Powder: -20°C for 3 years | In solvent: -80°C for 1 year
APTO-253 (LOR-253) 抑制 c-Myc 表达,稳定 G-四链体 DNA,并诱导急性髓细胞白血病细胞的细胞周期停滞和凋亡。 它通过诱导 KLF4 肿瘤抑制因子介导抗癌活性,具有抗关节炎活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 293 | 现货 | ||
2 mg | ¥ 415 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 970 | 现货 | ||
25 mg | ¥ 1,830 | 现货 | ||
50 mg | ¥ 3,160 | 现货 | ||
100 mg | ¥ 4,650 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 728 | 现货 |
产品描述 | APTO-253 (LOR-253) inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through the induction of the KLF4 tumor suppressor. |
体外活性 | APTO-253 (5 μM) induces KLF4 expression and enhances apoptosis induced by NSC 119875 in both SKOV3 and OVCAR3 cells. APTO-253 (5 μM) also leads to G1 phase arrest and reduces S and G2/M phase cells in SKOV3 and OVCAR3 cells [1]. APTO-253 is cytotoxic to Raji and Raji/253R cell lines (IC50s: 105 nM and 1387 nM). APTO-253 (0.5 μM) also causes DNA damage in Raji cells. BRCA1/2 deficient cells are hypersensitive to APTO-253. ABCG2 overexpressed HEK-293 cells are resistant to APTO-253 and inhibition of ABCG2 reverses resistance to APTO-253 in Raji/253R [2]. APTO-253 suppresses the proliferation of acute myeloid leukemia (AML) cell lines and various forms of lymphoma cell lines (IC50s: 57 nM to 1.75 μM). APTO-253 (500 nM) also causes G0/G1 cell cycle arrest, induces apoptosis, and down-regulates MYC RNA and protein expression in AML lines. APTO-253 (500 nM) leads to DNA damage response pathways in MV4-11 cells. Furthermore, APTO-253 is a potent stabilizer of G-quadruplex (G4) motifs and demonstrates the greatest propensity for stabilizing the MYC G4 sequences. |
别名 | LOR-253, LT-253 |
分子量 | 367.38 |
分子式 | C22H14FN5 |
CAS No. | 916151-99-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 32.33 mg/mL(88 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.722 mL | 13.6099 mL | 27.2198 mL | 68.0494 mL |
5 mM | 0.5444 mL | 2.722 mL | 5.444 mL | 13.6099 mL | |
10 mM | 0.2722 mL | 1.361 mL | 2.722 mL | 6.8049 mL | |
20 mM | 0.1361 mL | 0.6805 mL | 1.361 mL | 3.4025 mL | |
50 mM | 0.0544 mL | 0.2722 mL | 0.5444 mL | 1.361 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。
APTO-253 916151-99-0 Apoptosis Cell Cycle/Checkpoint MAPK c-Myc KLF Myc LOR-253 LT-253 inhibit LT 253 Inhibitor LT253 Krüppel-like factor APTO253 LOR253 APTO 253 LOR 253 inhibitor