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DSR-6434

Cat. No. M10813
DSR-6434  Structure
Size Price Availability Quantity
5mg USD 130  USD130 In stock
10mg USD 220  USD220 In stock
25mg USD 490  USD490 In stock
50mg USD 880  USD880 In stock
100mg USD 1500  USD1500 In stock
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Quality Control & Documentation
Biological Activity

DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist for both humans and mice with TLR7 EC50 7.2 nM and 4.6 nM, respectively. DSR-6434 has a strong antitumor effect.

Chemical Information
Molecular Weight 400.48
Formula C19H28N8O2
CAS Number 1059070-10-8
Solubility (25°C) DMSO ≥ 200 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] Andrew S Mikhail, et al. Int J Pharm. Evaluation of immune-modulating drugs for use in drug-eluting microsphere transarterial embolization

[2] Olof Berggren, et al. Scand J Immunol. Activation of plasmacytoid dendritic cells and B cells with two structurally different Toll-like receptor 7 agonists

[3] Erina Koga-Yamakawa, et al. Cancer Immunol Immunother. TLR7 tolerance is independent of the type I IFN pathway and leads to loss of anti-tumor efficacy in mice

[4] Amy L Adlard, et al. Int J Cancer. A novel systemically administered Toll-like receptor 7 agonist potentiates the effect of ionizing radiation in murine solid tumor models

[5] Tomoaki Nakamura, et al. Bioorg Med Chem Lett. Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility

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