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化合物 P276-00,Riviciclib hydrochloride

化合物 P276-00|T6924|TargetMol

價(jià)格 383 893 1490
包裝 1mg 5mg 10mg
最小起訂量 1mg
發(fā)貨地 上海
更新日期 2024-12-12
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產(chǎn)品詳情

中文名稱:化合物 P276-00英文名稱:Riviciclib hydrochloride
CAS:920113-03-7品牌: TargetMol
產(chǎn)地: 美國(guó)保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
純度規(guī)格: 99.36%產(chǎn)品類別: 抑制劑
貨號(hào): T6924
2024-12-12 化合物 P276-00 Riviciclib hydrochloride 1mg/383RMB;5mg/893RMB;10mg/1490RMB 383 TargetMol 美國(guó) Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 99.36% 抑制劑

Product Introduction

Bioactivity

名稱Riviciclib hydrochloride
描述Riviciclib hydrochloride (P276-00) is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Phase 2/3.
細(xì)胞實(shí)驗(yàn)The cells are seeded at a density of 3,000-5,000 cells per well, depending on cell type in 180 μL of culture medium in 96-well plate and incubated overnight to allow the cells to adhere. Varying concentrations of compounds are added to the wells and incubated for 48 h at 37°C. 3H-thymidine (0.25 μCi) is added to each well, and incorporation of the radiolabel is allowed to proceed for 5 to 7 h. Following this incubation, cells are harvested onto GF/B unifilter plates using a Packard Filtermate Universal harvester, and the plates are counted in a Packard Top Count 96-well liquid scintillation counter. (Only for Reference)
激酶實(shí)驗(yàn)Cdk4-D1/Cdk2-E enzyme assay: The Cdk4-D1/Cdk2-E enzyme assay is run in 96-well format using Millipore Multiscreen filtration plates. All assay steps are done in a single filter plate. The filtration wells are prewetted with 100 μL of kinase buffer [50 mmol/L HEPES (pH, 7.5), 10 mmol/L MgCl2, 1 mmol/L EGTA], and then the solution is removed by vacuum. With filter plate on vacuum manifold, 50 μL GST-Rb bound to GSH-Sepharose beads in kinase buffer (0.5 μg GST-Rb/50 μL) is added to each well, and vacuum is applied to the filter plate. About 25 μL of a reaction mix containing ATP (cold + hot) and 4× phosphatase inhibitor mix (40 μMol/L unlabeled ATP, 10 μCi/mL γ32P-ATP, 40 mmol/L h-glycerophosphate, 4 mmol/L DTT, 0.4 mmol/L NaF, 0.4 mmol/L sodium orthovanadate) diluted in kinase buffer is added to each well. The test compound (4×final concentration in kinase buffer) or kinase buffer alone (control) is then added in an additional 25 μL volume. To each well, 50 μL (100 ng) of human Cdk4-D1/Cdk2-E enzyme in kinase buffer is added to initiate the reaction, which is allowed to continue for 30 min at 30°C. When the reaction is completed, vacuum is applied again, and the plate is washed with the TNEN buffer [20 mmol/L Tris (pH, 8.0), 100 mmol/L NaCl, 1 mmol/L EDTA, 0.5% nonidet-P40] thrice; the filter plate is air-dried and is placed in a Multiscreen adapter plate. Packard Microscint-O cocktail (30 μL) is added, and the plate is covered with a Top-Seal A film. Quantitation of 32P-GST-Rb in 96-well filter plates is carried out by Top Count scintillation counter. All compounds are tested initially at 1 μMol/L concentration. Compounds showing more than or equal to 50% inhibition are further profiled for IC50 determination.
體外活性Riviciclib對(duì)Cdk4-D1顯示出比對(duì)Cdk2-E[1]高40倍的選擇性。它對(duì)多種人類癌癥細(xì)胞系展現(xiàn)出強(qiáng)大的抗增殖效果,包括HCT-116、U2OS、H-460、HL-60、HT-29、SiHa、MCF-7、Colo-205、SW-480、PC-3、Caco2、T-24,其IC50范圍從300到800 nmol/L,且相較于正常成纖維細(xì)胞,對(duì)癌細(xì)胞顯示出高度的選擇性[1]。Riviciclib能以與ATP競(jìng)爭(zhēng)的方式下調(diào)cyclin D1和Cdk4,并減少Cdk4特異性的pRb Ser780磷酸化。Riviciclib還通過(guò)激活細(xì)胞caspase-3活性和DNA階梯形成誘導(dǎo)凋亡[1]。
體內(nèi)活性Riviciclib通過(guò)腹膜注射給藥方式,每日50 mg/kg,連續(xù)治療20次,可顯著抑制小鼠結(jié)腸癌(CA-51)的生長(zhǎng)。然而,在小鼠肺癌模型(Lewis lung)中,通過(guò)每隔一天腹膜注射60 mg/kg(每日兩次,每次30 mg/kg),共治療7次,也顯示出顯著的生長(zhǎng)抑制效果[2]。此外,Riviciclib還能抑制人類結(jié)腸癌HCT-116異種移植物和人類非小細(xì)胞肺癌H-460異種移植物的生長(zhǎng)[2]。有效性研究表明,其最大耐受劑量為78 mg/kg/d[2]。
存儲(chǔ)條件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : 7 mg/mL (15.97 mM)
DMSO : 82 mg/mL (187.1 mM)
H2O : 81 mg/mL (184.8 mM)
關(guān)鍵字inhibit | Inhibitor | Riviciclib | CDK | Riviciclib hydrochloride | Riviciclib Hydrochloride | Cyclin dependent kinase | Apoptosis
相關(guān)產(chǎn)品L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate
相關(guān)庫(kù)抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 抗癌活性化合物庫(kù) | 抗癌化合物庫(kù) | 已知活性化合物庫(kù) | 激酶抑制劑庫(kù) | 抗衰老化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌臨床化合物庫(kù) | 抗癌藥物庫(kù)
關(guān)鍵字: P276-00|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓,致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū),已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù),以及多種類型的生化試劑產(chǎn)品,包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等,此外,我們還建設(shè)有CADD(計(jì)算機(jī)輔助藥物設(shè)計(jì))研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心,全方位滿足客戶的定制需求。 憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持,我們將有效幫助您縮短研發(fā)周期,取得更成功的結(jié)果。
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詢盤(pán)

化合物 P276-00|T6924|TargetMol相關(guān)廠家報(bào)價(jià)

產(chǎn)品名稱 價(jià)格   公司名稱 報(bào)價(jià)日期
¥4531.90
VIP1年
上海阿拉丁生化科技股份有限公司
2024-11-29
¥3263.90
VIP13年
上海阿拉丁生化科技股份有限公司
2024-10-31
詢價(jià)
程先生(個(gè)體經(jīng)營(yíng))
2023-12-04
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