Ambeed.cn

首页 / / / CDK / Palbociclib

帕博西尼 /Palbociclib 99%

货号:A295334 同义名: 帕布昔利布 / PD 0332991 Ambeed 开学季,买赠积分,赢豪礼

Palbociclib is a highly specific inhibitor of Cdk4 and Cdk6 with IC50s of 11 nM and16 nM.

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Palbociclib 化学结构 CAS号:571190-30-2
Palbociclib 化学结构
CAS号:571190-30-2
Palbociclib 3D分子结构
CAS号:571190-30-2
Palbociclib 化学结构 CAS号:571190-30-2
Palbociclib 3D分子结构 CAS号:571190-30-2
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb_sale, 1,1) ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]}
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} 现货 咨询 - +
购物车0 收藏 询单

Palbociclib 纯度/质量文件 产品仅供科研

货号:A295334 标准纯度: 99%
批次查询: 批次纯度:

全球学术期刊中引用的产品

Cell,2024. Ambeed. [ A125712 ]
Cancer Discov., 2024. Ambeed. [ A285925 ]
JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]
JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]
EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]
更多 >
产品名称 Cdc CDK1 CDK19 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CLK 其他靶点 纯度
XL413 hydrochloride ++++

Cdc7, IC50: 3.4 nM

99%+
SU9516 +++

CDK1, IC50: 40 nM

+++

CDK2, IC50: 22 nM

++

CDK4, IC50: 200 nM

99%+
RO-3306 +++

CDK1, Ki: 20 nM

SGK,ERK 98%
R547 ++++

CDK1/CyclinB, Ki: 2 nM

++++

CDK2/CyclinE, Ki: 3 nM

++++

CDK4/CyclinD1, Ki: 1 nM

99%+
BMS-265246 ++++

CDK1/CyclinB, IC50: 6 nM

++++

CDK2/CyclinE, IC50: 9 nM

+

CDK4/CyclinD, IC50: 230 nM

99%+
NU6027 +

CDK1, Ki: 2.5 μM

+

CDK2, Ki: 1.3 μM

DNA-PK 98%
Purvalanol A ++++

Cdc2/CyclinB, IC50: 4 nM

+++

CDK2/CyclinE, IC50: 35 nM

CDK2/CyclinA, IC50: 70 nM

+

CDK4/CyclinD1, IC50: 850 nM

99%+
SCH900776 ++

CDK2, IC50: 0.16 μM

99%+
AUZ 454 ++++

CDK2(A144C), Kd: 9.7 nM

CDK2(C118L), Kd: 18.6 nM

99%+
A-674563 HCl ++

CDK2, Ki: 46 nM

PKA 98%
JNJ-7706621 ++++

CDK1/CyclinB, IC50: 9 nM

++++

CDK2/CyclinE, IC50: 3 nM

CDK2/CyclinA, IC50: 4 nM

++

CDK3/CyclinE, IC50: 58 nM

+

CDK4/CyclinD1, IC50: 253 nM

++

CDK6/CyclinD1, IC50: 175 nM

99%+
AT7519 ++

CDK1/CyclinB, IC50: 210 nM

++

CDK2/CyclinA, IC50: 47 nM

+

CDK3/CyclinE, IC50: 360 nM

++

CDK4/CyclinD1, IC50: 100 nM

+++

CDK5/p35, IC50: 13 nM

++

CDK6/CyclinD3, IC50: 170 nM

++++

CDK9/CyclinT, IC50: <10 nM

98+%
PHA-793887 ++

CDK1/CyclinB, IC50: 60 nM

++++

CDK2/CyclinE, IC50: 8 nM

CDK2/CyclinA, IC50: 8 nM

++

CDK4/CyclinD1, IC50: 62 nM

++++

CDK5/p25, IC50: 5 nM

++++

CDK7/CyclinH, IC50: 10 nM

++

CDK9/CyclinT1, IC50: 138 nM

