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APTO-253

Chemical Structure : APTO-253

CAS No.: 916151-99-0

APTO-253 (APTO253, LOR253, LOR-253)

Catalog No.: PC-35075Not For Human Use, Lab Use Only.

APTO-253 (LOR-253) is a small molecule inducer of KLF4, stabilizes G-quadruplex DNA and reduces MYC mRNA expression and protein levels.

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Biological Activity

APTO-253 (LOR-253) is a small molecule inducer of KLF4, stabilizes G-quadruplex DNA and reduces MYC mRNA expression and protein levels.
APTO-253 is converted intracellularly from a monomer to a ferrous complex [Fe(253)3].
APTO-253 selectively induces CDKN1A (p21), promotes G0-G1 cell-cycle arrest, and triggers apoptosis in acute myeloid leukemia (AML) cells without producing myelosuppression in various animal species and humans, induces DNA Damage in AML cells.

Physicochemical Properties

M.Wt 367.387
Formula C22H14FN5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(5-Fluoro-2-methyl-1H-indol-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline

References

1. Tsai CY, et al. Mol Cancer Ther. 2018 Apr 6. doi: 10.1158/1535-7163.MCT-17-0834.

2. Cercek A, et al. Invest New Drugs. 2015 Oct;33(5):1086-92.

3. Wang B, et al. Biochem Biophys Res Commun. 2017 Mar 11;484(3):486-492.

4. Local A, et al. Mol Cancer Ther. 2018 Apr 6. doi: 10.1158/1535-7163.MCT-17-1209.

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