| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
SR-717 lithium is a novel, potent and non-nucleotide STING (stimulator of interferon genes) agonist with anticancer activities. It has EC50 values of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 functions as a direct cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic that induces the same 'closed' conformation of STING. SR-717 displayed antitumor activity; promoted the activation of CD8+ T, natural killer, and dendritic cells in relevant tissues; and facilitated antigen cross-priming. SR-717 also induced the expression of clinically relevant targets, including programmed cell death 1 ligand 1 (PD-L1), in a STING-dependent manner.
| ln Vitro |
By using the same closed conformation sense, SR-717 activates STING, opening up possibilities for investigating systemic STING agonists in many settings, including as anti-tumor immunity [1]. Through STING signaling, SR-717 (3.8 μM) stimulates the expression of PD-L1 in THP1 cells and primary human peripheral blood mononuclear cells [1].
|
|---|---|
| ln Vivo |
SR-717 (30 mg/kg intraperitoneally once day for one week) in WT or Stinggt/gt mice exhibits antitumor action [1]. In addition to promoting natural activation of CD8+ T cells, killer and procytic cells in relevant tissues, and cross-priming, SR-717 (30 mg/kg intraperitoneally for 7 days) demonstrates anti-tumor efficacy [1].
|
| Animal Protocol |
Animal/Disease Models: WT or Stinggt/gt mice [1] Usage and
Doses: 30 mg/kg Route of Administration: intraperitoneally (ip) (ip); one time/day for 1 week. Experimental Results: Maximum inhibition of tumor growth. |
| References |
[1]. Emily N Chin, et al. Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic. Science. 2020 Aug 21;369(6506):993-999.
|
| Molecular Formula |
C15H8F2LIN5O3MOLECULARWEIGHT
|
|---|---|
| Molecular Weight |
351.1935
|
| CAS # |
2375421-09-1
|
| Related CAS # |
SR-717 free acid;2375420-34-9
|
| SMILES |
O=C([O-])C1=CC(F)=C(F)C=C1NC(C2=NN=C(N3C=CN=C3)C=C2)=O.[Li+]
|
| InChi Key |
ODSAJRWPLSVEHJ-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C15H9F2N5O3.Li/c16-9-5-8(15(24)25)12(6-10(9)17)19-14(23)11-1-2-13(21-20-11)22-4-3-18-7-22/h1-7H,(H,19,23)(H,24,25)/q+1/p-1
|
| Chemical Name |
lithium 2-(6-(1H-imidazol-1-yl)pyridazine-3-carboxamido)-4,5-difluorobenzoate
|
| Synonyms |
SR-717 lithium SR 717 lithium SR717 lithium
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~20.83 mg/mL (~59.31 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.92 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10 mg/mL (28.47 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8475 mL | 14.2373 mL | 28.4746 mL | |
| 5 mM | 0.5695 mL | 2.8475 mL | 5.6949 mL | |
| 10 mM | 0.2847 mL | 1.4237 mL | 2.8475 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA