SR-717 lithium | CAS#2375421-09-1 | non-nucleotide STING agonist

MedKoo Cat#: 555833 | Name: SR-717 lithium

Description:

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

SR-717 is an agonist of stimulator of interferon genes STING for treating cancer. SR-717 demonstrates broad interspecies and interallelic specificity. 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.

Chemical Structure

SR-717 lithium

CAS#2375421-09-1 (lithium)

Theoretical Analysis

MedKoo Cat#: 555833

Name: SR-717 lithium

CAS#: 2375421-09-1 (lithium)

Chemical Formula: C15H8F2LiN5O3

Exact Mass: 0.0000

Molecular Weight: 351.20

Elemental Analysis: C, 51.30; H, 2.30; F, 10.82; Li, 1.98; N, 19.94; O, 13.67

Price and Availability

Size	Price	Availability
5mg	USD 90.00	Ready to ship
10mg	USD 150.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 450.00	Ready to ship
100mg	USD 750.00	Ready to ship
200mg	USD 1,350.00	Ready to ship
500mg	USD 2,950.00	Ready to ship

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Related CAS #

2375420-34-9 (free acid) 2375421-09-1 (lithium)

Synonym

SR-717 lithium; SR 717 lithium; SR717 lithium;

IUPAC/Chemical Name

lithium 2-(6-(1H-imidazol-1-yl)pyridazine-3-carboxamido)-4,5-difluorobenzoate

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

SMILES Code

O=C([O-])C1=CC(F)=C(F)C=C1NC(C2=NN=C(N3C=CN=C3)C=C2)=O.[Li+]

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

Stimulator of interferon genes (STING) links innate immunity to biological processes ranging from antitumor immunity to microbiome homeostasis. Mechanistic understanding of the anticancer potential for STING receptor activation is currently limited by metabolic instability of the natural cyclic dinucleotide (CDN) ligands.

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#A21T02K02

QC Data

View QC data: current batch, Lot#A21T02K02

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

SR-717 is a STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively.

In vitro activity:

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. Reference: Science. 2020 Aug 21;369(6506):993-999. https://pubmed.ncbi.nlm.nih.gov/32820126/

In vivo activity:

To be determined

	Solvent	mg/mL	mM
Solubility
	DMSO	17.5	49.83
	ethanol	0.0	0.00
	water	0.0	0.00

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 351.20 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.

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. Chin EN, Yu C, Vartabedian VF, Jia Y, Kumar M, Gamo AM, Vernier W, Ali SH, Kissai M, Lazar DC, Nguyen N, Pereira LE, Benish B, Woods AK, Joseph SB, Chu A, Johnson KA, Sander PN, Martínez-Peña F, Hampton EN, Young TS, Wolan DW, Chatterjee AK, Schultz PG, Petrassi HM, Teijaro JR, Lairson LL. Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic. Science. 2020 Aug 21;369(6506):993-999. doi: 10.1126/science.abb4255. PMID: 32820126.

In vitro protocol:

In vivo protocol:

To be determined

1: Chin EN, Yu C, Vartabedian VF, Jia Y, Kumar M, Gamo AM, Vernier W, Ali SH, Kissai M, Lazar DC, Nguyen N, Pereira LE, Benish B, Woods AK, Joseph SB, Chu A, Johnson KA, Sander PN, Martínez-Peña F, Hampton EN, Young TS, Wolan DW, Chatterjee AK, Schultz PG, Petrassi HM, Teijaro JR, Lairson LL. Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic. Science. 2020 Aug 21;369(6506):993-999. doi: 10.1126/science.abb4255. PMID: 32820126. 2: Caldwell SE, Janosko CP, Deiters A. Development of a light-activated STING agonist. Org Biomol Chem. 2024 Jan 3;22(2):302-308. doi: 10.1039/d3ob01578e. PMID: 38054844. 3: Wang H, Liu Z, Fang Y, Luo X, Zheng C, Xu Y, Zhou X, Yuan Q, Lv S, Ma L, Lao YH, Tao Y, Li M. Spatiotemporal release of non-nucleotide STING agonist and AKT inhibitor from implantable 3D-printed scaffold for amplified cancer immunotherapy. Biomaterials. 2024 Dec;311:122645. doi: 10.1016/j.biomaterials.2024.122645. Epub 2024 May 28. PMID: 38850717. 4: Li H, Zhang C, Chen Y, Xu Y, Yao W, Fan W. Biodegradable Long-Circulating Nanoagonists Optimize Tumor-Tropism Chemo-Metalloimmunotherapy for Boosted Antitumor Immunity by Cascade cGAS-STING Pathway Activation. ACS Nano. 2024 Aug 27;18(34):23711-23726. doi: 10.1021/acsnano.4c08463. Epub 2024 Aug 16. PMID: 39148423. 5: Zhou XW, Wang J, Tan WF. Apigenin Suppresses Innate Immune Responses and Ameliorates Lipopolysaccharide-Induced Inflammation via Inhibition of STING/IRF3 Pathway. Am J Chin Med. 2024;52(2):471-492. doi: 10.1142/S0192415X24500204. Epub 2024 Mar 14. PMID: 38480499. 6: Zou SS, Qiao Y, Zhu S, Gao B, Yang N, Liu YJ, Chen J. Intrinsic strategies for the evasion of cGAS-STING signaling-mediated immune surveillance in human cancer: How therapy can overcome them. Pharmacol Res. 2021 Apr;166:105514. doi: 10.1016/j.phrs.2021.105514. Epub 2021 Feb 23. PMID: 33631336. 7: Huang R, Shi Q, Zhang S, Lin H, Han C, Qian X, Huang Y, Ren X, Sun J, Feng N, Xia C, Shi M. Inhibition of the cGAS-STING Pathway Attenuates Lung Ischemia/Reperfusion Injury via Regulating Endoplasmic Reticulum Stress in Alveolar Epithelial Type II Cells of Rats. J Inflamm Res. 2022 Sep 5;15:5103-5119. doi: 10.2147/JIR.S365970. PMID: 36091334; PMCID: PMC9462969. 8: Lin C, He C, Li L, Liu Y, Tang L, Ni Z, Zhang N, Lai T, Chen X, Wang X. Alpha-lipoic acid (ALA) ameliorates early brain injury after subarachnoid hemorrhage in Sprague-Dawley (SD) rats via inhibiting STING-NLRP3 inflammatory signaling. Neuroreport. 2024 Mar 6;35(4):250-257. doi: 10.1097/WNR.0000000000001998. Epub 2024 Jan 15. PMID: 38305103; PMCID: PMC10852041. 9: Gao Y, Ling Y, Wu H, Zhang P, Zhou J, Gu H, Yang J, Zhou Y, Zhong Z, Chi J. Swimming training attenuates doxorubicin induced cardiomyopathy by targeting the mir-17-3p/KEAP1/NRF2 axis. Biochem Biophys Res Commun. 2024 Dec 20;739:150568. doi: 10.1016/j.bbrc.2024.150568. Epub 2024 Aug 19. PMID: 39178797. 10: Bi R, Yang Y, Liao H, Ji G, Ma Y, Cai L, Li J, Yang J, Sun M, Liang J, Shi L. Porphyromonas gingivalis induces an inflammatory response via the cGAS-STING signaling pathway in a periodontitis mouse model. Front Microbiol. 2023 Jun 19;14:1183415. doi: 10.3389/fmicb.2023.1183415. PMID: 37405166; PMCID: PMC10315844.