PD 0332991 HCl
英文名称: PD 0332991 HCl
型号:null    产品货号: ICC1102-0005MG
价格:请致电:010-57128832,18610462672
品牌: gene operation

 ICC1102-PD 0332991 HCl

PD 0332991 HCl>99%

【英文同义名】Palbociclib hydrochloride, PD 0332991 HCl, Palbociclib HCl, Tube006

订购信息:(原装进口,常备现货)

 

产品名称

产品货号

目录价(元)

Gene Operation

PD 0332991 HCl

ICC1102-0005MG

5 mg

¥869.00

ICC1102-0010MG

10 mg

¥1,299.00

ICC1102-0025MG

25 mg

¥3,299.00

产品描述

PD 0332991 HCl PD 0332991的盐酸盐形式。PD 0332991是一种具有选择性CDK4CDK6抑制剂,IC50分别为11nM 16nMPD 0332991对包括CDK1/ 2/5EGFRFGFRPDGFR和胰岛素受体等36种蛋白激酶没有活性。体外实验中PD 0332991能抑制视网膜母细胞瘤阳性肿瘤细胞的生长,包括停留细胞周期到G1期,降低Rb蛋白Ser780/ Ser795的***酸化。PD 0332991能消减Colo-205人结肠癌移植小鼠移植瘤 [1]PD 0332991也能在体内外抑制5T33MM细胞Rb蛋白Cdk4/6特异性***酸化及细胞周期G(1) [2]PD 0332991治疗原发性乳腺癌能够使Ki67降低4倍以上 [3]PD 0332991处理能阻断大肠癌细胞RB蛋***酸化并抑制细胞生长 [4]PD 0332991已进入临床三期实验用于治疗乳腺肿瘤。

靶点

靶点

CDK4/CyclinD3

CDK4/CyclinD1

CDK6/CyclinD2

IC50(半数有效浓度)

9 nM [1]

11 nM [1]

15 nM [1]

化学特性

Cas No.: 827022-32-2

分子量.: 483.99

分子式: C24H29N7O2.HCl

纯度: >99%

同义名: Palbociclib hydrochloride, PD 0332991 HCl, Palbociclib HCl, Tube006

化学名:
 6-acetyl-8-cyclopentyl-5-methyl-2-(5-(piperazin-1-yl)pyridin-2-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride

外观: 黄色粉末

溶解: 溶于水 (up to 50 mM)

保存::3 -20℃粉状

储存液配制

储存液 (1 ml H2O体系)

1 mM

5 mM

10 mM

25 mM

50 mM

100 mM

质量(mg)

0.4840

2.4200

4.8399

12.0998

24.1995

0.4840

结构式

                             

使用浓度(仅作参考)

PD 0332991 HCl具体使用浓度请参考相关文献,并根据自身实验条件(如实验目的,细胞种类,培养特性等)进行摸索和优化。

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. 3(11):1427-38(2004).

[2] Menu E, et al. A novel therapeutic combination using PD 0332991 and bortezomib:  study in the 5T33MM myeloma model. Cancer Res. 68(14):5519-23(2008).

[3] Witkiewicz AK, et al. CDK4/6 inhibition provides a potent adjunct to Her2-targeted therapies in preclinical breast cancer models. Genes Cancer. 5(7-8):261-72(2014).

[4] Li C, Qi L, et al. PD-0332991 induces G1 arrest of colorectal carcinoma cells through inhibition of the cyclin-dependent kinase-6 and retinoblastoma protein axis. Oncol Lett. 7(5):1673-1678(2014).