DDP-38003 dihydrochloride

• CAT Number: I010081
• CAS Number: 1831167-98-6
• Molecular Formula: C21H28Cl2N4O
• Molecular Weight: 423.38
• Purity: ≥95%
• Synonyms: N-[4-[(1S,2R)-2-aminocyclopropyl]phenyl]-4-(4-methylpiperazin-1-yl)benzamide;dihydrochloride
• InChI: InChI=1S/C21H26N4O.2ClH/c1-24-10-12-25(13-11-24)18-8-4-16(5-9-18)21(26)23-17-6-2-15(3-7-17)19-14-20(19)22;;/h2-9,19-20H,10-14,22H2,1H3,(H,23,26);2*1H/t19-,20+;;/m0../s1
• InChIKey: HFSFENIQYFFMGC-HUQPAIQZSA-N
• SMILES: CN1CCN(CC1)C2=CC=C(C=C2)C(=O)NC3=CC=C(C=C3)C4CC4N.Cl.Cl

DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM[1].
DDP-38003 inhibits KDM1A with an IC50 of 84 nM. DDP-38003 is more active in reducing the colony forming ability and in inducing thedifferentiation of THP-1 cells compared to the 1R, 2S analogue[1].
DDP-38003 exhibits in vivo efficacy after oral administration, determining a 62% increased survival in mouse leukemia models with evidence of KDM1A inhibition. The half life of DDP-38003 is 8 h. A significant dose dependent increase of mice survival is obtained by DDP-38003 treatment. The survival rate increases 35% and 62% at the dose of 11.25 and 22.50 mg/kg, respectively. DDP-38003 is a potential oral anticancer agent[1].

Reference

[1]. Vianello P, et al. Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent. J Med Chem. 2016 Feb 25;59(4):1501-17.
 [Content Brief]