In vitro: In AML cells, SP2509 inhibits the association of LSD1 with CoREST, increases promoter-specific H3K4Me3 and induces p53, p21 and C/EBPα. SP2509 also significantly inhibits the colony growth and induces apoptosis of OCI-AML3. In addition, SP2509 induces differentiation of cultured and primary AML cells, and exerts synergistic lethal activity when used in combination with panobinostat.
In vivo: In mice bearing OCI-AML3 xenografts, SP2509 (25 mg/kg i.p.) significantly improved the survival of the mice, while co-treatment with SP2509 and panobinostat exerts superior in vivo activity.
Cell Experiment | |
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Cell lines | OCI-AML3, MV4-11 and MOLM13 cells |
Preparation method | Cultured AML cells are treated with SP2509 and/or PS for 96 h. At the end of treatment, cells are washed free of the drugs and 500 cells per condition are plated in methylcellulose and incubated at 37 °C. Colony formation is measured 7–10 days after plating. |
Concentrations | ~10 μM |
Incubation time | 96 h |
Animal Experiment | |
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Animal models | NOD/SCID mice bearing OCI-AML3 xenografts |
Formulation | 20% Cremaphor, 20% DMSO, 60% sterile water |
Dosages | 25 mg/kg twice per week |
Administration | i.p. |
Molecular Weight | 437.90 |
Formula | C19H20ClN3O5S |
CAS Number | 1423715-09-6 |
Solubility (25°C) | 38 mg/mL in DMSO |
Storage | 2-8°C, protect from light |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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