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APTO-253

Cat. No. M13539

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APTO-253 Structure
Synonym:

LOR-253; LT-253

Size Price Availability Quantity
10mM*500uL in DMSO USD 55  USD55 In stock
1mg USD 36  USD36 In stock
2mg USD 50  USD50 In stock
5mg USD 72  USD72 In stock
10mg USD 110  USD110 In stock
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Quality Control & Documentation
Biological Activity

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. 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 (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.

Chemical Information
Molecular Weight 367.38
CAS Number 916151-99-0
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Wataru Nakajima, et al. Genes (Basel). Krüppel-Like Factor 4 and Its Activator APTO-253 Induce NOXA-Mediated, p53-Independent Apoptosis in Triple-Negative Breast Cancer Cells

[2] Michael J Duffy, et al. Cancer Treat Rev. MYC as a target for cancer treatment

[3] Saikat Pal, et al. Phys Chem Chem Phys. An in silico investigation of the binding modes and pathway of APTO-253 on c-KIT G-quadruplex DNA

[4] Andrea Local, et al. Mol Cancer Ther. APTO-253 Stabilizes G-quadruplex DNA, Inhibits MYC Expression, and Induces DNA Damage in Acute Myeloid Leukemia Cells

[5] Cheng-Yu Tsai, et al. Mol Cancer Ther. APTO-253 Is a New Addition to the Repertoire of Drugs that Can Exploit DNA BRCA1/2 Deficiency

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Keywords: APTO-253, LOR-253; LT-253 supplier, c-Myc, inhibitors, activators

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