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EC359

Cat. No. M13503
EC359 Structure
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Biological Activity

EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a Kd of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions.

Chemical Information
Molecular Weight 540.68
CAS Number 2012591-09-0
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Suryavathi Viswanadhapalli, et al. Genes Dis. Targeting LIF/LIFR signaling in cancer

[2] Mengxing Li, et al. Commun Biol. LIFR inhibition enhances the therapeutic efficacy of HDAC inhibitors in triple negative breast cancer

[3] Weiwei Tang, et al. Cell Death Discov. LIF/LIFR oncogenic signaling is a novel therapeutic target in endometrial cancer

[4] Suryavathi Viswanadhapalli, et al. Mol Cancer Ther. EC359: A First-in-Class Small-Molecule Inhibitor for Targeting Oncogenic LIFR Signaling in Triple-Negative Breast Cancer

[5] Bradley R Hall, et al. Genes Cancer. Utilizing cell line-derived organoids to evaluate the efficacy of a novel LIFR-inhibitor, EC359 in targeting pancreatic tumor stroma

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