99%+
Milciclib +

CDK1/CyclinB, IC50: 398 nM

++

CDK2/CyclinE, IC50: 363 nM

CDK2/CyclinA, IC50: 45 nM

++

CDK4/CyclinD1, IC50: 160 nM

+

CDK5/p35, IC50: 265 nM

++

CDK7/CyclinH, IC50: 150 nM

99%+
Kenpaullone +

CDK1/CyclinB, IC50: 0.4μM

+

CDK2/CyclinE, IC50: 7.5μM

CDK2/CyclinA, IC50: 0.68μM

+

CDK5/p35, IC50: 0.85μM

98%
SNS-032 +++

CDK2/CyclinE, IC50: 48 nM

CDK2/CyclinA, IC50: 38 nM

+

CDK5/p35, IC50: 340 nM

++

CDK7/CyclinH, IC50: 62 nM

++++

CDK9/CyclinT, IC50: 4 nM

99%+
Dinaciclib ++++

CDK1, IC50: 3 nM

++++

CDK2, IC50: 1 nM

++++

CDK5, IC50: 1 nM

++++

CDK9, IC50: 4 nM

99%+
PHA-767491 hydrochloride ++++

Cdc7, IC50: 10 nM

+

CDK1, IC50: 250 nM

+

CDK2, IC50: 240 nM

+

CDK5, IC50: 460 nM

+++

CDK9, IC50: 34 nM

MK2 98%
(R)-Roscovitine +

Cdc2/CyclinB, IC50: 0.65 μM

+

CDK2/CyclinE, IC50: 0.7 μM

CDK2/CyclinA, IC50: 0.7 μM

++

CDK5/p35, IC50: 0.16 μM

99%+
Narazaciclib ++++

CDK4/CyclinD1, IC50: 3.87 nM

++++

CDK6/CyclinD1, IC50: 9.82 nM

RET 99%+
Palbociclib ++++

CDK4/CyclinD3, IC50: 9 nM

CDK4/CyclinD1, IC50: 11 nM

+++

CDK6/CyclinD2, IC50: 15 nM

99%
Abemaciclib ++++

CDK4, IC50: 2 nM

++++

CDK6, IC50: 10 nM

99%
Ribociclib ++++

CDK4, IC50: 10 nM

+++

CDK6, IC50: 39 nM

98%
Palbociclib isethionate ++++

CDK4/CyclinD3, IC50: 9 nM

CDK4/CyclinD1, IC50: 11 nM

+++

CDK6/CyclinD2, IC50: 15 nM

99%+
BS-181 HCl +++

CDK7, IC50: 21 nM

99%+
(E/Z)-THZ1 dihydrochloride ++++

CDK7, IC50: 3.2 nM

99%+
LDC4297 ++++

CDK7, IC50: 0.13 nM

99%+
Senexin A +

CDK19, Kd: 0.31 μM

+

CDK8, Kd: 0.83 μM

98+%
MSC2530818 ++++

CDK8, IC50: 2.6 nM

99%+
Wogonin 99%+
Riviciclib HCl ++

CDK1/CyclinB, IC50: 79 nM

+

CDK2/CyclinE, IC50: 2.54 μM

CDK2/CyclinA, IC50: 224 nM

++

CDK4/CyclinD1, IC50: 63 nM

+

CDK6/CyclinD3, IC50: 396 nM

+

CDK7/CyclinH, IC50: 2.87 μM

+++

CDK9/CyclinT1, IC50: 20 nM

99+%
LDC000067 +

CDK2, IC50: 2.441 μM

++

CDK9, IC50: 44 nM

98%
Flavopiridol +++

CDK1, IC50: 40 nM

+++

CDK2, IC50: 40 nM

+++

CDK4, IC50: 40 nM

+++

CDK6, IC50: 40 nM

+

CDK7, IC50: 300 nM

+++

CDK9, IC50: 20 nM

99%+
LY2857785 +

CDK7, IC50: 0.246 μM

+++

CDK8, IC50: 0.016 μM

+++

CDK9, IC50: 0.011 μM

99%+
AZD-5438 +++

CDK1, IC50: 16 nM

++++

CDK2, IC50: 6 nM

+++

CDK9, IC50: 20 nM

99%+
ML167 ++

Dyrk1B , IC50: 1648 nM

CLK4, IC50: 136 nM

99%+
(E/Z)-TG003 +++

mCLK4, IC50: 15 nM

mCLK1, IC50: 200 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Palbociclib 生物活性

