Description
DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
Product information
Molecular Weight: 459.84
Formula: C21H29Cl3N4O
Chemical Name: N-{4-[(1S,2R)-2-aminocyclopropyl]phenyl}-4-(4-methylpiperazin-1-yl)benzamide trihydrochloride
Smiles: Cl.Cl.Cl.CN1CCN(CC1)C1C=CC(=CC=1)C(=O)NC1C=CC(=CC=1)[C@@H]1C[C@H]1N
InChiKey: IMWGCHSQCRLEGY-QWDWFLGPSA-N
InChi: InChI=1S/C21H26N4O.3ClH/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);3*1H/t19-,20+;;;/m0.../s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (217.47 mM; Need ultrasonic). H2O : 50 mg/mL (108.73 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
In Vivo:
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.
Products are for research use only. Not for human use.
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