keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MSC-4106 是一种有效的、具有口服活性的 YAP/TAZ-TEAD 抑制剂。 MSC-4106 阻断 TEAD1 和 TEAD3 的自棕榈酰化,并且对 NCI-H226 异种移植瘤模型显示抑制作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 997 | 现货 | ||
5 mg | ¥ 2,450 | 现货 | ||
10 mg | ¥ 3,930 | 现货 | ||
25 mg | ¥ 6,290 | 现货 | ||
50 mg | ¥ 8,660 | 现货 | ||
100 mg | ¥ 11,600 | 现货 | ||
500 mg | ¥ 23,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,630 | 现货 |
产品描述 | MSC-4106, an orally active and potent YAP/TAZ-TEAD inhibitor, disrupts TEAD1 and TEAD3 auto-palmitoylation and demonstrates significant efficacy in the NCI-H226 tumor xenograft model [1]. |
体外活性 | MSC-4106 (10 μM, 24 h) inhibited SK-HEP-1 reporter and NCI-266 cell viability with IC 50 values of 4 nM and 14 nM, respectively [1]. MSC-4106 (10 μM, 6 h) crystallizes in the P-site of TEAD1, and against TEAD1 or TEAD3 palmitoylation in TEAD-Overexpressing HEK293 Cells by 97.3% and 75.9%, respectively [1]. MSC-4106 (10 μM, 4 d) targets TEAD suggested by a reduction in viability of NCI-H226 cells [1]. Cell Viability Assay [1] Cell Line: NCI-H226 (YAP dependent); SW620 YAP/TAZ KO (Yap-independent) cells Concentration: 0, 3, 6, 9, 12, 15, 18, 21, 24, 26, 30 μM Incubation Time: 96 hours Result: Showed inhibitory effect to NCI-H226 and general cytotoxic to SW620 (IC 50 >30 μM). Immunofluorescence [1] Cell Line: SK-HEP-1 Concentration: 0, 3, 6, 9, 12, 15, 18, 21, 24, 26, 30 μM Incubation Time: 24 hours Result: Inhibited YAP-TEAD interation. |
体内活性 | MSC-4106 (P.O.; 100 mg/kg once daily; 7 days) shows anti-tumor effect with controlled tumor volume and good tolerability with stable body weight in mice [1]. MSC-4106 (P.O.; 1, 5, 100 mg/kg once daily; 6, 24, 30, 48, and 72 h) down-regulates Cyr61 (cysteine-rich angiogenic inducer 61) expression, the TEAD-regulated target gene, in tumor lysates at all time points at 100 mg/kg and 24 h at 5 mg/kg [1]. Pharmacokinetics (PK) profile in different species [1] Parameter Mouse Rat Dog Cl (l/h/kg) 0.2 0.7 0.05 PO t 1/2 (h) 45 40 3.6 PO AUC (μg h/mL) 45 10 33 V ss (L/kg) 2 5 0.3 F (%) >90 80 18 Note : PO studies were performed at 10 mg/kg; MSC-4106 was formulated in 20% Kleptose in 50 mM PBS at pH 7.4. Animal Model: NCI-H226 xenograft model in H2d Rag2 female mice (9-week-old) [1] Dosage: 5, 100 mg/kg Administration: Oral gavage; once daily; 32 days Result: Resulted tumor growth controlled with 5 mg/kg while regressed with 100 mg/kg dosing after 32 treatment days. |
分子量 | 359.3 |
分子式 | C18H12F3N3O2 |
CAS No. | 2738542-58-8 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 225 mg/mL (626.2 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7832 mL | 13.9159 mL | 27.8319 mL | 69.5797 mL |
5 mM | 0.5566 mL | 2.7832 mL | 5.5664 mL | 13.9159 mL | |
10 mM | 0.2783 mL | 1.3916 mL | 2.7832 mL | 6.958 mL | |
20 mM | 0.1392 mL | 0.6958 mL | 1.3916 mL | 3.479 mL | |
50 mM | 0.0557 mL | 0.2783 mL | 0.5566 mL | 1.3916 mL | |
100 mM | 0.0278 mL | 0.1392 mL | 0.2783 mL | 0.6958 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
MSC-4106 2738542-58-8 Stem Cells YAP MSC4106 MSC 4106 Inhibitor inhibitor inhibit