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APTO-253

Catalog No. T10352 CAS 916151-99-0

Synonyms: LOR-253, LT-253

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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APTO-253, CAS 916151-99-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 73.00
10 mg	In stock	$ 103.00
25 mg	In stock	$ 189.00
50 mg	In stock	$ 337.00
100 mg	In stock	$ 513.00
1 mL * 10 mM (in DMSO)	In stock	$ 81.00

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Purity: 99.43%

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Description

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.

Synonyms	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

Solubility Information

DMSO: 32.33 mg/mL(88 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Clinical Compound Library Anti-Cancer Metabolism Compound Library HIF-1 Signaling Pathway Compound Library Anti-Prostate Cancer Compound Library Reprogramming Compound Library

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Keywords

APTO-253 916151-99-0 Apoptosis Cell Cycle/Checkpoint MAPK KLF c-Myc Myc LOR-253 LT-253 inhibit LT 253 Inhibitor LT253 Krüppel-like factor APTO253 LOR253 APTO 253 LOR 253 inhibitor

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