靶点
  • CDK4

    CDK4/CyclinD3, IC50:9 nM

    CDK4/CyclinD1, IC50:11 nM

  • CDK6

    CDK6/CyclinD2, IC50:15 nM

描述 Palbociclib (PD 0332991) is an orally active, selective inhibitor of CDK4 and CDK6, showing IC50 values of 11 nM and 16 nM respectively. It exhibits strong anti-proliferative properties and is capable of inducing cell cycle arrest in cancer cells. This makes it a valuable agent in the study of HR-positive and HER2-negative breast cancer as well as hepatocellular carcinoma[1].[3].[4].
体内研究

When administered orally at doses of 75 or 150 mg/kg daily for 14 days, Palbociclib leads to rapid tumor regressions and delays in tumor growth[1].

An oral dose of 90 mg/kg daily for 12 days decreases Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes of tumor-free mice, indicating its effects independent of tumors[2].

At a dose of 100 mg/kg administered daily for one week, Palbociclib demonstrates significant anti-tumor activity in a genetically engineered mosaic mouse model of liver cancer[4].

体外研究

In laboratory tests, Palbociclib (0-1 μM, over 24 hours) inhibits Rb phosphorylation at Ser795 in MDA-MB-435 cells with an IC50 of 0.063 μM. It shows comparable effects on phosphorylation at both Ser780 and Ser795 in Colo-205 colon carcinoma cells[1].

Additionally, Palbociclib (0-10 μM, over 24 hours) specifically arrests MDA-MB-453 breast cancer cells in the G1 phase[1].

Over a period of 7 days, a 500 nM concentration of Palbociclib boosts the expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells[2].

Palbociclib inhibits growth in various luminal ER-positive and HER2-amplified breast cancer cell lines when applied at concentrations from 0-1 μM for 6 days, with IC50 values ranging between 4 nM and 1 μM[3].

In human liver cancer cell lines, Palbociclib (0-1 μM, over 3 days) restricts proliferation with IC50 values from 0.01 μM to 3.49 μM and induces reversible cell cycle arrest[4].

作用机制 Palbociclib can inhibit CDK4/6 in an ATP-competitive manner through its pyridopyrimidine structure[1][3][4].

Palbociclib 动物研究

Dose Rat: 25 mg/kg[6] (i.p.); 1 mg/kg - 5 mg/kg[5] (i.v.) Mice: 100 mg/kg[7] (i.g., b.w.), 25 mg/kg - 125 mg/kg[8] (p.o.), 5 mg/kg - 200 mg/kg[5] (p.o.)
Administration i.p., i.g., p.o.
Pharmacokinetics
Animal Rats[5]
Dose 5 mg/kg
Administration i.v. or p.o.
Vd 7070 ml/kg (i.v.)
T1/2 2.60 h (i.v.)
2.3 h (p.o.)
Tmax 0.08 h (i.v.)
3.5 h (p.o.)
CL 37 ml/min/kg (i.v.)
Cmax 2507 ng/ml (i.v.)
178 ng/ml (p.o.)
AUC0→t 2160 ng·h/ml (i.v.)
1140 ng·h/ml (p.o.)

