APTO-253
Names
[ CAS No. ]:
1422826-80-9
[ Name ]:
APTO-253
Biological Activity
[Description]:
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
[References]
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. View Related Products by Target c-Myc Blood Cancer
Chemical & Physical Properties
[ Molecular Formula ]:
C22H14FN5
[ Molecular Weight ]:
367.387