| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
JMS-17-2 is a novel, potent and selective antagonist of CX3CR1 with anticancer activity. It exhibits antitumor properties and inhibits CX3CR1 with an IC50 of 0.32 nM. In human breast tumors and skeletal metastases, CX3CR1 is overexpressed. JMS-17-2 treatment reduced the number of tumor foci and overall tumor burden in an animal model of MDA-231 tumors at least as well as CRISPRi treatment did. When considered collectively, these findings suggest that CX3CR1 plays a critical role in controlling the disseminated breast cancer cells' ability to seed, colonize, and spread.
| Targets |
CX3CR1 ( IC50 = 0.32 nM )
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|---|---|
| ln Vitro |
JMS-17-2 (10 mg/kg; intraperitoneal injection; twice daily for three days) significantly reduced the amount of tumors in the visceral and peripheral organs in SCID mice [1].
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| ln Vivo |
JMS-17-2 (10 mg/kg; intraperitoneal injection; twice daily for three days) resulted in significant reductions in peripheral and visceral organ tumors in SCID mice [1]. Animal model: SCID mouse (~25g) MDA-231 xenograft [1] Dose: 10 mg/kg Administration: intraperitoneal injection; twice daily for three weeks Results: Significant tumor growth in bones and visceral organs reduce.
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| Animal Protocol |
SCID mice (~25g) with MDA-231 xenograft
10 mg/kg Aministered i.p.; twice a day for three weeks |
| References |
| Molecular Formula |
C25H26CLN3O
|
|---|---|
| Molecular Weight |
419.95
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| Exact Mass |
419.176
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| Elemental Analysis |
C, 71.50; H, 6.24; Cl, 8.44; N, 10.01; O, 3.81
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| CAS # |
1380392-05-1
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| Related CAS # |
JMS-17-2 hydrochloride; 2341841-07-2
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| PubChem CID |
57382073
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
603.8±55.0 °C at 760 mmHg
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| Flash Point |
319.0±31.5 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.661
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| LogP |
4.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
585
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC(=CC=1)C1CCN(CCCN2C(C3=CC=CN3C3C=CC=CC2=3)=O)CC1
|
| InChi Key |
WOSMCMULWWHMIV-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
5-[3-[4-(4-chlorophenyl)piperidin-1-yl]propyl]pyrrolo[1,2-a]quinoxalin-4-one
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| Synonyms |
JMS-172; JMS-17-2; JMS172; JMS 17-2; JMS-17 2; JMS 17 2; JMS17-2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25~40 mg/mL (59.5~95.2 mM)
Ethanol: 10 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 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 (4.95 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3812 mL | 11.9062 mL | 23.8124 mL | |
| 5 mM | 0.4762 mL | 2.3812 mL | 4.7625 mL | |
| 10 mM | 0.2381 mL | 1.1906 mL | 2.3812 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.
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