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SP2509

Cat. No. M6143
SP2509 Structure
Synonym:

HCI-2509

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 30  USD30 In stock
5mg USD 60  USD60 In stock
10mg USD 99  USD99 In stock
50mg USD 280  USD280 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
Cell Experiment
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
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.
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Inui K, et al. Protein Sci. Stepwise assembly of functional C-terminal REST/NRSF transcriptional repressor complexes as a drug target.

[2] Fiskus W, et al. Leukemia. Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells.

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Keywords: SP2509, HCI-2509 supplier, Histone demethylase, inhibitors, activators


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