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帕博西尼

印度帕博西尼

资料发布时间:2018-10-30 14:50:00 最后更新时间:2020-03-27 09:59:08

【药品简介】 帕博西尼是一种细胞周期蛋白依赖性激酶抑制剂(CDK)4和6的抑制剂。周期蛋白D1和CDK4/6是导致细胞增殖的信号。对雌激素受体阳性乳癌细胞株,帕博西尼通过阻断细胞从细胞周期G1进入S期的进展减低细胞增殖。用帕博西尼和抗雌激素联合处理雌激素受体阳性乳癌细胞株,可阻止癌细胞生长和增殖,加快癌细胞衰老。帕博西尼和来曲唑联合应用对肿瘤生长也有抑制作用。

【适应症状】 帕博西尼,帕博西尼与来曲唑治疗绝经后妇女的雌激素受体(ER)阳性,人表皮生长因子受体2(HER2)阴性晚期乳腺癌,作为初始内分泌为基础的治疗对于其转移性疾病治疗中的激酶抑制剂。

【 药品别名 】 帕博西尼 Palbociclib

印度帕博西尼(帕博西尼 Palbociclib)价格,正品图片,治疗乳腺癌药物, 购买帕博西尼请到印度药房官方网站进行购买 【印度药房大全目录】

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【印度帕博西尼说明书,怎么吃?】

【用法用量】
 
起始剂量:帕博西尼125mg,帕博西尼每天一次与食物一起服用21天,帕博西尼随后7天停止治疗。
 
帕博西尼中断给药和(或)帕博西尼减量是基于个人的帕博西尼安全性和帕博西尼耐受性建议。
 
 
【不良反应】
 
帕博西尼最常见的不良反应(发生率≥10%)为白细胞减少,白细胞减少,乏力,贫血,上呼吸道感染,恶心,口腔炎,脱发,腹泻,血小板减少症,食欲下降,呕吐,无力,周围神经病变,和鼻出血。
 
 
【注意事项】
 
1) 血液系统:白细胞减少。监测全血细胞计数前两个周期的开始帕博西尼疗法中,并在每个周期的开始之前,以及在第14天,并作为临床指征。
 
2)感染:用于监控的症状和体征,并扣留帕博西尼剂量适当。
 
3)胚胎胎儿毒性:帕博西尼可引起胎儿造成伤害。提醒帕博西尼潜在风险的患者胎儿,并使用有效的避孕措施。
帕博西尼

Palbociclib uses

It is also used to treat patients with certain types of breast cancer (estrogen receptor-positive, human epidermal growth factor receptor 2-negative) which have spread to other organs. It is given together with hormonal anticancer therapies.

How palbociclib works

Palbociclib is an anti-cancer medication. Cyclin dependent kinase 4 and 6 (chemical messengers) are downstream of signaling pathways which lead to the proliferation of cells. This medicine works by inhibiting cyclin dependent kinase 4 and 6, thus arrests the cancer cell cycle (cell growing process). It also targets the estrogen (hormone) receptor-positive breast cancer cells by disrupting the cell cycle.

Common side effects of palbociclib

Fatigue, Hair loss, Rash, Vomiting, Diarrhea, Nausea, Decreased appetite, Infection, Increased white blood cell count, Stomatitis (Inflammation of the mouth), Anemia (low number of red blood cells), Weakness, Fever

Palbociclib

生物活性

产品描述

Palbociclib is an orally available cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclib selectively inhibits cyclin-dependent kinase 4 (CDK4) and 6 (CDK6), thereby inhibiting retinoblastoma (Rb) protein phosphorylation early in the G1 phase leading to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation.

