Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Varlitinib (ASLAN001) 是有效,可逆的泛 EGFR 小分子抑制剂,对 HER1,HER2 和 HER4 的 IC50 值分别为7,2,4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 330 | 现货 | ||
2 mg | ¥ 460 | 现货 | ||
5 mg | ¥ 925 | 现货 | ||
10 mg | ¥ 1,516 | 现货 | ||
25 mg | ¥ 2,532 | 现货 | ||
50 mg | ¥ 3,798 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 950 | 现货 |
产品描述 | Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively. |
靶点活性 | ERB1:7 nM, ErbB2:2 nM |
体外活性 | In cell-based assays using tumor cells that over-express EGFR (A431) or ErbB-2 (BT474), Varlitinib (ARRY-334543) potently inhibits substrate phosphorylation. Varlitinib is shown to be highly selective for EGFR/ErbB-2, and does not show any significant activity when screened against a panel of 104 kinases[2]. |
体内活性 | Varlitinib treatment potently inhibits tumor growth with complete tumor regression observed at dosing of 100 mg/kg twice a day. After five days of Varlitinib treatment, phosphorylation of HER1-3, RAS/RAF/MEK/MAPK, p70S6K, S6 ribosomal, 4EBP1, Cdk-2, Cdc-2 and retinoblastoma are strongly inhibited. Varlitinib treatment results in a significant reduction in survivin and a concomittant increase in Caspase 3 cleavage products[1]. In murine xenograft models, Varlitinib (ARRY-334543) demonstrates significant dose-related (25, 50, 100 mg/kg) tumor growth inhibition in A431-derived tumors when administered orally, twice a day, for 21 days[2]. |
别名 | ASLAN001, ARRY-334543 |
分子量 | 466.94 |
分子式 | C22H19ClN6O2S |
CAS No. | 845272-21-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 31.5 mg/mL (67.5 mM), Sonication and heating to 60℃ are recommended.
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1416 mL | 10.708 mL | 21.416 mL | 53.5401 mL |
5 mM | 0.4283 mL | 2.1416 mL | 4.2832 mL | 10.708 mL | |
10 mM | 0.2142 mL | 1.0708 mL | 2.1416 mL | 5.354 mL | |
20 mM | 0.1071 mL | 0.5354 mL | 1.0708 mL | 2.677 mL | |
50 mM | 0.0428 mL | 0.2142 mL | 0.4283 mL | 1.0708 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。
Varlitinib 845272-21-1 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors HER ARRY 334543 ASLAN001 ARRY-334543 ARRY334543 ASLAN-001 ASLAN 001 Inhibitor inhibitor inhibit