breast cancer defined by ex vivo analyses of human tumors.

[4] Flaherty KT et al. Clin Cancer Res. Phase I, dose-escalation trial of the oral cyclin-dependent kinase 4/6 inhibitor PD 0332991, administered using a 21-day schedule in patients with advanced cancer.

[5] Smith D et al. J Chromatogr B Analyt Technol Biomed Life Sci. Quantitative analysis of PD 0332991 in mouse plasma using automated micro-sample processing and microbore liquid chromatography coupled with tandem mass spectrometry.

[6] Katsumi Y et al. Biochem Biophys Res Commun. Sensitivity of malignant rhabdoid tumor cell lines to PD 0332991 is inversely correlated with p16 expression.

获取最新目录册

其他相关的CDK产品
PF-07224826 PF-07224826是一种 CDK2/4/6 抑制剂。
INCB123667 INCB123667 是一种 CDK2 抑制剂。
Senexin B Senexin B 是一种有效的，具有口服活性的 CDK8/19 抑制剂，对 CDK8 和 CDK19 的 Kd 值分别为 140 nM 和 80 nM。
Q901 Q901 是一种 CDK7 抑制剂，可用于肿瘤的相关研究。
NUV-422 NUV-422 是一种CDK2/4/6抑制剂，可用于恶性胶质瘤的相关研究。

信号通路

产品类型