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MedKoo Cat#: 408077 | Name: DSR-6434
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

DSR-6434 is a potent TLR7 agonist (EC50 = 7.2 nM). DSR-6434 activates several immune effector cells in vitro. DSR-6434 indicated an optimal balance between the agonistic potency and high water solubility. It also demonstrated a strong antitumor effect in vivo by intravenous administration in a tumor bearing mice model.

Chemical Structure

DSR-6434
DSR-6434
CAS#1059070-10-8

Theoretical Analysis

MedKoo Cat#: 408077

Name: DSR-6434

CAS#: 1059070-10-8

Chemical Formula: C19H28N8O2

Exact Mass: 400.2335

Molecular Weight: 400.49

Elemental Analysis: C, 56.98; H, 7.05; N, 27.98; O, 7.99

Price and Availability

Size Price Availability Quantity
25mg USD 350.00 2 Weeks
50mg USD 650.00 2 Weeks
100mg USD 1,050.00 2 Weeks
200mg USD 1,650.00 2 Weeks
500mg USD 3,250.00 2 Weeks
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Related CAS #
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Synonym
DSR-6434; DSR 6434; DSR6434;
IUPAC/Chemical Name
6-Amino-2-(butylamino)-9-[[6-[2-(dimethylamino)ethoxy]-3-pyridinyl]methyl]-7,9-dihydro-8H-purin-8-one
InChi Key
SSZHESNDOMBSRV-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H28N8O2/c1-4-5-8-21-18-24-16(20)15-17(25-18)27(19(28)23-15)12-13-6-7-14(22-11-13)29-10-9-26(2)3/h6-7,11H,4-5,8-10,12H2,1-3H3,(H,23,28)(H3,20,21,24,25)
SMILES Code
O=C1NC2=C(N)N=C(NCCCC)N=C2N1CC3=CC=C(OCCN(C)C)N=C3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
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.
In vitro activity:
DSR 6434, a Toll-like receptor agonist, and BMS-202, a PD-L1 checkpoint inhibitor, induced immune cell replication and were successfully loaded into radiopaque DEE microspheres in high concentrations. Reference: Int J Pharm. 2022 Mar 25;616:121466. https://pubmed.ncbi.nlm.nih.gov/35065205/
In vivo activity:
This study shows that TLR7 tolerance was independent of type I interferon (IFN) negative feedback because induction of TLR7 tolerance was also observed in IFN-α/β receptor knockout mice treated with DSR-6434. Moreover, these data demonstrate that treatment of bone marrow-derived plasmacytoid dendritic cells (BM-pDC) with DSR-6434 led to downregulation of TLR7 expression. Reference: Cancer Immunol Immunother. 2015 Oct;64(10):1229-39. https://pubmed.ncbi.nlm.nih.gov/26091797/
Solvent mg/mL mM comments
Solubility
DMSO 145.0 362.12
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 400.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Mikhail AS, Mauda-Havakuk M, Negussie AH, Hong N, Hawken NM, Carlson CJ, Owen JW, Franco-Mahecha O, Wakim PG, Lewis AL, Pritchard WF, Karanian JW, Wood BJ. Evaluation of immune-modulating drugs for use in drug-eluting microsphere transarterial embolization. Int J Pharm. 2022 Mar 25;616:121466. doi: 10.1016/j.ijpharm.2022.121466. Epub 2022 Jan 20. PMID: 35065205; PMCID: PMC9139086. 2. Berggren O, Pucholt P, Amcoff C, Rönnblom L, Eloranta ML. Activation of plasmacytoid dendritic cells and B cells with two structurally different Toll-like receptor 7 agonists. Scand J Immunol. 2020 Jun;91(6):e12880. doi: 10.1111/sji.12880. Epub 2020 Apr 13. PMID: 32219875. 3. Koga-Yamakawa E, Murata M, Dovedi SJ, Wilkinson RW, Ota Y, Umehara H, Sugaru E, Hirose Y, Harada H, Jewsbury PJ, Yamamoto S, Robinson DT, Li CJ. TLR7 tolerance is independent of the type I IFN pathway and leads to loss of anti-tumor efficacy in mice. Cancer Immunol Immunother. 2015 Oct;64(10):1229-39. doi: 10.1007/s00262-015-1730-4. Epub 2015 Jun 20. PMID: 26091797. 4. Nakamura T, Wada H, Kurebayashi H, McInally T, Bonnert R, Isobe Y. Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility. Bioorg Med Chem Lett. 2013 Feb 1;23(3):669-72. doi: 10.1016/j.bmcl.2012.11.114. Epub 2012 Dec 5. PMID: 23265901.
In vitro protocol:
1. Mikhail AS, Mauda-Havakuk M, Negussie AH, Hong N, Hawken NM, Carlson CJ, Owen JW, Franco-Mahecha O, Wakim PG, Lewis AL, Pritchard WF, Karanian JW, Wood BJ. Evaluation of immune-modulating drugs for use in drug-eluting microsphere transarterial embolization. Int J Pharm. 2022 Mar 25;616:121466. doi: 10.1016/j.ijpharm.2022.121466. Epub 2022 Jan 20. PMID: 35065205; PMCID: PMC9139086. 2. Berggren O, Pucholt P, Amcoff C, Rönnblom L, Eloranta ML. Activation of plasmacytoid dendritic cells and B cells with two structurally different Toll-like receptor 7 agonists. Scand J Immunol. 2020 Jun;91(6):e12880. doi: 10.1111/sji.12880. Epub 2020 Apr 13. PMID: 32219875.
In vivo protocol:
1. Koga-Yamakawa E, Murata M, Dovedi SJ, Wilkinson RW, Ota Y, Umehara H, Sugaru E, Hirose Y, Harada H, Jewsbury PJ, Yamamoto S, Robinson DT, Li CJ. TLR7 tolerance is independent of the type I IFN pathway and leads to loss of anti-tumor efficacy in mice. Cancer Immunol Immunother. 2015 Oct;64(10):1229-39. doi: 10.1007/s00262-015-1730-4. Epub 2015 Jun 20. PMID: 26091797. 2. Nakamura T, Wada H, Kurebayashi H, McInally T, Bonnert R, Isobe Y. Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility. Bioorg Med Chem Lett. 2013 Feb 1;23(3):669-72. doi: 10.1016/j.bmcl.2012.11.114. Epub 2012 Dec 5. PMID: 23265901.
1: Mauda-Havakuk M, Hawken NM, Owen JW, Mikhail AS, Starost MF, Karim B, Wakim PG, Franco-Mahecha OL, Lewis AL, Pritchard WF, Karanian JW, Wood BJ. Immune Effects of Cryoablation in Woodchuck Hepatocellular Carcinoma. J Hepatocell Carcinoma. 2023 Nov 6;10:1973-1990. doi: 10.2147/JHC.S426442. PMID: 37954494; PMCID: PMC10637190. 2: Negussie AH, Mikhail AS, Owen JW, Hong N, Carlson CJ, Tang Y, Carrow KP, Mauda-Havakuk M, Lewis AL, Karanian JW, Pritchard WF, Wood BJ. In vitro characterization of immune modulating drug-eluting immunobeads towards transarterial embolization in cancer. Sci Rep. 2022 Dec 19;12(1):21886. doi: 10.1038/s41598-022-26094-1. Erratum in: Sci Rep. 2023 Mar 2;13(1):3559. doi: 10.1038/s41598-023-30659-z. PMID: 36535979; PMCID: PMC9763333. 3: Mikhail AS, Mauda-Havakuk M, Negussie AH, Hong N, Hawken NM, Carlson CJ, Owen JW, Franco-Mahecha O, Wakim PG, Lewis AL, Pritchard WF, Karanian JW, Wood BJ. Evaluation of immune-modulating drugs for use in drug-eluting microsphere transarterial embolization. Int J Pharm. 2022 Mar 25;616:121466. doi: 10.1016/j.ijpharm.2022.121466. Epub 2022 Jan 20. PMID: 35065205; PMCID: PMC9139086. 4: Berggren O, Pucholt P, Amcoff C, Rönnblom L, Eloranta ML. Activation of plasmacytoid dendritic cells and B cells with two structurally different Toll- like receptor 7 agonists. Scand J Immunol. 2020 Jun;91(6):e12880. doi: 10.1111/sji.12880. Epub 2020 Apr 13. PMID: 32219875. 5: Koga-Yamakawa E, Murata M, Dovedi SJ, Wilkinson RW, Ota Y, Umehara H, Sugaru E, Hirose Y, Harada H, Jewsbury PJ, Yamamoto S, Robinson DT, Li CJ. TLR7 tolerance is independent of the type I IFN pathway and leads to loss of anti- tumor efficacy in mice. Cancer Immunol Immunother. 2015 Oct;64(10):1229-39. doi: 10.1007/s00262-015-1730-4. Epub 2015 Jun 20. PMID: 26091797; PMCID: PMC11029383. 6: Adlard AL, Dovedi SJ, Telfer BA, Koga-Yamakawa E, Pollard C, Honeychurch J, Illidge TM, Murata M, Robinson DT, Jewsbury PJ, Wilkinson RW, Stratford IJ. A novel systemically administered Toll-like receptor 7 agonist potentiates the effect of ionizing radiation in murine solid tumor models. Int J Cancer. 2014 Aug 15;135(4):820-9. doi: 10.1002/ijc.28711. Epub 2014 Jan 17. PMID: 24390981; PMCID: PMC4286010. 7: Nakamura T, Wada H, Kurebayashi H, McInally T, Bonnert R, Isobe Y. Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility. Bioorg Med Chem Lett. 2013 Feb 1;23(3):669-72. doi: 10.1016/j.bmcl.2012.11.114. Epub 2012 Dec 5. PMID: 23265901.

View History

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KUN75125

ICI-130685

ICI-130685

FM04

FM04