靶点活性

CDK4,11nM

CDK6,16nM

体外活性

The IC50 of Palbociclib (PD 0332991) for reduction of retinoblastoma (Rb) phosphorylation at Ser780 in MDA-MB-435 breast carcinoma cells is 66 nM. Palbociclib is equally effective at reducing Rb phosphorylation at Ser795 in this tumor with an IC50 of 63 nM, and similar effects on both Ser780 and Ser795 phosphorylation are obtained in the Colo-205 colon carcinoma[1]. The MP-MRT-AN (AN), KP-MRT-RY (RY), G401, and KP-MRT-NS (NS) cell lines are effectively inhibited by Palbociclib (PD) in a concentration-dependent manner in a WST-8 assay. The IC50s are 0.01 µM, 0.01 µM, 0.06 µM, and 0.6 µM, respectively. In contrast, the KP-MRT-YM (YM) cell line is resistant to Palbociclib (IC50>10 µM). The flow cytometry results show that Palbociclib at concentrations between 0 to 1.0 µM induces G1 arrest in the AN, RY, G401 and NS cell lines in a concentration-dependent manner, but has no effect on YM cells. The BrdU incorporation results are consistent with the WST-8 and flow cytometry results: PD reduces BrdU incorporation (indicating G1 arrest) in the AN, RY, G401 and NS cell lines, but not in the YM cell line. Palbociclib, even at a concentration of 0.05 µM, significantly reduces BrdU incorporation in the AN, RY, and G401 cell lines (p<0.05)[2].

体内活性

Palbociclib (PD 0332991) exhibits significant antitumor efficacy against multiple human tumor xenograft models. In mice bearing Colo-205 colon carcinoma xenografts (p16 deleted), daily p.o. dosing for 14 days with Palbociclib (150 or 75 mg/kg) produces rapid tumor regressions and a corresponding tumor growth delay of ~50 days with >1 log of tumor cell kill at the highest dose tested. At 37.5 mg/kg, the tumor slowly regressed during treatment. Even at doses as low as 12.5 mg/kg, a 13-day growth delay is obtained indicating a 90% inhibition of tumor growth rate. Likewise, robust antitumor activity is seen in the MDA-MB-435 breast carcinoma (p16 deleted) where complete tumor stasis is apparent at 150 mg/kg and some cell kill is evident at the highest dose[1].

激酶实验

CDK assays are performed in 96-well filter plates. All CDK-cyclin kinase complexes are expressed in insect cells through baculovirus infection and purified. The substrate for the assays is a fragment (amino acids 792-928) of pRb fused to GST (GST·RB-Cterm). The total volume in each well is 0.1 mL containing a final concentration of 20 mM Tris-HCl, pH 7.4, 50 mM NaCl, 1 mM dithiothreitol, 10 mM MgCl2, 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 Palbociclib (0.001-0.1μM). All components except the [γ-32P]ATP are added to the wells, and the plate is placed on a plate mixer for 2 min. The reaction is started by adding the [γ-32P]ATP and the plate is incubated at 25°C for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid and the plate is kept at 4°C for at least 1 hour to allow the substrate to precipitate. The wells are then washed 5 times with 0.2 mL of 10% trichloroacetic acid and radioactive incorporation is determined with a β plate counter.

细胞实验

Palbociclib (PD) is prepared in DMSO and stored (−80°C), and then diluted with appropriate media before use[1]. MRT cell lines, G401, MP-MRT-AN (AN), KP-MRT-RY (RY), KP-MRT-NS (NS), and KP-MRT-YM (YM) cell lines are seeded in normal growth medium into 96-well cell plates. After 24 h, the culture medium is replaced with culture medium containing Palbociclib (0.05 or 1 µM) or DMSO. Cells are cultured and treated in triplicate. Cell proliferation is determined 8 days after the treatment by WST-8 assay using a Cell Counting Kit-8.

动物实验

动物模型:mice

化学信息

分子量

447.54

分子式

C24H29N7O2

CAS

571190-30-2

溶解度

DMSO: >10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

  1 mg 5 mg 10 mg
1 mM 2.234 ml 11.172 ml 22.344 ml
5 mM 0.447 ml 2.234 ml 4.469 ml
10 mM 0.223 ml 1.117 ml 2.234 ml
50 mM 0.045 ml 0.223 ml 0.447 ml

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 03321991 is inversely correlated with p16 expression. Biochem Biophys Res Commun, 2011, 413(1), 62-68.
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