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帕布昔利布鹽酸鹽,Palbociclib monohydrochloride
  • 帕布昔利布鹽酸鹽,Palbociclib monohydrochloride

帕布昔利布鹽酸鹽|T6239|TargetMol

價(jià)格 詢價(jià)
包裝 1下架
最小起訂量 1下架
發(fā)貨地 上海
更新日期 2024-12-02
QQ交談 微信洽談

產(chǎn)品詳情

中文名稱:帕布昔利布鹽酸鹽英文名稱:Palbociclib monohydrochloride
CAS:827022-32-2品牌: TargetMol
產(chǎn)地: 美國保存條件: 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.
純度規(guī)格: 99.79%產(chǎn)品類別: 抑制劑
貨號: T6239
2024-12-02 帕布昔利布鹽酸鹽 Palbociclib monohydrochloride 1下架/RMB TargetMol 美國 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. 99.79% 抑制劑

Product Introduction

Bioactivity

名稱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.
細(xì)胞實(shí)驗(yàn)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].
激酶實(shí)驗(yàn)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].
動(dòng)物實(shí)驗(yàn)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].
體外活性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].
體內(nèi)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].
存儲(chǔ)條件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.
關(guān)鍵字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
相關(guān)產(chǎn)品Ribociclib | Abemaciclib methanesulfonate | CASIN | Olomoucine | Palbociclib | GW 441756 | Dinaciclib | Ro-3306 | GSK 3 Inhibitor IX | Abemaciclib
相關(guān)庫抑制劑庫 | 抗癌活性化合物庫 | 已知活性化合物庫 | 抗衰老化合物庫 | 高選擇性抑制劑庫 | FDA 上市藥物庫 | 藥物功能重定位化合物庫 | FDA 上市激酶抑制劑庫 | 抗癌臨床化合物庫 | 抗癌藥物庫
關(guān)鍵字: 帕布昔利布鹽酸鹽|||PD 0332991 hydrochloride|||Palbociclib hydrochloride|||Palbociclib (PD-0332991) HCl|TargetMol

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起,為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部,化學(xué)事業(yè)部,生物事業(yè)部和新材料部。 從虛擬篩選到實(shí)體化合物分子供應(yīng);從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成;從對明確靶點(diǎn)的分子篩選到對明確分子的多靶點(diǎn)篩選,從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化,我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。 經(jīng)過在中國市場五年的精心耕耘,我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商,為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩
成立日期 2013-04-18 (12年) 注冊資本 566.2651萬人民幣
員工人數(shù) 100-500人 年?duì)I業(yè)額 ¥ 1億以上
主營行業(yè) 化學(xué)試劑,生物活性小分子 經(jīng)營模式 貿(mào)易,試劑,定制,服務(wù)
  • TargetMol中國(陶術(shù)生物)
VIP 12年
  • 公司成立:12年
  • 注冊資本:566.2651萬人民幣
  • 企業(yè)類型:有限責(zé)任公司(自然人投資或控股)
  • 主營產(chǎn)品:小分子抑制劑,藥物篩選化合物庫,天然產(chǎn)物,活性分子化合物等
  • 公司地址:上海市閘北區(qū)江場三路28號4樓
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