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APTO-253

APTO-253
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Purity:99.43%
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APTO-253

Catalog No. T10352Cas No. 916151-99-0
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.
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Pack SizePriceAvailabilityQuantity
1 mg$36In Stock
2 mg$50In Stock
5 mg$73In Stock
10 mg$103In Stock
25 mg$189In Stock
50 mg$337In Stock
100 mg$513In Stock
1 mL x 10 mM (in DMSO)$81In Stock
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Product Introduction

Bioactivity
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.
AliasLOR-253, LT-253
Chemical Properties
Molecular Weight367.38
FormulaC22H14FN5
Cas No.916151-99-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 32.33 mg/mL(88 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7220 mL13.6099 mL27.2198 mL136.0989 mL
5 mM0.5444 mL2.7220 mL5.4440 mL27.2198 mL
10 mM0.2722 mL1.3610 mL2.7220 mL13.6099 mL
20 mM0.1361 mL0.6805 mL1.3610 mL6.8049 mL
50 mM0.0544 mL0.2722 mL0.5444 mL2.7220 mL

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