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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。
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 | 库存 | 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 x 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 | LT-253, LOR-253 |
分子量 | 367.38 |
分子式 | C22H14FN5 |
CAS No. | 916151-99-0 |
Smiles | Cc1[nH]c2ccc(F)cc2c1-c1nc2c([nH]1)c1cccnc1c1ncccc21 |
密度 | 1.481 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 32.33 mg/mL (88 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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