價(jià)格 | ¥358 | ¥519 | ¥863 |
包裝 | 1mg | 2mg | 5mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-12 |
中文名稱:化合物 Prexasertib | 英文名稱:Prexasertib |
CAS:1234015-52-1 | 品牌: TargetMol |
產(chǎn)地: 美國(guó) | 保存條件: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 97.3% | 產(chǎn)品類(lèi)別: 抑制劑 |
貨號(hào): T4310 |
名稱 | Prexasertib |
描述 | Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity. |
細(xì)胞實(shí)驗(yàn) | LY2606368 is broadly antiproliferative with IC50s of 3 nM, 3 nM, 10 nM, 37 nM, and 68 nM against U-2 OS, Calu-6, HT-29, HeLa, and NCI-H460 cell lines, respectively. LY2606368 (25 μM) exhibits inhibitory activities against proliferation of AGS and MKN1 cells. LY2606368 (20 nM) inhibits HR repair capacity DR-GFP cells. |
動(dòng)物實(shí)驗(yàn) | LY2606368 is formulated in vehicle consisting of 20% Captisol.Female CD-1 nu-/nu- mice (26-28 g) are used for this study. Tumor growth is initiated by subcutaneous injection of 1×106 Calu-6 cells in a 1:1 mixture of serum-free growth medium and Matrigel in the rear flank of each subject animal. When tumor volumes reach approximately 150 mm3 in size, the animals are randomized by tumor size and body weight, and placed into their respective treatment groups. Vehicle consisting of 20% Captisol pH4 or LY2606368 is administered by subcutaneous injection in a volume of 200 μL. Four, eight, 12, 24, and 48 hours after drug administration, blood for plasma drug exposure is extracted via cardiac puncture and assayed on a Sciex API 4000 LC/MS-MS system. The xenograft tissue is promptly removed and prepared. Lysates are analyzed by immunoblot analysis for protein phosphorylation levels. Group means, SEs and P values are calculated using Kronos. |
體外活性 | LY2606368在p53缺失的HeLa細(xì)胞中強(qiáng)效抑制由多柔比星激活的G2-M檢查點(diǎn)(EC50=9 nM)。LY2606368是一種強(qiáng)效的、選擇性的ATP競(jìng)爭(zhēng)性Chk1抑制劑(IC50 <1 nM),同時(shí)也能抑制CHK2(IC50=8 nM)。 |
體內(nèi)活性 | 在異種移植瘤模型中,LY2606368 (15 mg/kg, s.c.) 顯著抑制腫瘤生長(zhǎng),并且動(dòng)物體重?fù)p失較少。 |
存儲(chǔ)條件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : < 1 mg/mL (insoluble or slightly soluble) |
關(guān)鍵字 | SIK | Prexasertib | Checkpoint Kinase (Chk) | HT-29 | S296 | Apoptosis | DNA | double-stranded | inhibit | autophosphorylation | LY-2606368 | H2AX | ATP-competitive | HeLa | MELK | RSK1 | CDK2 | Inhibitor | S516 | ARK5 | replication | BRSK2 | CDC25A | LY 2606368 |
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) | 已知活性化合物庫(kù) | 激酶抑制劑庫(kù) | 抗衰老化合物庫(kù) | 抗病毒庫(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) |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.265100萬(wàn)人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營(yíng)行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營(yíng)模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
產(chǎn)品名稱 | 價(jià)格 | 公司名稱 | 報(bào)價(jià)日期 | |
---|---|---|---|---|
詢價(jià) |
VIP6年
|
上海澤葉生物科技有限公司
|
2025-01-10 | |
詢價(jià) |
VIP1年
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廣州佳途科技股份有限公司
|
2024-12-24 | |
詢價(jià) |
上海瀚香生物科技有限公司
|
2020-04-07 |