1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. DSR-6434

DSR-6434 

Cat. No.: HY-110120 Purity: 99.49%
Handling Instructions

DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect.

For research use only. We do not sell to patients.

DSR-6434 Chemical Structure

DSR-6434 Chemical Structure

CAS No. : 1059070-10-8

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 115 In-stock
Estimated Time of Arrival: December 31
5 mg USD 130 In-stock
Estimated Time of Arrival: December 31
10 mg USD 220 In-stock
Estimated Time of Arrival: December 31
25 mg USD 490 In-stock
Estimated Time of Arrival: December 31
50 mg USD 900 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect[1][2].

IC50 & Target[1]

TLR7

7.2 nM (EC50, Human)

TLR7

4.6 nM (EC50, Mice)

In Vitro

To assess the specificity of DSR-6434 toward TLR7, an NF-κB-driven reporter assay is performed in HEK293 cells engineered to express either hTLR7, TLR8 or TLR9. In this assay, successful binding of DSR-6434 to the specific receptor leads to NF-κB activation. DSR-6434 is capable of stimulating reporter gene activity only in HEK293 cells expressing hTLR7 and not in HEK293 cells expressing the structurally similar hTLR8 or hTLR9[2].

In Vivo

DSR-6434 treatment (Compound 20; 0.1-1 mg/kg; intravenous injection; biweekly; for 4 weeks; B6C3F1 mice) suppresses the lung metastasis significantly, 78% inhibition at 0.1 mg/kg dosing (with no tumor metastasis at the 1 mg/kg group)[1].

Animal Model: B6C3F1 mice injected with HM-1 ovarian cancer cells[1]
Dosage: 0.1 mg/kg, 1 mg/kg
Administration: Intravenous injection; biweekly; for 4 weeks
Result: Suppressed the lung metastasis significantly, 78% inhibition was seen at 0.1 mg/kg dosing (with no tumor metastasis at the 1 mg/kg group).
Molecular Weight

400.48

Formula

C₁₉H₂₈N₈O₂

CAS No.

1059070-10-8

SMILES

O=C1N(C2=NC(NCCCC)=NC(N)=C2N1)CC3=CN=C(OCCN(C)C)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (624.25 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4970 mL 12.4850 mL 24.9700 mL
5 mM 0.4994 mL 2.4970 mL 4.9940 mL
10 mM 0.2497 mL 1.2485 mL 2.4970 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (2.50 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (2.50 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

DSR-6434DSR6434DSR 6434Toll-like Receptor (TLR)Watersolubilitytumorbearingmicemodelsurvivallong-termimmunologicalmemoryInhibitorinhibitorinhibit

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Product Name:
DSR-6434
Cat. No.:
HY-110120
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