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  • 帕布昔利布盐酸盐|T6239|TargetMol

帕布昔利布盐酸盐|T6239|TargetMol

Palbociclib monohydrochloride
827022-32-2
询价 1下架 起订
上海 更新日期：2024-09-23

TargetMol中国（陶术生物）

VIP12年
联系人：邵小姐
电话：021-021-33632979拨打
手机：15002134094 拨打
邮箱：marketing@targetmol.com

产品详情:

中文名称：
帕布昔利布盐酸盐
英文名称：
Palbociclib monohydrochloride
CAS号：
827022-32-2
品牌：
TargetMol
产地：
美国
保存条件：
keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.79%
产品类别：
抑制剂
货号：
T6239

Product Introduction

Bioactivity

名称Palbociclib monohydrochloride
描述Palbociclib monohydrochloride (PD 0332991 hydrochloride) is a selective inhibitor of CDK4/6 (IC50s: 11/16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.
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].
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].
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].
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].
存储条件keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 5 mg/mL (10.33 mM)
H2O : 20 mg/mL (41.32 mM), Sonication is recommended.
关键字cell cycle | estrogen receptor | HER2 | PD 0332991 monohydrochloride | inhibit | Cyclin dependent kinase | Palbociclib monohydrochloride | hepatocellular carcinoma | PD0332991 Hydrochloride | Breast cancer | PD-0332991 Hydrochloride | PD 0332991 Hydrochloride | Inhibitor | Palbociclib Hydrochloride | Palbociclib Monohydrochloride | Palbociclib | HCC | CDK
相关产品Ribociclib | Abemaciclib methanesulfonate | CASIN | Olomoucine | Palbociclib | GW 441756 | Dinaciclib | Ro-3306 | GSK 3 Inhibitor IX | Abemaciclib
相关库抑制剂库 | 抗癌活性化合物库 | 已知活性化合物库 | 抗衰老化合物库 | 高选择性抑制剂库 | FDA 上市药物库 | 药物功能重定位化合物库 | FDA 上市激酶抑制剂库 | 抗癌临床化合物库 | 抗癌药物库
帕布昔利布盐酸盐|||PD 0332991 hydrochloride|||Palbociclib hydrochloride|||Palbociclib (PD-0332991) HCl|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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  • 2024-10-29
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