SR-717 lithium


Catalog No. size PriceQuantity
M7039-2 2mg solid $127
M7039-10 10mg solid $531

Description

Cas:2375421-09-1 (lithium)

Product Information

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 Formula: C15H8F2LiN5O3

 

Molecular Weight: 351.1978

 

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

 

Synonym: 

 

SR-717 lithium

SR 717 lithium

SR717 lithium

 

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+]

 

 

Technical Data:

 

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

 

In Vitro

SR-717 activates STING by inducing the same closed conformation, which thereby provides an avenue to explore this class of systemic STING agonist in diverse contexts, including antitumor immunity.

SR-717 (3.8 μM) induces the expression of PD-L1 in THP1 cells and in primary human peripheral blood mononuclear cells in a STING-dependent manner.

 

In Vivo

SR-717 (30 mg/kg intraperitoneal once-per-day for 1 week) shows antitumor activities in WT or Stinggt/gt mice.

SR-717 (30 mg/kg intraperitoneally for 7 days) displays antitumor activity; promots the activation of CD8+ T, natural killer, and dendritic cells in relevant tissues; and facilitates antigen cross-priming.

 

 

References

 

  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.

 

Products are for research use only. Not for human use.

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