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APTO-253

Catalog No. T10352 CAS 916151-99-0

Synonyms: LT-253, LOR-253

APTO-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

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Purity: 98%

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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	LT-253, LOR-253
Molecular Weight	367.38
Formula	C22H14FN5
CAS No.	916151-99-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 32.33 mg/mL(88 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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 Compound Library Anti-Cancer Metabolism Compound Library Glutamine Metabolism Compound Library Cell Cycle Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Stem Cell Differentiation Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Bioactive Compound Library

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Keywords

APTO-253 916151-99-0 MAPK信号通路凋亡细胞周期 Apoptosis c-Myc KLF LT 253 LT253 Myc inhibit LT-253 APTO 253 LOR 253 APTO253 LOR-253 Inhibitor Krüppel-like factor LOR253 inhibitor

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