916151-99-0APTO-253 (LOR-253)

产品属性：

Cas No.916151-99-0

别名 N/A

化学名 N/A

分子式 C22H14FN5

分子量 367.38

溶解度 DMSO : 33.33 mg/mL (90.72 mM);H2O : < 0.1 mg/mL (insoluble)

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
APTO-253 is an inducer of Kruppel-like factor 4 (KLF4), and also stabilizes Gquadruplex, with anti-proliferative activity.

APTO-253 is an inducer of KLF4. APTO-253 (5 μM) induces KLF4 expression, and enhances apoptosis induced by cisplatin 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, 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[2]. 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 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. Futhermore, APTO-253 is a potent stabilizer of Gquadruplex (G4) motifs, and demonstrates the greatest propensity for stabilizing the MYC G4 sequences[3].

[1]. Wang B, et al. KLF4 expression enhances the efficacy of chemotherapy drugs in ovarian cancer cells. Biochem Biophys Res Commun. 2017 Mar 11;484(3):486-492. [2]. Tsai CY, et al. APTO-253 is a new addition to the repertoire of drugs that can exploit DNA BRCA1/2 deficiency. Mol Cancer Ther. 2018 Apr 6. pii: molcanther.0834.2017. [3]. 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 Apr 6. pii: molcanther.1209.2017.