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Tilsotolimod

Cat. No. M42064
Tilsotolimod Structure
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Biological Activity

Tilsotolimod is a synthetic Toll-like receptor 9 (TLR9) agonist that has demonstrated antitumor activity in preclinical models.

Chemical Information
Molecular Weight 7228
Formula C223H284N74O115P22S22
CAS Number 1948266-37-2
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] Salman R Punekar et al. Clin Cancer Res. Intratumoral Therapy to Make a "Cold" Tumor "Hot": The Jury Is Still Out

[2] Hani Babiker et al. Clin Cancer Res. Tilsotolimod Exploits the TLR9 Pathway to Promote Antigen Presentation and Type 1 IFN Signaling in Solid Tumors: A Multicenter International Phase I/II Trial (ILLUMINATE-101)

[3] Christian Karime et al. Expert Opin Investig Drugs. Tilsotolimod: an investigational synthetic toll-like receptor 9 (TLR9) agonist for the treatment of refractory solid tumors and melanoma

[4] Misam Zawit et al. Ann Transl Med. Current status of intralesional agents in treatment of malignant melanoma

[5] Cara Haymaker et al. Cancer Discov. Tilsotolimod with Ipilimumab Drives Tumor Responses in Anti-PD-1 Refractory Melanoma

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