價格 | ¥310 | ¥539 | ¥888 |
包裝 | 1mg | 5mg | 10mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-02 |
名稱 | SAR125884 hydrochlorid (1116743-46-4(free base)) |
描述 | SAR125844 is a potent and selective MET kinase inhibitor with a favorable preclinical toxicity profile,(IC50=4.2 nM). |
動物實驗 | The antitumor activity of SAR125844 was investigated after administration of SAR125844 solution daily in SNU-5 bearing mice at 10, 20, and 45 mg/kg and every 2 days in Hs 746T tumor–bearing mice (at 5, 10, 20, and 45 mg/kg for SAR125844 solution and at 5, 11, 21, 53, 106, and 213 mg/kg for SAR125844 nanosuspension). Tumor volumes (in mm^3, based on the following formula, volume = length (mm) × width2 (mm2)/2), were measured twice weekly and body weight recorded every day. Endpoints collected were complete regressions (CR, regression below the palpable limit), partial regressions (PR, regression of 50% of the initial tumor volume), and the percentage of tumor regression (% of volume decrease posttreatment compared with pretreatment). Statistical significance was determined by a Dunnett test versus vehicle after a two-way ANOVA with repeated measures performed separately on ranks of changes from baseline with P < 0.05 considered significant[1]. |
體外活性 | MKN-45、Hs 746T 及 SNU-5 細胞在含有完整培養(yǎng)基的poly d-lysine 96孔板中種植。隨后,孔板在逐漸增加的SAR125844濃度下孵育了1小時,按標(biāo)準(zhǔn)程序生成細胞裂解物,并評估pMETY1230/1234/1235水平。使用軟件和四參數(shù)logistic模型[1]計算了IC50值。 |
體內(nèi)活性 | SAR125844抑制了AXL的自磷酸化和TPM–NTRK1過度表達的KM12細胞系的細胞增殖,其IC50值分別為110和1,400nM/升,分別表明在基于細胞的實驗中對AXL和NTRK1具有30倍和500倍的選擇性指數(shù)。SAR125844的選擇性概況在單數(shù)字nM抗增殖活性的MET依賴型細胞系中得到進一步證實,并且在不依賴MET途徑的細胞中完全沒有影響。這與ARQ197在MET依賴型和MET獨立型腫瘤細胞系上具有相等的抗增殖活性形成對比[1]。 |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 55 mg/mL (93.7 mM) |
關(guān)鍵字 | SAR125884 hydrochlorid (1116743-46-4(free base)) | SAR-125884 hydrochlorid (1116743-46-4(free base)) | SAR125884 hydrochlorid (1116743464(free base)) | SAR125884 hydrochlorid (1116743 46 4(free base)) |
相關(guān)產(chǎn)品 | Capmatinib 2HCl | Cabozantinib S-malate | Crizotinib | Amuvatinib | BMS 777607 | (±)-Norcantharidin | Capmatinib xHCl | LMTK3-IN-1 | L-Ascorbic acid 2-phosphate trisodium | Norcantharidin | Bacitracin Zinc | AMG-458 |
相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 抗癌化合物庫 | 已知活性化合物庫 | 細胞因子抑制劑庫 | 抗結(jié)直腸癌化合物庫 | 激酶抑制劑庫 | 膜蛋白靶向化合物庫 | 酪氨酸激酶分子庫 | 細胞重編程化合物庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 589.8595萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 中間體,天然產(chǎn)物,生物化工,化學(xué)試劑,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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