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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $36 | In Stock | |
2 mg | $50 | In Stock | |
5 mg | $73 | In Stock | |
10 mg | $103 | In Stock | |
25 mg | $189 | In Stock | |
50 mg | $337 | In Stock | |
100 mg | $513 | In Stock | |
1 mL x 10 mM (in DMSO) | $81 | In Stock |
Description | 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. |
In vitro | 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. |
Alias | LOR-253, LT-253 |
Molecular Weight | 367.38 |
Formula | C22H14FN5 |
Cas No. | 916151-99-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 32.33 mg/mL (88 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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