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APTO-253 hydrochloride

Chemical Structure : APTO-253 hydrochloride

CAS No.: 1422731-37-0

APTO-253 hydrochloride (APTO253;LOR253;LOR-253)

Catalog No.: PC-35076Not For Human Use, Lab Use Only.

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

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

APTO-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]; 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.

Blood Cancer

Phase 1 Clinical

Physicochemical Properties

M.Wt 403.845
Formula C22H15ClFN5
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-(6-fluoro-2-methyl-1H-indol-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline hydrochloride

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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