Specification
Description
JMS-17-2 is a potent and selective antagonist of CX3CR1.
Synonyms
JMS-17-2; JMS172; JMS 17 2; JMS17-2; JMS-172; JMS 17-2; JMS-17 2
IUPAC Name
5-(3-(4-(4-Chlorophenyl)piperidin-1-yl)propyl)pyrrolo[1,2-a]quinoxalin-4(5H)-one
Canonical SMILES
O=C1C2=CC=CN2C3=C(C=CC=C3)N1CCCN4CCC(C5=CC=C(Cl)C=C5)CC4
InChI
InChI=1S/C25H26ClN3O/c26-21-10-8-19(9-11-21)20-12-17-27(18-13-20)14-4-16-29-23-6-2-1-5-22(23)28-15-3-7-24(28)25(29)30/h1-3,5-11,15,20H,4,12-14,16-18H2
InChI Key
WOSMCMULWWHMIV-UHFFFAOYSA-N
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM.
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 71.50; H, 6.24; Cl, 8.44; N, 10.01; O, 3.81
HS Tariff Code
2934.99.9001
In Vitro Activity
This study hypothesized that contact-independent proliferation might be more sensitive to CX3CR1 inhibition, so this study performed soft agar growth assays of PDAC cells with 21-26 d exposure to JMS-17-2. The small molecule antagonist potently inhibited colony formation of both AsPC-1 and MIAPaCa-2 cells with as little as 1 nM exposure (Fig. 4A and B).
Reference: Biochem Biophys Res Commun. 2018 Jan 15;495(3):2264-2269. https://pubmed.ncbi.nlm.nih.gov/29274778/
In Vivo Activity
These experiments showed that, in contrast to control animals presenting multiple tumors both in the skeleton and visceral sites, seven of the eight animals that received cancer cells pre-incubated with JMS-17-2 were found free of tumors (Fig. 4A and B). Notably, these animals were also found devoid of microscopic tumor foci and DTCs when inspected for fluorescent signals with multispectral microscopy-based imaging of frozen tissue sections (Fig. 4C).
Reference: Mol Cancer Res. 2016 Jun;14(6):518-27. https://pubmed.ncbi.nlm.nih.gov/27001765/
Shipping
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.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).