APTO-253 (LOR-253) 是一种小分子，可抑制c-Myc表达，稳定 G-四链体 DNA 并诱导急性髓样白血病细胞的细胞周期停滞和凋亡。APTO-253 通过诱导 Kruppel-like factor 4 (KLF4) 抑癌因子介导抗癌活性。APTO-253 具有抗关节炎活性。

APTO-253 (LOR-253) is a small molecule that 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 induction of the Krüppel-like factor 4 (KLF4) tumor suppressor. APTO-253 has antiarthritic activity.

Solid

c-Myc; KLF4

APTO-253 (LOR-253) is an inducer of KLF4. 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.
APTO-253 is cytotoxic to Raji and Raji/253R cell lines, with IC50s of 105 ± 2.4 nM and 1387 ± 94 nM, respectively. 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.
APTO-253 suppresses the proliferation of acute myeloid leukemia (AML) cell lines and various forms of lymphoma cell lines with IC50s ranging from 57 nM to 1.75 μM. APTO-253 (500 nM) also causes G0/G1 cell cycle arrest, induces apopt

APTO-253 (LOR-253; 15 mg/kg; IV; twice per day for 2 consecutive days per week for 14 days) has antiarthritic activity in a CIA model.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Local A, et al. APTO-253 Stabilizes G-quadruplex DNA, Inhibits MYC Expression, and Induces DNA Damage in Acute Myeloid Leukemia Cells. Mol Cancer Ther. 2018 Jun;17(6):1177-1186.
[2]. Hongying Zhang, et al. Inhibition of c-Myc By Apto-253 As an Innovative Therapeutic Approach to Induce Cell Cycle Arrest and Apoptosis in Acute Myeloid Leukemia. Blood 2016 128:1716.

In Vitro: DMSO : 60 mg/mL (163.32 mM; Need ultrasonic)配制储备液