Palbociclib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03007979 Breast Cancer ... 展开 >> Breast Carcinoma Cancer of Breast Malignant Tumor of Breast 收起 << Phase 2 Recruiting June 30, 2021 United States, Missouri ... 展开 >> Washington University School of Medicine Recruiting Saint Louis, Missouri, United States, 63110 Contact: Cynthia X Ma, M.D., Ph.D.    314-362-9383    cynthiaxma@wustl.edu    Principal Investigator: Cynthia X Ma, M.D., Ph.D.          Sub-Investigator: Foluso O Ademuyiwa, M.D.          Sub-Investigator: Ron Bose, M.D., Ph.D.          Sub-Investigator: Mathew Cherian, M.D.          Sub-Investigator: Ashley Frith, M.D.          Sub-Investigator: Leonel Hernandez Aya, M.D.          Sub-Investigator: Peter Oppelt, M.D.          Sub-Investigator: Haeseong Park, M.D.          Sub-Investigator: Caron Rigden, M.D.          Sub-Investigator: Rama Suresh, M.D.          Sub-Investigator: Katherine Weilbaecher, M.D.          Sub-Investigator: Rebecca Aft, M.D., Ph.D.          Sub-Investigator: Lindsay Peterson, M.D.          United States, Nebraska University of Nebraska Recruiting Lincoln, Nebraska, United States, 68588 Contact: Jairam Krishnamurthy, M.D.    402-559-1800    jairam.krishnamurthy@unmc.edu    Principal Investigator: Jairam Krishnamurthy, M.D.          Sub-Investigator: Kenneth Cowan, M.D.          Sub-Investigator: Elizabeth Reed, M.D.          Sub-Investigator: Pavankumar Tandra, M.D. 收起 <<
NCT01907607 Advanced Gastrointestinal Stro... 展开 >>mal Tumors 收起 << Phase 2 Active, not recruiting April 2019 France ... 展开 >> Institut Bergonié Bordeaux, Gironde, France, 33076 Centre Georges-Francois Leclerc Dijon, France, 21079 Centre Oscar Lambret Lille, France, 59020 Centre Léon Bérard Lyon, France, 69373 Hôpital de la Timone - AP-HM Marseille, France, 13385 Centre René Gauducheau Nantes, France, 44805 Hôpital Saint-Antoine (AP-HP) Paris, France, 75571 CHU de REIMS - Hôpital Robert Debré Reims, France, 51092 Institut Gustave Roussy Villejuif, France, 94800 收起 <<
NCT03304080 Breast Neoplasms ... 展开 >> Breast Diseases 收起 << Phase 1 Phase 2 Recruiting November 1, 2019 United States, New York ... 展开 >> Mount Sinai Beth Israel Comprehensive Cancer Center West Recruiting New York, New York, United States, 10011 Contact: Paula Klein, MD    212-604-6021    paula.klein@mountsinai.org    Perlmutter Cancer Center NYU Langone Not yet recruiting New York, New York, United States, 10016 Contact: Sylvia Adams, MD    212-731-5795    sylvia.adams@nyumc.org    Sub-Investigator: Sylvia Adams, MD          Mount Sinai West Recruiting New York, New York, United States, 10019 Contact: Krystal Cascetta, MD    212-523-8692    krystal.cascetta@mountsinai.org    New York Presbyterian Herbert Irving Comprehensive Cancer Center at Columbia University Not yet recruiting New York, New York, United States, 10032 Contact: Kevin Kalinsky, MD    212-305-1945    Kk2693@columbia.edu    New York Presbyterian Meyer Cancer Center at Weill Cornell Not yet recruiting New York, New York, United States, 10065 Contact: Eleni Andreopoulou, MD    646-962-9888    ela9082@med.cornell.edu 收起 <<

Palbociclib 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]Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475.

[3]Richard S Finn, 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]Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66(7):1286-1296.

Palbociclib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.17mL

2.23mL

1.12mL

22.34mL

4.47mL

2.23mL

Palbociclib 技术信息

CAS号571190-30-2
分子式C24H29N7O2
分子量 447.533
别名 帕布昔利布 ;PD 0332991
运输蓝冰
存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 10 mg/mL(22.34 mM),配合低频超声,水浴加热至45℃,并调节pH至4,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

0.1 M HCL: 25 mg/mL(55.86 mM),配合低频超声,并调节pH至4

动物实验配方
Ambeed 相关网站 Ambeed.cn Ambeed.com
Ambeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
  • 客户支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    Ambeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务,不为任何个人或者非科研性质用途提供服务。